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(+)-canadaline
41.02% inhibition at 0.005 mM
(+)-corynoline
21.91% inhibition at 0.005 mM
(+)-N-((4S,4aS,6S,8aR)-10-amino-4,4a,5,6,7,8-hexahydro-1H,3H-4,8a-(epithiomethenoazeno)isochromen-6-yl)-3-chlorobenzamide
-
(+/-)-corycavidine
26.87% inhibition at 0.005 mM
(-)-corycavamine
34.4% inhibition at 0.005 mM
(-)-isocorypalmine
26.68% inhibition at 0.005 mM
(-)-scoulerine
24.34% inhibition at 0.005 mM
(1R,4S,5R,7R)-3,4-dibenzyl-2-oxo-N-(prop-2-yn-1-yl)-6,8-dioxa-3-azabicyclo[3.2.1]octane-7-carboxamide
32% inhibition at 0.01 mM
(1R,4S,5R,7R)-3,4-dibenzyl-7-(piperidin-1-ylcarbonyl)-6,8-dioxa-3-azabicyclo[3.2.1]octan-2-one
46% inhibition at 0.01 mM
(1R,5R,7R)-3-benzyl-7-(piperidin-1-ylcarbonyl)-6,8-dioxa-3-azabicyclo[3.2.1]octan-2-one
10% inhibition at 0.01 mM
(1R,5R,7R)-3-benzyl-N-[(2S)-1-hydroxy-4-methylpentan-2-yl]-2-oxo-6,8-dioxa-3-azabicyclo[3.2.1]octane-7-carboxamide
8% inhibition at 0.01 mM
(2R,4S)-N-butyl-4-hydroxy-2-methyl-4-[(2S,5S,7R)-1,2,7-trimethyl-3,16-dioxo-1,4-diazacyclohexadecan-5-yl]butanamide
56fold selectivity for beta-secretase over cathepsin D
(2R,4S)-N-butyl-4-[(2S,5S,7R)-2,7-dimethyl-3,15-dioxo-1,4-diazacyclopentadecan-5-yl]-4-hydroxy-2-methylbutanamide
-
(2R,4S)-N-butyl-4-[(2S,5S,7R)-2,7-dimethyl-3,16-dioxo-1,4-diazacyclohexadecan-5-yl]-4-hydroxy-2-methylbutanamide
-
(2S)-2-((3R)-3-acetamido-3-isobutyl-2-oxo-1-pyrrolidinyl)-N-((1S,2R)-1-(3,5-difluorobenzyl)-2-hydroxy-2-(1,2,3,4-tetrahydro-3-isoquinolinyl)ethyl)-4-phenylbutanamide
crystallization data, EC50 value for HEK293 cells 10 nM
(2S)-2-((S)-3-acetamido-3-((R)-sec-butyl)-2-oxopyrrolidin-1-yl)-N-((1S,2S)-3-(3,5-difluorophenyl)-1-hydroxy-1-((2R)-5-(propylsulfonyl)pyrrolidin-2-yl)propan-2-yl)-4-phenylbutanamide
EC50 value for HEK293 cells 5 nM, shows apical to basolateral permeability of <15 nm/s in the bi-directional Caco-2 model
(2S,5S,8S,11S,14S)-14-amino-5-benzyl-8-(cyclohexylmethyl)-16-(5-fluoro-2,6-dioxo-1,2,3,6-tetrahydropyrimidin-4-yl)-2-hydroxy-11-(1-methylethyl)-4,7,10,13,16-pentaoxo-N-[3-(2H-tetrazol-5-yl)phenyl]-3,6,9,12-tetraazahexadecan-1-amide
i.e. KMI-574, 100% and 97% inhibition at 2 microM and 0.2 microM, respectively, 84% inhibition of beta-secretase BACE1 in cultured cell-based assay at 100 microM
(3aR,6aS)-N-[(2R)-1-([(2S,3R)-3-hydroxy-4-[(3-methoxybenzyl)amino]-1-phenylbutan-2-yl]amino)-3-(methylsulfonyl)-1-oxopropan-2-yl]-3a,4,5,6a-tetrahydrofuro[3,2-d][1,2]oxazole-3-carboxamide
-
(3aR,6aS)-N-[(4R,7S,8S,10R,13S)-8-hydroxy-10,17-dimethyl-7-(2-methylpropyl)-2,2-dioxido-5,11,14-trioxo-13-(propan-2-yl)-2l6-thia-6,12,15-triazaoctadecan-4-yl]-3a,4,5,6a-tetrahydrofuro[3,2-d][1,2]oxazole-3-carboxamide
-
(3aR,6aS)-N-[(4R,7S,8S,10R,13S)-8-hydroxy-10,17-dimethyl-7-(2-methylpropyl)-5,11,14-trioxo-13-(propan-2-yl)-2-thia-6,12,15-triazaoctadecan-4-yl]-3a,4,5,6a-tetrahydrofuro[3,2-d][1,2]oxazole-3-carboxamide
-
(3aR,7aS)-N-[(4R,7S,8S,10R,13S)-8-hydroxy-10,17-dimethyl-7-(2-methylpropyl)-2,2-dioxido-5,11,14-trioxo-13-(propan-2-yl)-2l6-thia-6,12,15-triazaoctadecan-4-yl]-3a,5,6,7a-tetrahydro-4H-pyrano[3,2-d][1,2]oxazole-3-carboxamide
-
(3aS,6aR)-N-[(2R)-1-([(2S,3R)-3-hydroxy-4-[(3-methoxybenzyl)amino]-1-phenylbutan-2-yl]amino)-3-(methylsulfonyl)-1-oxopropan-2-yl]-3a,4,5,6a-tetrahydrofuro[3,2-d][1,2]oxazole-3-carboxamide
-
(3aS,6aR)-N-[(4R,7S,8S,10R,13S)-8-hydroxy-10,17-dimethyl-7-(2-methylpropyl)-2,2-dioxido-5,11,14-trioxo-13-(propan-2-yl)-2l6-thia-6,12,15-triazaoctadecan-4-yl]-3a,4,5,6a-tetrahydrofuro[3,2-d][1,2]oxazole-3-carboxamide
-
(3aS,6aR)-N-[(4R,7S,8S,10R,13S)-8-hydroxy-10,17-dimethyl-7-(2-methylpropyl)-5,11,14-trioxo-13-(propan-2-yl)-2-thia-6,12,15-triazaoctadecan-4-yl]-3a,4,5,6a-tetrahydrofuro[3,2-d][1,2]oxazole-3-carboxamide
-
(3aS,7aR)-N-[(4R,7S,8S,10R,13S)-8-hydroxy-10,17-dimethyl-7-(2-methylpropyl)-2,2-dioxido-5,11,14-trioxo-13-(propan-2-yl)-2l6-thia-6,12,15-triazaoctadecan-4-yl]-3a,5,6,7a-tetrahydro-4H-pyrano[3,2-d][1,2]oxazole-3-carboxamide
-
(3S,14R,16S)-16-[(1R)-1-hydroxy-2-([3-(1-methylethyl)benzyl]amino)ethyl]-3,4,14-trimethyl-1,4-diazacyclohexadecane-2,5-dione
60fold preference for beta-secretase over cathepsin D
(3S,14R,16S)-16-[(1S)-2-[[(1R)-3,3-dimethyl-7-(1-methylethyl)-1,2,3,4-tetrahydronaphthalen-1-yl]amino]-1-hydroxyethyl]-3,4,14-trimethyl-1,4-diazacyclohexadecane-2,5-dione
inhibitory similarly to beta-sectretase and cathepsin D
(3S,5R)-3-(4-amino-3-fluoro-5-[[(2R)-1,1,1-trifluoro-3-hydroxypropan-2-yl]oxy]benzyl)-5-[(3-tert-butylbenzyl)amino]-4-hydroxytetrahydro-2H-thiopyranium-1-olate
highly potent, selective inhibitors with improved cellular activity. Sufficient central nervous system exposure can be achieved with a single oral dose of 60 micromol/kg to effect significant reduction in brain amyloid beta in APP51/16 transgenic mice
(4aR,6R,8aS)-8a-(2,4-difluorophenyl)-6-(fluoromethyl)-4,4a,5,6,8,8a-hexahydropyrano[3,4-d][1,3]thiazin-2-amine
upon oral administration, inhibitor exhibits robust brain availability and is efficacious in lowering central amyloid beta levels in mouse and dog. Chronic treatment in aged PS1/APP mice effects a decrease in the number and size of amyloid-beta-derived plaques. Evaluation of the inhibitor in a 2-week exploratory toxicology study exhibits no accumulation of autofluorescent material in retinal pigment epithelium or histology findings in the eye
(4aS,4'S,10aR)-8-(2-fluoropyridin-3-yl)-4a-methyl-3,4,4a,10a-tetrahydro-2H,5'H-spiro[pyrano[3,2-b]chromene-10,4'-thiazol]-2'-amine
compound demonstrates a 69% reduction in rat cerebrospinal fluid amyloid beta1?40 at 60 mg/kg
(5S)-2-amino-5-[3-fluoro-5-(2-fluoropyridin-3-yl)phenyl]-5-(4-methoxy-3-methylphenyl)-3-methyl-3,5-dihydro-4H-imidazol-4-one
aminohydantoin inhibitor, EC50 value in ELISA-assay 20 nM, and demonstrates more than 100fold selectivity for the other structurally related aspartyl proteases BACE2, cathepsinD, renin, and pepsin
(6R)-2-amino-3,6-dimethyl-6-(2-phenylethyl)-5,6-dihydropyrimidin-4(3H)-one
-
(6R)-2-amino-6-[2-(3'-methoxybiphenyl-4-yl)ethyl]-3,6-dimethyl-5,6-dihydropyrimidin-4(3H)-one
-
(6R)-2-amino-6-[2-(biphenyl-4-yl)ethyl]-3,6-dimethyl-5,6-dihydropyrimidin-4(3H)-one
-
(6S)-2-amino-6-(3'-methoxybiphenyl-3-yl)-3,6-dimethyl-5,6-dihydropyrimidin-4(3H)-one
-
(R)-N-(3-(3-amino-1-methyl-9-oxa-4-thia-2-azaspiro[5.5]undec-2-en-1-yl)-4-fluorophenyl)-5-(fluoromethoxy)pyrazine-2-carboxamide
-
(R)-N-(3-(3-amino-5-methyl-9,9-dioxido-2,9-dithia-4-azaspiro[5.5]undec-3-en-5-yl)-4-fluorophenyl)-5-(fluoromethoxy)pyrazine-2-carboxamide
-
(R)-N-(3-(3-amino-9,9-difluoro-5-methyl-2-thia-4-azaspiro[5.5]undec-3-en-5-yl)-4-fluorophenyl)-5-(fluoromethoxy)pyrazine-2-carboxamide
-
(R)-N-(3-(7-amino-2,2-difluoro-9-methyl-6-thia-8-azaspiro[3.5]non-7-en-9-yl)-4-fluorophenyl)-5-(fluoromethoxy)pyrazine-2-carboxamide
-
(S)-3-(6,6-dimethyl-3,6-dihydro-2H-pyran-4-yl)-7-(2-fluoropyridin-3-yl)-5'H-spiro[chromeno[2,3-b]pyridine-5,4'-oxazol]-2'-amine
inhibitor shows good BACE1 functional potency, permeability, intrinsic stability, and P-glycoprotein efflux ratios
(S)-7-(2-fluoropyridin-3-yl)-3-((3-methyloxetan-3-yl)ethynyl)-5H-spiro[chromeno[2,3-b]pyridine-5,4-oxazol]-2-amine
i.e. AMG-8718.compound exhibits a balanced profile of BACE1 potency, hERG binding affinity, and P-glycoprotein recognition. Compound produces robust and sustained reductions of cerebrospinal fluid and brain amyloid beta levels in a rat pharmacodynamic model
(S)-N-(3-(2-amino-4-methyl-5,6-dihydro-4H-1,3-thiazin-4-yl)-4-fluorophenyl)-5-(2,2,2-trifluoroethoxy)pyrazine-2-carboxamide
-
(S)-N-(3-(2-amino-4-methyl-5,6-dihydro-4H-1,3-thiazin-4-yl)-4-fluorophenyl)-5-(difluoromethyl)pyrazine-2-carboxamide
-
(S)-N-(3-(2-amino-4-methyl-5,6-dihydro-4H-1,3-thiazin-4-yl)-4-fluorophenyl)-5-(fluoromethoxy)pyrazine-2-carboxamide
-
(S)-N-(3-(2-amino-4-methyl-5,6-dihydro-4H-1,3-thiazin-4-yl)-4-fluorophenyl)-5-chloropicolinamide
-
(S)-N-(3-(2-amino-4-methyl-5,6-dihydro-4H-1,3-thiazin-4-yl)-4-fluorophenyl)-5-cyanopicolinamide
-
(S)-N-(3-(2-amino-4-methyl-5,6-dihydro-4H-1,3-thiazin-4-yl)-4-fluorophenyl)-5-fluoropicolinamide
-
(S)-N-(3-(2-amino-4-methyl-5,6-dihydro-4H-1,3-thiazin-4-yl)-4-fluorophenyl)-5-methoxypyrazine-2-carboxamide
-
1,3-bis(3,5-bis(trifluoromethyl)phenyl)urea
100% inhibition at 100 nM, 15% inhibition at 10 nM
1-(3,5-bis(trifluoromethyl)-phenyl)-3-(3,5-dimethylphenyl)urea
80% inhibition at 100 nM
15,16-dihydrotanshinone
-
2,3-dihydro-6-methylginkgetin
isolated from from Cephalotaxus harringtonia var. fastigiata
2,3-dihydroamentoflavone
a 2,3-dihydroamentoflavone from Cycas revoluta
2-((4-amino-6-oxo-1,6-dihydropyrimidin-2-yl)thio)eN-(4-phenylthiazol-2-yl)acetamide
17.8% inhibition at 0.05 mM
2-((5-amino-1,3,4-thiadiazol-2-yl)thio)eN-(4-phenylthiazol-2-yl)acetamide
21.8% inhibition at 0.05 mM
2-((5-cyano-4-(2-methoxyphenyl)-6-oxo-1,6-dihydropyrimidin-2-yl)thio)eN-(4-(3-nitrophenyl)thiazol-2-yl)acetamide
62.4% inhibition at 0.05 mM
2-((5-cyano-4-(2-methoxyphenyl)-6-oxo-1,6-dihydropyrimidin-2-yl)thio)eN-(4-(4-nitrophenyl)thiazol-2-yl)acetamide
77.5% inhibition at 0.05 mM
2-((5-cyano-4-(2-methoxyphenyl)-6-oxo-1,6-dihydropyrimidin-2-yl)thio)eN-(4-phenylthiazol-2-yl)acetamide
25.9% inhibition at 0.05 mM
2-((5-cyano-4-(3-ethoxyphenyl)-6-oxo-1,6-dihydropyrimidin-2-yl)thio)eN-(4-(4-methoxyphenyl)thiazol-2-yl)acetamide
9.4% inhibition at 0.05 mM
2-((5-cyano-4-(3-ethoxyphenyl)-6-oxo-1,6-dihydropyrimidin-2-yl)thio)eN-(4-(4-nitrophenyl)thiazol-2-yl)acetamide
85.6% inhibition at 0.05 mM
2-((5-cyano-4-(3-ethoxyphenyl)-6-oxo-1,6-dihydropyrimidin-2-yl)thio)eN-(4-(p-tolyl)thiazol-2-yl)acetamide
11.5% inhibition at 0.05 mM
2-((5-cyano-4-(3-ethoxyphenyl)-6-oxo-1,6-dihydropyrimidin-2-yl)thio)eN-(4-phenyl-1H-imidazol-2-yl)acetamide
84.5% inhibition at 0.01 mM
2-((5-cyano-4-(3-methoxyphenyl)-6-oxo-1,6-dihydropyrimidin-2-yl)thio)eN-(4-(2-nitrophenyl)thiazol-2-yl)acetamide
6.5% inhibition at 0.05 mM
2-((5-cyano-4-(3-methoxyphenyl)-6-oxo-1,6-dihydropyrimidin-2-yl)thio)eN-(4-(3-(2-fluoropyridin-3-yl)phenyl)thiazol-2-yl)acetamide
88.7% inhibition at 0.05 mM
2-((5-cyano-4-(3-methoxyphenyl)-6-oxo-1,6-dihydropyrimidin-2-yl)thio)eN-(4-(3-nitrophenyl)thiazol-2-yl)acetamide
78.5% inhibition at 0.05 mM
2-((5-cyano-4-(3-methoxyphenyl)-6-oxo-1,6-dihydropyrimidin-2-yl)thio)eN-(4-(4-methoxyphenyl)thiazol-2-yl)acetamide
16.5% inhibition at 0.05 mM
2-((5-cyano-4-(3-methoxyphenyl)-6-oxo-1,6-dihydropyrimidin-2-yl)thio)eN-(4-(4-nitrophenyl)thiazol-2-yl)acetamide
83.9% inhibition at 0.05 mM
2-((5-cyano-4-(3-methoxyphenyl)-6-oxo-1,6-dihydropyrimidin-2-yl)thio)eN-(4-(p-tolyl)thiazol-2-yl)acetamide
8.1% inhibition at 0.05 mM
2-((5-cyano-4-(3-methoxyphenyl)-6-oxo-1,6-dihydropyrimidin-2-yl)thio)eN-(4-phenyl-1H-imidazol-2-yl)acetamide
78.6% inhibition at 0.01 mM
2-((5-cyano-4-(3-methoxyphenyl)-6-oxo-1,6-dihydropyrimidin-2-yl)thio)eN-(4-phenylthiazol-2-yl)acetamide
50.7% inhibition at 0.05 mM
2-((5-cyano-4-(4-methoxyphenyl)-6-oxo-1,6-dihydropyrimidin-2-yl)thio)eN-(4-(3-nitrophenyl)thiazol-2-yl)acetamide
12.3% inhibition at 0.01 mM
2-((5-cyano-4-(4-methoxyphenyl)-6-oxo-1,6-dihydropyrimidin-2-yl)thio)eN-(4-(4-nitrophenyl)thiazol-2-yl)acetamide
5.9% inhibition at 0.01 mM
2-((5-cyano-4-(4-methoxyphenyl)-6-oxo-1,6-dihydropyrimidin-2-yl)thio)eN-(4-phenylthiazol-2-yl)acetamide
10.7% inhibition at 0.05 mM
2-((5-cyano-6-oxo-4-(3-(trifluoromethoxy)phenyl)-1,6-dihydropyrimidin-2-yl)thio)eN-(4-phenylthiazol-2-yl)acetamide
85.8% inhibition at 0.05 mM
2-((5-cyano-6-oxo-4-(3-(trifluoromethyl)phenyl)-1,6-dihydropyrimidin-2-yl)thio)eN-(4-phenylthiazol-2-yl)acetamide
82.5% inhibition at 0.05 mM
2-((6-oxo-1,6-dihydropyrimidin-2-yl)thio)eN-(4-phenylthiazol-2-yl)acetamide
22.5% inhibition at 0.05 mM
2-(2-(4-(6-bromo-3-(tert-butylamino)imidazo[1,2-a]pyridin-2-yl)phenoxy)propyl)isoindoline-1,3-dione
34.28% inhibition at 0.05 mM
2-(3-(4-(3-(cyclohexylamino)-5-methylimidazo[1,2-a]pyridin-2-yl)phenoxy)propyl)isoindoline-1,3-dione
87.94% inhibition at 0.05 mM
2-(3-(4-(3-(cyclohexylamino)-6-methylimidazo[1,2-a]pyridin-2-yl)phenoxy)propyl)isoindoline-1,3-dione
63.7% inhibition at 0.05 mM
2-(3-(4-(3-(cyclohexylamino)-7-methylimidazo[1,2-a]pyridin-2-yl)phenoxy)propyl)isoindoline-1,3-dione
complete inhibition at 0.05 mM
2-(3-(4-(3-(cyclohexylamino)-8-methylimidazo[1,2-a]pyridin-2-yl)phenoxy)propyl)isoindoline-1,3-dione
69.43% inhibition at 0.05 mM
2-(3-(4-(3-(cyclohexylamino)imidazo[1,2-a]pyridin-2-yl)-2-methoxyphenoxy)propyl)isoindoline-1,3-dione
69.49% inhibition at 0.05 mM
2-(3-(4-(3-(cyclohexylamino)imidazo[1,2-a]pyridin-2-yl)phenoxy)propyl)isoindoline-1,3-dione
less than 10% inhibition at 0.05 mM
2-(3-(4-(3-(tert-butylamino)-6-chloroimidazo[1,2-a]pyridin-2-yl)-2-methoxyphenoxy)propyl)isoindoline-1,3-dione
37.9% inhibition at 0.05 mM
2-(3-(4-(3-(tert-butylamino)-6-chloroimidazo[1,2-a]pyridin-2-yl)phenoxy)propyl)isoindoline-1,3-dione
32.95% inhibition at 0.05 mM
2-(3-(4-(3-(tert-butylamino)-7-methylimidazo[1,2-a]pyridin-2-yl)phenoxy)propyl)isoindoline-1,3-dione
24.24% inhibition at 0.01 mM
2-(3-(4-(6-bromo-3-(cyclohexylamino)imidazo[1,2-a]pyridin-2-yl)-2-methoxyphenoxy)propyl) isoindoline-1,3-dione
43.17% inhibition at 0.05 mM
2-(3-(4-(6-bromo-3-(cyclohexylamino)imidazo[1,2-a]pyridin-2-yl)phenoxy)propyl)isoindoline-1,3-dione
45.3% inhibition at 0.05 mM
2-(3-(4-(6-bromo-3-(tert-butylamino)imidazo[1,2-a]pyridin-2-yl)-2-methoxyphenoxy)propyl) isoindoline-1,3-dione
48.72% inhibition at 0.05 mM
2-(3-(4-(6-chloro-3-(cyclohexylamino)imidazo[1,2-a]pyridin-2-yl)-2-methoxyphenoxy)propyl) isoindoline-1,3-dione
88.097% inhibition at 0.05 mM
2-(3-(4-(6-chloro-3-(cyclohexylamino)imidazo[1,2-a]pyridin-2-yl)phenoxy)propyl)isoindoline-1,3-dione
19.6% inhibition at 0.05 mM
2-(3-(imidazo[1,2-a]pyridin-2-yl)phenyl)-6-methoxy-1Hbenzo[d]imidazole
inhibitor of BACE1, EC 3.4.23.46. 150fold more effective on BACE1 than BACE2
2-amino-3-methyl-6-(naphthalen-2-ylmethyl)pyrimidin-4(3H)-one
-
2-amino-3-[(1R)-1-cyclohexyl-2-[(cyclohexylcarbonyl)amino]ethyl]-6-phenoxyquinazolin-3-ium
-
2-amino-4a,5,6,7,8,8a-hexahydro-4H-3,1-benzothiazin-6-yl 3-chlorobenzoate
-
2-amino-5-[4-fluoro-3-(pyrimidin-5-yl)phenyl]-5-(4-methoxy-3-methylphenyl)-3-methyl-3,5-dihydro-4H-imidazol-4-one
aminohydantoin inhibitor, shows comparable activity in a cell-based assay, and demonstrates more than 100fold selectivity for the other structurally related aspartyl proteases BACE2, cathepsinD, renin, and pepsin
2-amino-6-(3a,7a-dihydro-1H-indol-6-ylmethyl)-3-methylpyrimidin-4(3H)-one
-
2-amino-6-(3a,7a-dihydro-1H-indol-6-ylmethyl)pyrimidin-4(3H)-one
-
2-amino-6-benzyl-3-methylpyrimidin-4(3H)-one
-
2-amino-8-(2-nitrophenyl)-9-phenyl-1,9-dihydro-6H-purin-6-one
-
2-amino-8-(4-bromophenyl)-9-phenyl-1,9-dihydro-6H-purin-6-one
-
2-[[(1S,2S)-1-benzyl-2-hydroxy-3-oxo-3-[[3-(2H-tetrazol-5-yl)phenyl]amino]propyl]carbamoyl]-6-[[(4S)-4-phenyl-1,3-oxazolidin-3-yl]carbonyl]pyridin-4-yl methanesulfonate
i.e. KMI-1036, BACE1 inhibitors with a 5-membered ring at the P3 position and their BACE1 inhibitory activities summarized
3-(5-((7aR)-6-(5-fluoropyrimidin-2-yl)-2-imino-3-methyl-4-oxooctahydro-1H-pyrrolo[3,4-d]pyrimidin-7a-yl)thiophen-3-yl)benzonitrile
orally active, brain penetrant inhibitor that reduces amyloid beta40 in the plasma, cerebrospinal fluid, and cortex of rats in a dose-dependent manner
3-[(2H-tetrazol-5-ylcarbonyl)amino]-L-alanyl-L-valyl-N-((1S,2R)-1-benzyl-3-[(3,5-di-2H-tetrazol-5-ylphenyl)amino]-2-hydroxy-3-oxopropyl)-L-leucinamide
i.e. KMI-684, beta-secretase inhibitors with a hydroxymethylcarbonyl (HMC) isostere, inihbitory activities optimized
3-[(2H-tetrazol-5-ylcarbonyl)amino]-L-alanyl-L-valyl-N-((1S,2R)-1-benzyl-3-[(3,5-dicarboxyphenyl)amino]-2-hydroxy-3-oxopropyl)-L-leucinamide
i.e. KMI-429, beta-secretase inhibitors with a hydroxymethylcarbonyl (HMC) isostere, inihbitory activities optimized
3-[(2H-tetrazol-5-ylcarbonyl)amino]-L-alanyl-L-valyl-N-((1S,2R)-1-benzyl-3-[(3-carboxyphenyl)amino]-2-hydroxy-3-oxopropyl)-L-leucinamide
i.e. KMI-420, beta-secretase inhibitors with a hydroxymethylcarbonyl (HMC) isostere, inihbitory activities optimized
3-[(2H-tetrazol-5-ylcarbonyl)amino]-L-alanyl-L-valyl-N-[(1S,2R)-1-benzyl-2-hydroxy-3-oxo-3-([3-(2H-tetrazol-5-yl)phenyl]amino)propyl]-L-leucinamide
i.e. KM-570, beta-secretase inhibitors with a hydroxymethylcarbonyl (HMC) isostere, inihbitory activities optimized
4',5,7-trimethoxyflavone
-
4-[2-(2,6-diethylpyridin-4-yl)-5-(pyrimidin-5-yl)phenyl]-1-methyl-4,5-dihydro-1H-imidazol-2-amine
-
4a,5,6,7,8,8a-hexahydro-4H-3,1-benzothiazin-2-amine
-
5-[(E)-benzylideneamino]-6-methoxy-N4-phenylpyrimidine-2,4-diamine
-
5-[(E)-[(2,4,-diclorophenyl)methylidene]amino]-6-methoxy-N4-phenylpyrimidine-2,4-diamine
-
5-[(E)-[(2-chlorophenyl)methylidene]amino]-6-methoxy-N4-phenylpyrimidine-2,4-diamine
-
6-fluoro-2-(3-(7-fluoroimidazo[1,2-a]pyridin-2-yl)phenyl)-1H-benzo[d]imidazole
inhibitor of BACE1, EC 3.4.23.46. 200fold more effective on BACE1 than BACE2
6-fluoro-2-(3-(imidazo[1,2-a]pyridin-2-yl)phenyl)-1H-benzo-[d]imidazole
inhibitor of BACE1, EC 3.4.23.46. 100fold more effective on BACE1 than BACE2
6-methoxy-5-[(E)-(4-methylbenzylidene)amino]-N4-phenylpyrimidine-2,4-diamine
-
6-methoxy-5-[(E)-[(2-nitrophenyl)methylidene]amino]-N4-phenylpyrimidine-2,4-diamine
-
6-methoxy-N4-phenyl-5-[(E)-[4-(trifluoromethyl)benzylidene]amino]pyrimidine-2,4-diamine
-
6-[(3R,4S)-3-benzyl-4-hydroxy-5-oxo-5-[[3-(2H-tetrazol-5-yl)phenyl]amino]pentanoyl]-N-[(1R)-1-(4-fluorophenyl)ethyl]-4-oxo-4H-pyran-2-carboxamide
76% inhibition at 2 microM
Allocryptopine
26.18% inhibition at 0.005 mM
chitosan oligosaccharide
IC50 of 0.098 mg/ml
deoxyneocryptotanshinone
mixed-type inhibition
ethyl 4-[[(1R,4S,5R,7R)-3,4-dibenzyl-2-thioxo-6,8-dioxa-3-azabicyclo[3.2.1]oct-7-yl]carbonyl]piperazine-1-carboxylate
9% inhibition at 0.01 mM
ethyl 4-[[(1R,5R,7R)-3-benzyl-2-thioxo-6,8-dioxa-3-azabicyclo[3.2.1]oct-7-yl]carbonyl]piperazine-1-carboxylate
29% inhibition at 0.01 mM
GRL-8234
i.e. inhibitor 24, inhibitory and cellular assays described
KTEETSEVN(statine)VAEF
i.e. P10-P40 StatVal, activity completely abolished using saturating dose of 2.1 microM of the inhibitor, cleavage products of beta-secretase measured by fluoresence assay
magnesium lithospermate
-
methyl (1R,4S,5R,7R)-3,4-dibenzyl-2-thioxo-6,8-dioxa-3-azabicyclo[3.2.1]octane-7-carboxylate
16% inhibition at 0.01 mM
methyl (1R,5R,7R)-3-benzyl-2-thioxo-6,8-dioxa-3-azabicyclo[3.2.1]octane-7-carboxylate
16% inhibition at 0.01 mM
methyl (1S,4R,5S,7S)-3,4-dibenzyl-2-thioxo-6,8-dioxa-3-azabicyclo[3.2.1]octane-7-carboxylate
16% inhibition at 0.01 mM
N'-[(2S,3R)-3-hydroxy-4-([(2S,3S)-3-hydroxy-1-[(2-methylpropyl)amino]-1-oxobutan-2-yl]amino)-1-phenylbutan-2-yl]-N,5-dimethyl-N-[(1R)-1-phenylethyl]benzene-1,3-dicarboxamide
-
N'-[(2S,3R)-3-hydroxy-4-([(2S,3S)-3-hydroxy-1-[(2-methylpropyl)amino]-1-oxobutan-2-yl]amino)-1-phenylbutan-2-yl]-N-methyl-5-[methyl(methylsulfonyl)amino]-N-[(1R)-1-phenylethyl]benzene-1,3-dicarboxamide
-
N'-[(2S,3R)-3-hydroxy-4-([(2S,3S)-3-hydroxy-1-[(2-methylpropyl)amino]-1-oxohexan-2-yl]amino)-1-phenylbutan-2-yl]-N,5-dimethyl-N-[(1R)-1-phenylethyl]benzene-1,3-dicarboxamide
-
N'-[(2S,3R)-3-hydroxy-4-([(2S,3S)-3-hydroxy-1-[(2-methylpropyl)amino]-1-oxohexan-2-yl]amino)-1-phenylbutan-2-yl]-N-methyl-N-[(1R)-1-phenylethyl]benzene-1,3-dicarboxamide
-
N'-[(2S,3R)-3-hydroxy-4-[(3-methoxybenzyl)amino]-1-phenylbutan-2-yl]-N,5-dimethyl-N-[(1R)-1-phenylethyl]benzene-1,3-dicarboxamide
-
N-((4aRS,6RS,8aSR)-2-amino-5,6,7,8-tetrahydro-4H-4a,8a-(methanooxymethano)benzo[d][1,3]thiazin-6-yl)-3-chlorobenzamide
-
N-(2-amino-4a,5,6,7,8,8a-hexahydro-4H-3,1-benzothiazin-6-yl)-3-chlorobenzamide
-
N-(2-amino-4a,5,6,7,8,8a-hexahydro-4H-3,1-benzothiazin-6-yl)-5-fluoropyridine-2-carboxamide
-
N-(2-amino-4a,5,6,7,8,8a-hexahydro-4H-3,1-benzothiazin-6-yl)benzamide
-
N-(3-((4R,5R)-2-amino-5-methoxy-4-methyl-5,6-dihydro-4H-1,3-thiazin-4-yl)-4-fluorophenyl)-5-(fluoromethoxy)pyrazine-2-carboxamide
-
N-(3-((4S,5R)-2-amino-4-methyl-5-(tetrahydro-2H-pyran-4-yl)-5,6-dihydro-4H-1,3-thiazin-4-yl)-4-fluorophenyl)-5-(fluoromethoxy)pyrazine-2-carboxamide
-
N-(3-((4S,5R)-2-amino-4-methyl-5-phenyl-5,6-dihydro-4H-1,3-thiazin-4-yl)-4-fluorophenyl)-5-(fluoromethoxy)pyrazine-2-carboxamide
-
N-(3-((4S,5S)-2-amino-4-methyl-5-phenyl-5,6-dihydro-4H-1,3-thiazin-4-yl)-4-fluorophenyl)-5-(fluoromethoxy)pyrazine-2-carboxamide
-
N-(4-(3-bromophenyl)thiazol-2-yl)-2-((5-cyano-4-(3-methoxyphenyl)-6-oxo-1,6-dihydropyrimidin-2-yl)thio)acetamide
90.4% inhibition at 0.05 mM
N-(4-(4-acetamido-3,5-dichlorophenyl)thiazol-2-yl)-2-((5-cyano-4-(3-ethoxyphenyl)-6-oxo-1,6-dihydropyrimidin-2-yl)thio)acetamide
4.7% inhibition at 0.05 mM
N-(4-(4-acetamido-3,5-dichlorophenyl)thiazol-2-yl)-2-((5-cyano-4-(3-methoxyphenyl)-6-oxo-1,6-dihydropyrimidin-2-yl)thio)acetamide
1.4% inhibition at 0.05 mM
N-(4-(4-amino-3,5-dichlorophenyl)-1H-imidazol-2-yl)-2-((5-cyano-4-(3-methoxyphenyl)-6-oxo-1,6-dihydropyrimidin-2-yl)thio)acetamide
87.7% inhibition at 0.01 mM
N-(4-(4-amino-3,5-dichlorophenyl)thiazol-2-yl)-2-((5-cyano-4-(3-ethoxyphenyl)-6-oxo-1,6-dihydropyrimidin-2-yl)thio)acetamide
79.9% inhibition at 0.05 mM
N-(4-(4-amino-3,5-dichlorophenyl)thiazol-2-yl)-2-((5-cyano-4-(3-methoxyphenyl)-6-oxo-1,6-dihydropyrimidin-2-yl)thio)acetamide
91.8% inhibition at 0.05 mM
N-(4-(4-amino-3,5-dichlorophenyl)thiazol-2-yl)-2-((5-cyano-6-oxo-4-(3-(trifluoromethoxy)phenyl)-1,6-dihydropyrimidin-2-yl)thio)acetamide
39.6% inhibition at 0.05 mM
N-(4-(4-amino-3,5-dichlorophenyl)thiazol-2-yl)-2-((5-cyano-6-oxo-4-(3-(trifluoromethyl)phenyl)-1,6-dihydropyrimidin-2-yl)thio)acetamide
86.1% inhibition at 0.05 mM
N-[(1S,2R,4R)-4-((S)-1-benzylcarbamoyl-2-methylpropylcarbamoyl)-1-(3,5-difluoro-phenoxymethyl)-2-hydroxy-4-methoxy-butyl]-5-(methanesulfonyl-methyl-amino)-N'-((R)-1-phenyl-ethyl)-isophthalamide
-
N-[(1S,2S)-1-benzyl-2-hydroxy-3-oxo-3-[[3-(2H-tetrazol-5-yl)phenyl]amino]propyl]-4-oxo-6-[[(4S)-4-phenyl-1,3-oxazolidin-3-yl]carbonyl]-1,4-dihydropyridine-2-carboxamide
i.e. KMI-1030, BACE1 inhibitors with a 5-membered ring at the P3 position and their BACE1 inhibitory activities summarized
N-[(1S,2S)-1-benzyl-2-hydroxy-3-oxo-3-[[3-(2H-tetrazol-5-yl)phenyl]amino]propyl]-4-oxo-6-[[(4S)-4-phenyl-1,3-oxazolidin-3-yl]carbonyl]-4H-pyran-2-carboxamide
i.e. KMI-1027, BACE1 inhibitors with a 5-membered ring at the P3 position and their BACE1 inhibitory activities summarized
N-[(1S,2S)-1-benzyl-2-hydroxy-3-oxo-3-[[3-(2H-tetrazol-5-yl)phenyl]amino]propyl]-6-[[(4S)-4-phenyl-1,3-oxazolidin-3-yl]carbonyl]pyridine-2-carboxamide
i.e. KMI-1023, BACE1 inhibitors with a 5-membered ring at the P3 position and their BACE1 inhibitory activities summarized
N-[(1S,2S,4R)-2-azido-4-((S)-1-benzylcarbamoyl-2-methyl-propylcarbamoyl)-1-(3,5-difluoro-phenoxymethyl)-4-methoxy-butyl]-5-(methanesulfonyl-methyl-amino)-N'-((R)-1-phenyl-ethyl)-isophthalamide
-
N-[(1S,2S,4R)-4-((S)-1-benzylcarbamoyl-2-methylpropylcarbamoyl)-1-(3,5-difluoro-phenoxymethyl)-2-hydroxy-4-(2-methoxy-ethoxy)-butyl]-5-(methanesulfonyl-methylamino)-N'-((R)-1-phenyl-ethyl)-isophthalamide
-
N-[(1S,2S,4R)-4-((S)-1-benzylcarbamoyl-2-methylpropylcarbamoyl)-1-(3,5-difluoro-phenoxymethyl)-2-hydroxy-4-propyloxy-butyl]-5-(methanesulfonyl-methyl-amino)-N'-((R)-1-phenyl-ethyl)-isophthalamide
-
N-[(1S,2S,4R)-4-((S)-1-benzylcarbamoyl-2-methylpropylcarbamoyl)-1-(3,5-difluoro-phenoxymethyl)-4-ethyloxy-2-hydroxy-butyl]-5-(methanesulfonyl-methyl-amino)-N'-((R)-1-phenyl-ethyl)-isophthalamide
-
N-[(1S,2S,4R)-4-((S)-1-benzylcarbamoyl-2-methylpropylcarbamoyl)-2-amino-1-(3,5-difluoro-phenoxymethyl)-4-methoxy-butyl]-5-(methanesulfonyl-methyl-amino)-N'-((R)-1-phenyl-ethyl)-isophthalamide
-
N-[(1S,2S,4R)-4-((S)-1-benzylcarbamoyl-2-methylpropylcarbamoyl)-4-allyloxy-1-(3,5-difluoro-phenoxymethyl)-2-hydroxy-butyl]-5-(methanesulfonyl-methyl-amino)-N'-((R)-1-phenyl-ethyl)-isophthalamide
-
N-[(1S,2S,4R)-4-((S)-1-benzylcarbamoyl-2-methylpropylcarbamoyl)-4-benzyloxy-1-(3,5-difluoro-phenoxymethyl)-2-hydroxy-butyl]-5-(methanesulfonyl-methyl-amino)-N'-((R)-1-phenyl-ethyl)-isophthalamide
-
N-[(1S,2S,4R)-4-((S)-1-benzylcarbamoyl-2-methylpropylcarbamoyl)-4-cyclopropylmethoxy-1-(3,5-difluorophenoxymethyl)-2-hydroxy-butyl]-5-(methanesulfonylmethyl-amino)-N'-((R)-1-phenyl-ethyl)-isophthalamide
-
N-[(1S,4R)-4-((S)-1-benzylcarbamoyl-2-methylpropylcarbamoyl)-1-(3,5-difluoro-phenoxymethyl)-4-methoxybutyl]-5-(methanesulfonyl-methyl-amino)-N'-((R)-1-phenylethyl)-isophthalamide
-
N-[(2S)-1-[[(2S,3S)-1-(butan-2-ylamino)-3-hydroxy-1-oxohexan-2-yl]amino]-3-phenylpropan-2-yl]-7-ethyl-1-methyl-3,4-dihydro-1H-[1,2,5]thiadiazepino[3,4,5-hi]indole-9-carboxamide 2,2-dioxide
compound designed specifically to interact with S1' active site residues to provide selectivity over memapsin 1 and cathepsin D. Inhibitor exhibits exceedingly potent inhibitory activity and high selectivity over BACE 2 and cathepsin D
N-[(2S)-1-[[(3S)-1-(butan-2-ylamino)-3-hydroxy-1-oxobutan-2-yl]amino]-3-phenylpropan-2-yl]-5-[methyl(methylsulfonyl)amino]-N'-[(1R)-1-phenylethyl]benzene-1,3-dicarboxamide
compound designed specifically to interact with S1' active site residues to provide selectivity over memapsin 1 and cathepsin D. Inhibitor exhibits exceedingly potent inhibitory activity and high selectivity over BACE 2 and cathepsin D
N-[(2S,3R)-3-hydroxy-4-([(2S,3S)-3-hydroxy-1-[(2-methylpropyl)amino]-1-oxobutan-2-yl]amino)-1-phenylbutan-2-yl]-5-methyl-N'-[(1R)-1-phenylethyl]benzene-1,3-dicarboxamide
-
N-[(2S,3R)-3-hydroxy-4-([(2S,3S)-3-hydroxy-1-[(2-methylpropyl)amino]-1-oxobutan-2-yl]amino)-1-phenylbutan-2-yl]-5-[methyl(methylsulfonyl)amino]-N'-[(1R)-1-phenylethyl]benzene-1,3-dicarboxamide
-
N-[(2S,3R)-3-hydroxy-4-[(3-methoxybenzyl)amino]-1-phenylbutan-2-yl]-5-[methyl(methylsulfonyl)amino]-N'-[(1R)-1-phenylethyl]benzene-1,3-dicarboxamide
-
N-[(2S,3S,5R)-6-[[(2S)-1-(benzylamino)-3-methyl-1-oxobutan-2-yl]amino]-1-(3,5-difluorophenoxy)-3-hydroxy-5-methoxy-6-oxohexan-2-yl]-5-[methyl(methylsulfonyl)amino]-N'-[(1R)-1-phenylethyl]benzene-1,3-dicarboxamide
-
N-[2-(3,4-dimethoxyphenyl)ethyl]-2-[(6-[[4,6-di(piperidin-1-yl)-1,3,5-triazin-2-yl]amino]-1,3-benzothiazol-2-yl)sulfanyl]acetamide
-
N-[2-[(4aR,6S,8aR)-2-amino-6-methyl-4,4a,5,6-tetrahydropyrano[3,4-d][1,3]thiazin-8a(8H)-yl]-1,3-thiazol-4-yl]-5-(difluoromethoxy)pyridine-2-carboxamide
-
N-[3-(2-amino-4-methyl-5,6-dihydro-4H-1,3-thiazin-4-yl)-4-fluorophenyl]-5-chloropyridine-2-carboxamide
-
N-[3-(9H-carbazol-9-yl)-2-hydroxypropyl]-3,4-dichloro-N-phenylbenzamide
-
N-[3-(9H-carbazol-9-yl)-2-hydroxypropyl]-4-methoxy-N-phenylbenzamide
-
N-[3-(9H-carbazol-9-yl)-2-hydroxypropyl]-N-(2-phenylethyl)benzamide
-
N-[3-[(4aS,5S,7aS)-2-amino-5-(trifluoromethyl)-4a,5-dihydro-4H-furo[3,4-d][1,3]thiazin-7a(7H)-yl]-4-fluorophenyl]-5-(1H-1,2,4-triazol-1-yl)pyrazine-2-carboxamide
-
N1-((2S,3R)-3-hydroxy-1-phenyl-4-((3-(trifluoromethyl)benzyl)amino)butan-2-yl)-N3,5-dimethyl-N3-((R)-1-phenylethyl)isophthalamide
more than 500fold selectivity for BACE2 over BACE1
N1-((2S,3S)-4-(4-(diethylcarbamoyl)-1H-pyrazol-1-yl)-3-hydroxy-1-phenylbutan-2-yl)-N3-((R)-1-(4-fluorophenyl)ethyl)-5-(N-methylmethylsulfonamido)isophthalamide
compound exhibits good inhibition effects on amyloid beta production in the cell-based assay
N1-((R)-1-(4-fluorophenyl)ethyl)-N3-((2S,3S)-3-hydroxy-4-(4-((R)-1-hydroxy ethyl)-1H-1,2,3-triazol-1-yl)-1-phenylbutan-2-yl)-5-(N-methylmethylsulfonamido)isophthalamide
-
N3-[(1S,2R)-1-benzyl-2-hydroxy-3-[[(1S,2S)-2-hydroxy-1-(isobutylcarbamoyl)pentyl]amino]propyl]-N1-methyl-N1-[(1R)-1-phenylpropyl]benzene-1,3-dicarboxamide
174000fold selectivity for BACE2 over BACE1
N3-[(1S,2R)-1-benzyl-2-hydroxy-3-[[(1S,2S)-2-hydroxy-1-(isobutylcarbamoyl)propyl]amino]propyl]-5-[methyl(methylsulfonyl)amino]-N1-[(1R)-1-phenylpropyl]benzene-1,3-dicarboxamide
-
salvianolic acid A
competitive type inhibition
salvianolic acid C
mixed-type inhibition
tert-butyl [(2S)-3-[[(4S,5S,7R)-5-hydroxy-2,7-dimethyl-8-([(2S)-3-methyl-1-[(2-methylpropyl)amino]-1-oxobutan-2-yl]amino)-8-oxooctan-4-yl]amino]-3-oxo-2-[[(3aR,6aS)-3a,4,5,6a-tetrahydrofuro[3,2-d][1,2]oxazol-3-ylcarbonyl]amino]propyl]carbamate
-
tert-butyl [(2S)-3-[[(4S,5S,7R)-5-hydroxy-2,7-dimethyl-8-([(2S)-3-methyl-1-[(2-methylpropyl)amino]-1-oxobutan-2-yl]amino)-8-oxooctan-4-yl]amino]-3-oxo-2-[[(3aS,6aR)-3a,4,5,6a-tetrahydrofuro[3,2-d][1,2]oxazol-3-ylcarbonyl]amino]propyl]carbamate
-
[(1R,4S,5R,7R)-3,4-dibenzyl-2-thioxo-6,8-dioxa-3-azabicyclo[3.2.1]oct-7-yl](morpholin-4-yl)methanone
61% inhibition at 0.01 mM
[(1R,5R,7R)-3-benzyl-2-thioxo-6,8-dioxa-3-azabicyclo[3.2.1]oct-7-yl](morpholin-4-yl)methanone
15% inhibition at 0.01 mM
[(1S,4R,5S,7S)-3,4-dibenzyl-2-thioxo-6,8-dioxa-3-azabicyclo[3.2.1]oct-7-yl](morpholin-4-yl)methanone
5% inhibition at 0.01 mM
[(1S,5S,6S)-3-amino-5-(2-fluoro-5-[(Z)-2-fluoro-2-[5-(prop-2-yn-1-yloxy)pyrazin-2-yl]ethenyl]phenyl)-5-methyl-2-thia-4-azabicyclo[4.1.0]hept-3-en-1-yl][(3R)-3-methylmorpholin-4-yl]methanone
-
(-)-gallocatechin gallate
-
less potent inhibitor
(13S)-15-amino-10,13-dicyclohexyl-19-fluoro-2-oxa-10,14,16-triazatetracyclo[12.5.3.1(3,7).0(17,21)]tricosa-1(19),3(23),4,6,15,17,20-heptaen-11-one
-
-
(13S)-15-amino-10,13-dicyclohexyl-19-methoxy-2-oxa-10,14,16-triazatetracyclo[12.5.3.1(3,7).0(17,21)]tricosa-1(19),3(23),4,6,15,17,20-heptaen-11-one
-
-
(13S)-15-amino-10,13-dicyclohexyl-2-oxa-10,14,16,19-tetraazatetracyclo[12.5.3.1(3,7).0(17,21)]tricosa-1(19),3(23),4,6,15,17,20-heptaen-11-one
-
-
(14S)-16-amino-10,14-dicyclohexyl-2-oxa-10,15,17-triazatetracyclo[13.5.3.1(3,7).0(18,22)]tetracosa-1(20),3(24),4,6,16,18,21-heptaen-11-one
-
potent inhibitor
(14S)-16-amino-10-cyclohexyl-14-(propan-2-yl)-2-oxa-10,15,17-triazatetracyclo[13.5.3.1(3,7).0(18,22)]tetracosa-1(20),3(24),4,6,16,18,21-heptaen-11-one
-
-
(14S)-16-amino-14-(propan-2-yl)-10-(tetrahydro-2H-pyran-4-yl)-2-oxa-10,15,17-triazatetracyclo[13.5.3.1(3,7).0(18,22)]tetracosa-1(20),3(24),4,6,16,18,21-heptaen-11-one
-
-
(14S)-16-amino-14-cyclohexyl-10-(tetrahydro-2H-pyran-4-yl)-2-oxa-10,15,17-triazatetracyclo[13.5.3.1(3,7).0(18,22)]tetracosa-1(20),3(24),4,6,16,18,21-heptaen-11-one
-
-
(15R)-17-amino-11,15-dicyclohexyl-2-oxa-11,16,18-triazatetracyclo[14.5.3.1(3,7).0(19,23)]pentacosa-1(21),3(25),4,6,17,19,22-heptaen-12-one
-
-
(15S)-17-amino-11,15-dicyclohexyl-2-oxa-11,16,18-triazatetracyclo[14.5.3.1(3,7).0(19,23)]pentacosa-1(21),3(25),4,6,17,19,22-heptaen-12-one
-
-
(1R,3S)-3-[(1S)-1-(acetylamino)-2-methylpropyl]-N-[(2S,3S,5R)-6-(butylamino)-3-hydroxy-5-methyl-6-oxo-1-phenylhexan-2-yl]cyclohexanecarboxamide
-
-
(1R,3S)-3-[(1S)-1-(acetylamino)-3-methylbutyl]-N-[(2S,3S,5R)-6-(butylamino)-3-hydroxy-5-methyl-6-oxo-1-phenylhexan-2-yl]cyclohexanecarboxamide
-
11% inhibition at 0.01 mM
(1R,3S)-3-[(1S)-1-(acetylamino)butyl]-N-[(2S,3S,5R)-6-(butylamino)-3-hydroxy-5-methyl-6-oxo-1-phenylhexan-2-yl]cyclohexanecarboxamide
-
15% inhibition at 0.01 mM
(1R,3S)-3-[(1S)-1-(acetylamino)ethyl]-N-[(2S,3S,5R)-6-(butylamino)-3-hydroxy-5-methyl-6-oxo-1-phenylhexan-2-yl]cyclohexanecarboxamide
-
8% inhibition at 0.01 mM
(1R,3S)-3-[(1S)-1-(acetylamino)propyl]-N-[(2S,3S,5R)-6-(butylamino)-3-hydroxy-5-methyl-6-oxo-1-phenylhexan-2-yl]cyclohexanecarboxamide
-
17% inhibition at 0.01 mM
(1R,3S)-3-[1-(acetylamino)-3-methylbutyl]-N-[(2S,3S,5R)-6-(butylamino)-3-hydroxy-5-methyl-6-oxo-1-phenylhexan-2-yl]cyclohexanecarboxamide
-
42% inhibition at 0.01 mM
(1R,3S)-3-[1-(acetylamino)butyl]-N-[(2S,3S,5R)-6-(butylamino)-3-hydroxy-5-methyl-6-oxo-1-phenylhexan-2-yl]cyclohexanecarboxamide
-
80% inhibition at 0.01 mM
(1R,3S)-3-[1-(acetylamino)cyclopentyl]-N-[(2S,3S,5R)-6-(butylamino)-3-hydroxy-5-methyl-6-oxo-1-phenylhexan-2-yl]cyclohexanecarboxamide
-
-
(1R,3S)-3-[1-(acetylamino)ethyl]-N-[(2S,3S,5R)-6-(butylamino)-3-hydroxy-5-methyl-6-oxo-1-phenylhexan-2-yl]cyclohexanecarboxamide
-
14% inhibition at 0.01 mM
(1R,3S)-3-[1-(acetylamino)propyl]-N-[(2S,3S,5R)-6-(butylamino)-3-hydroxy-5-methyl-6-oxo-1-phenylhexan-2-yl]cyclohexanecarboxamide
-
24% inhibition at 0.01 mM
(1R,3S)-3-[2-(acetylamino)propan-2-yl]-N-[(2S,3S)-3-hydroxy-1-phenyl-4-[[3-(propan-2-yl)benzyl]amino]butan-2-yl]cyclohexanecarboxamide
-
-
(1R,3S)-3-[2-(acetylamino)propan-2-yl]-N-[(2S,3S,5R)-6-(butylamino)-3-hydroxy-5-methyl-6-oxo-1-phenylhexan-2-yl]cyclohexanecarboxamide
-
-
(1R,3S)-N-[(2S,3S)-3-hydroxy-1-phenyl-4-[[3-(propan-2-yl)benzyl]amino]butan-2-yl]-3-[2-(2-oxopiperidin-1-yl)propan-2-yl]cyclohexanecarboxamide
-
-
(1R,3S)-N-[(2S,3S)-3-hydroxy-1-phenyl-4-[[3-(propan-2-yl)benzyl]amino]butan-2-yl]-3-[2-(2-oxopyrrolidin-1-yl)propan-2-yl]cyclohexanecarboxamide
-
-
(1R,3S)-N-[(2S,3S)-3-hydroxy-1-phenyl-4-[[3-(propan-2-yl)benzyl]amino]butan-2-yl]-3-[2-(propanoylamino)propan-2-yl]cyclohexanecarboxamide
-
-
(1R,3S)-N-[(2S,3S)-3-hydroxy-1-phenyl-4-[[3-(propan-2-yl)benzyl]amino]butan-2-yl]-3-[2-[methyl(propanoyl)amino]propan-2-yl]cyclohexanecarboxamide
-
-
(1S,2R)-N-[1-benzyl-2-hydroxy-3-(S)-[(1-benzylpiperidin-4-yl)amino]-propyl]-5-[methyl(methylsulfonyl)amino]-N'-[(R)-1-phenylethyl]isophthalamide
-
-
(1S,2R)-N-[1-benzyl-2-hydroxy-3-(S)-[2-(1-benzylpiperidin-4-yl)ethylamino]-propyl]-5-[methyl(methylsulfonyl)-amino]-N'-[(R)-1-(4-fluorophenyl)ethyl]isophthalamide
-
-
(1S,2R)-N-[1-benzyl-2-hydroxy-3-(S)-[2-(1-benzylpiperidin-4-yl)ethylamino]-propyl]-5-[methyl(methylsulfonyl)amino]-N'-[(R)-1-phenylethyl]isophthalamide
-
dual inhibitor of both beta-secretase and acetylcholinesterase, good inhibitory effects on amyloid beta production of amyloid precursor protein transfected HEK293 cells
(2R,4S,5S)-N-benzyl-4-hydroxy-2,7-dimethyl-5-[(N-[(2Z)-3-[4-(trifluoromethyl)phenyl]prop-2-enoyl]-L-seryl)amino]octanamide
-
16.45% inhibition at 0.01 mg/ml
(2R,4S,5S)-N-benzyl-4-hydroxy-5-([N-[(4-methoxyphenyl)acetyl]-L-seryl]amino)-2,7-dimethyloctanamide
-
25.09% inhibition at 0.01 mg/ml
(4S)-4-[(1R)-1-hydroxy-2-([1-[3-(propan-2-yl)phenyl]cyclopropyl]amino)ethyl]-19-(2-oxopyrrolidin-1-yl)-11,16-dioxa-3-azatricyclo[15.3.1.1(6,10)]docosa-1(21),6(22),7,9,17,19-hexaen-2-one
-
-
(4S)-4-[(1R)-1-hydroxy-2-([1-[3-(propan-2-yl)phenyl]cyclopropyl]amino)ethyl]-19-(methoxymethyl)-11,16-dioxa-3,18-diazatricyclo[15.3.1.1(6,10)]docosa-1(21),6(22),7,9,17,19-hexaen-2-one
-
-
(4S)-4-[(1R)-1-hydroxy-2-([1-[3-(propan-2-yl)phenyl]cyclopropyl]amino)ethyl]-19-methyl-11,16-dioxa-3,18-diazatricyclo[15.3.1.1(6,10)]docosa-1(21),6(22),7,9,17,19-hexaen-2-one
-
-
(4S)-4-[(1R)-1-hydroxy-2-([1-[3-(propan-2-yl)phenyl]ethyl]amino)ethyl]-19-methyl-11,16-dioxa-3,18-diazatricyclo[15.3.1.1(6,10)]docosa-1(21),6(22),7,9,17,19-hexaen-2-one
-
-
(4S)-4-[(1R)-1-hydroxy-2-([2-[3-(propan-2-yl)phenyl]propan-2-yl]amino)ethyl]-19-(methoxymethyl)-11-oxa-3,16-diazatricyclo[15.3.1.1(6,10)]docosa-1(21),6(22),7,9,17,19-hexaen-2-one
-
-
(4S)-4-[(1R)-1-hydroxy-2-[[3-(propan-2-yl)benzyl]amino]ethyl]-11-oxa-3,16-diazatricyclo[15.3.1.1(6,10)]docosa-1(21),6(22),7,9,17,19-hexaen-2-one
-
-
(4S)-4-[(1R)-1-hydroxy-2-[[3-(propan-2-yl)benzyl]amino]ethyl]-19-(methoxymethyl)-11-oxa-3,16-diazatricyclo[15.3.1.1(6,10)]docosa-1(21),6(22),7,9,17,19-hexaen-2-one
-
-
(4S)-4-[(1R)-1-hydroxy-2-[[3-(propan-2-yl)benzyl]amino]ethyl]-19-methyl-11,16-dioxa-3,18-diazatricyclo[15.3.1.1(6,10)]docosa-1(21),6(22),7,9,17,19-hexaen-2-one
-
-
(4S)-4-[(1R)-1-hydroxy-2-[[3-(propan-2-yl)benzyl]amino]ethyl]-19-methyl-11-oxa-3,16,18-triazatricyclo[15.3.1.1(6,10)]docosa-1(21),6(22),7,9,17,19-hexaen-2-one
-
-
(4S)-4-[(1R)-2-[[1-(3-tert-butylphenyl)-2,2,2-trifluoroethyl]amino]-1-hydroxyethyl]-19-(methoxymethyl)-11-oxa-3,16-diazatricyclo[15.3.1.1(6,10)]docosa-1(21),6(22),7,9,17,19-hexaen-2-one
-
-
(4S)-4-[(1R)-2-[[1-(3-tert-butylphenyl)-2-fluoroethyl]amino]-1-hydroxyethyl]-19-(methoxymethyl)-11-oxa-3,16-diazatricyclo[15.3.1.1(6,10)]docosa-1(21),6(22),7,9,17,19-hexaen-2-one
-
-
(4S)-4-[(1R)-2-[[1-(3-tert-butylphenyl)-2-methoxyethyl]amino]-1-hydroxyethyl]-19-(methoxymethyl)-11-oxa-3,16-diazatricyclo[15.3.1.1(6,10)]docosa-1(21),6(22),7,9,17,19-hexaen-2-one
-
-
(4S)-4-[(1R)-2-[[1-(3-tert-butylphenyl)cyclobutyl]amino]-1-hydroxyethyl]-19-(methoxymethyl)-11-oxa-3,16-diazatricyclo[15.3.1.1(6,10)]docosa-1(21),6(22),7,9,17,19-hexaen-2-one
-
-
(4S)-4-[(1R)-2-[[1-(3-tert-butylphenyl)cyclopentyl]amino]-1-hydroxyethyl]-19-(methoxymethyl)-11-oxa-3,16-diazatricyclo[15.3.1.1(6,10)]docosa-1(21),6(22),7,9,17,19-hexaen-2-one
-
-
(5S)-2-amino-5-(2',4'-difluorobiphenyl-3-yl)-3-methyl-5-(pyridin-4-yl)-3,5-dihydro-4H-imidazol-4-one
-
5fold selectivity for BACE2 over BACE1, 27fold selectivity for BACE2 over cathepsin D
(6R)-2,6-anhydro-5-O-[(E)-2-(4-hydroxyphenyl)ethenyl]-6-[2-[(2R)-2-hydroxypropyl]-7-methoxy-5-methyl-4-oxo-4H-chromen-8-yl]-L-glucitol
-
inhibitor isolated from Aloe vera and Aloe nobilis. Inhibition of amyloid beta1-42 production by 7.4% in B103 neuroblastoma cells at 30 ppm
(6R)-2,6-anhydro-6-[7-methoxy-5-methyl-4-oxo-2-[(1E)-prop-1-en-1-yl]-4H-chromen-8-yl]-L-glucitol
-
inhibitor isolated from Aloe vera and Aloe nobilis. Inhibition of amyloid beta1-42 production by 12.3% in B103 neuroblastoma cells at 30 ppm
(7S,12Z)-N-[(2S,4R)-2-hydroxy-4-methyl-5-[[(1S)-2-methyl-1-(phenylcarbamoyl)propyl]amino]-1-(2-methylpropyl)-5-oxopentyl]-4-(1-methylethyl)-2,5,9-trioxo-1-oxa-3,6,10-triazacyclohexadec-12-ene-7-carboxamide
-
-
(R)-3-(2-amino-6-(3-chloropyridin-2-yl)quinolin-3-yl)-N-(3,3-dimethylbutyl)-2-methylpropanamide
-
EC50 value for cell assay 80 nM
(R)-3-(2-amino-6-(3-methylpyridin-2-yl)quinolin-3-yl)-N-(3,3-dimethylbutyl)-2-methylpropanamide
-
EC50 value for cell assay 35 nM
1,1'-piperazine-1,4-diylbis[3-(3,6-dichloro-9H-carbazol-9-yl)propan-2-ol]
-
inhibitor identified by in silico mulit-filter approaches. Calculated binding free energy of R,S-isomer -48 kcal/mol
1,1'-piperazine-1,4-diylbis[3-(9H-carbazol-9-yl)propan-2-ol]
-
inhibitor identified by in silico mulit-filter approaches. Calculated binding free energy of S,R-isomer -48.2 kcal/mol
1-(2-chlorobenzyl)-4-(4-(dibenzo[b,d]furan-1-yl)benzyl)-1H-imidazol-2-amine
-
0.005 mM, 37.8% inhibition. Inhibitor is predicted to be able to cross the blood-brain barrier
1-(4-fluorobenzyl)-4-((30,50-dimethoxybiphenyl-4-yl)methyl)-1H-imidazol-2-amine
-
0.005 mM, 40% inhibition. Inhibitor is predicted to be able to cross the blood-brain barrier
1-[ (3-benzoylamino-phenylcarbamoyl)-methyl]-pyridinium chloride
-
51% inhibition at 0.05 mM
1-[(3-benzoylamino-phenylcarbamoyl)-methyl]-3-carbamoyl-pyridiniumchloride
-
54% inhibition at 0.05 mM
1-[(3-benzoylamino-phenylcarbamoyl)-methyl]-3-phenethylcarbamoyl-pyridinium chloride
-
55% inhibition at 0.05 mM
1-[(3-m-tolylcarbamoyl-phenylcarbamoyl)-methyl]-pyridinium chloride
-
61% inhibition at 0.05 mM
1-[(3-p-tolylcarbamoyl-phenylcarbamoyl)-methyl]-pyridinium chloride
-
42% inhibition at 0.05 mM
1-[(E)-[(4-methylquinazolin-2-yl)amino][(phenylcarbamoyl)amino]methylidene]-3-phenylurea
-
complete inhibition at 0.1 mM
1-[[3-(4-chloro-phenylcarbamoyl)-phenylcarbamoyl]-methyl]-3-phenethylcarbamoyl-pyridinium chloride
-
78% inhibition at 0.05 mM
1-[[3-(4-chloro-phenylcarbamoyl)-phenylcarbamoyl]-methyl]-pyridinium chloride
-
complete inhibition at 0.05 mM
1-[[3-(4-methoxy-phenylcarbamoyl)-phenylcarbamoyl]-methyl]-3-phenethylcarbamoyl-pyridinium chloride
-
44% inhibition at 0.05 mM
1-[[3-(4-methoxy-phenylcarbamoyl)-phenylcarbamoyl]-methyl]-pyridinium chloride
-
complete inhibition at 0.05 mM
1-[[3-(4-methoxy-phenylsulfamoyl)-phenylcarbamoyl]-methyl]-pyridinium chloride
-
50% inhibition at 0.05 mM
1-[[3-(4-methyl-benzoylamino)-phenylcarbamoyl]-methyl]-3-phenethylcarbamoyl-pyridinium chloride
-
complete inhibition at 0.05 mM
1-[[3-(4-methyl-benzoylamino)-phenylcarbamoyl]-methyl]-pyridinium chloride
-
-
11-oxo-N-(pyridin-4-yl)-10,11-dihydro-5H-dibenzo[b,e][1,4]-diazepine-3-carboxamide
-
-
16-amino-11-cyclohexyl-2-oxa-11,15,17-triazatetracyclo[13.5.3.1(3,7).0(18,22)]tetracosa-1(20),3(24),4,6,16,18,21-heptaen-12-one
-
-
1[[3-(4-methyl-benzoylamino)-phenylcarbamoyl]-methyl]-pyridinium chloride
-
68% inhibition at 0.05 mM
2-(2,4-dihydroxyphenyl)-5,7-dihydroxy-4H-chromen-4-one
-
i.e. norartocarpetin, prenylated flavone from the stem bark of Morus lhou, noncompetitive
2-amino-3,4-dihydroquinazoline
-
-
2-amino-3-ethyl-5,5-diphenyl-3,5-dihydro-4H-imidazol-4-one
-
2-amino-3-methyl-5,5-diphenyl-3,5-dihydro-4H-imidazol-4-one
-
-
2-amino-3-methyl-5-(2-methylpyridin-4-yl)-5-[3-(pyridin-3-yl)phenyl]-3,5-dihydro-4H-imidazol-4-one
-
-
2-amino-3-methyl-5-(2-methylpyridin-4-yl)-5-[3-(pyrimidin-5-yl)phenyl]-3,5-dihydro-4H-imidazol-4-one
-
-
2-amino-3-methyl-5-(pyridin-4-yl)-5-[3-(pyridin-3-yl)phenyl]-3,5-dihydro-4H-imidazol-4-one
-
exhibits modest selectivity (about 8fold) against BACE2
2-amino-3-methyl-5-(tricyclo[3.3.1.1(3,7)]dec-1-yl)-5-[3-(trifluoromethoxy)phenyl]-3,5-dihydro-4H-imidazol-4-one
-
2-amino-3-methyl-5-phenyl-5-(pyridin-4-yl)-3,5-dihydro-4H-imidazol-4-one
-
-
2-amino-3-methyl-5-phenyl-5-(tricyclo[3.3.1.13,7]dec-1-yl)-3,5-dihydro-4H-imidazol-4-one
-
2-amino-3-methyl-5-[2-(propan-2-yl)pyridin-4-yl]-5-[3-(pyrimidin-5-yl)phenyl]-3,5-dihydro-4H-imidazol-4-one
-
-
2-amino-3-methyl-5-[2-methyl-6-(propan-2-yl)pyridin-4-yl]-5-[3-(pyrimidin-5-yl)phenyl]-3,5-dihydro-4H-imidazol-4-one
-
24% inhibition at 0.0125 mM
2-amino-5,5-diphenyl-3,5-dihydro-4H-imidazol-4-one
-
2-amino-5-(1,3-benzodioxol-5-yl)-3-methyl-5-[3-(pyridin-3-yl)phenyl]-3,5-dihydro-4H-imidazol-4-one
-
2-amino-5-(2,3-dihydro-1,4-benzodioxin-6-yl)-3-methyl-5-[3-(pyridin-3-yl)phenyl]-3,5-dihydro-4H-imidazol-4-one
-
2-amino-5-(2,3-dihydro-1-benzofuran-5-yl)-3-methyl-5-[3-(pyridin-3-yl)phenyl]-3,5-dihydro-4H-imidazol-4-one
-
2-amino-5-(2,6-diethylpyridin-4-yl)-3-methyl-5-[3-(pyrimidin-5-yl)phenyl]-3,5-dihydro-4H-imidazol-4-one
-
-
2-amino-5-(2,6-dimethylpyridin-4-yl)-3-methyl-5-[3-(pyrimidin-5-yl)phenyl]-3,5-dihydro-4H-imidazol-4-one
-
-
2-amino-5-(2-ethyl-6-methylpyridin-4-yl)-3-methyl-5-[3-(pyrimidin-5-yl)phenyl]-3,5-dihydro-4H-imidazol-4-one
-
28% inhibition at 0.0125 mM
2-amino-5-(2-ethylpyridin-4-yl)-3-methyl-5-[3-(pyrimidin-5-yl)phenyl]-3,5-dihydro-4H-imidazol-4-one
-
-
2-amino-5-(3,4-dimethoxyphenyl)-3-methyl-5-(tricyclo[3.3.1.1(3,7)]dec-1-yl)-3,5-dihydro-4H-imidazol-4-one
-
2-amino-5-(3-butoxyphenyl)-3-methyl-5-(tricyclo[3.3.1.1(3,7)]dec-1-yl)-3,5-dihydro-4H-imidazol-4-one
-
2-amino-5-(3-chlorophenyl)-3-methyl-5-phenyl-3,5-dihydro-4H-imidazol-4-one
-
2-amino-5-(3-ethoxyphenyl)-3-methyl-5-(tricyclo[3.3.1.1(3,7)]dec-1-yl)-3,5-dihydro-4H-imidazol-4-one
-
2-amino-5-(3-methoxy-4-methylphenyl)-3-methyl-5-(tricyclo[3.3.1.1(3,7)]dec-1-yl)-3,5-dihydro-4H-imidazol-4-one
-
2-amino-5-(3-methoxyphenyl)-3-methyl-5-(tricyclo[3.3.1.1(3,7)]dec-1-yl)-3,5-dihydro-4H-imidazol-4-one
-
2-amino-5-(3-methoxyphenyl)-3-methyl-5-phenyl-3,5-dihydro-4H-imidazol-4-one
-
2-amino-5-(4-chlorophenyl)-3-methyl-5-phenyl-3,5-dihydro-4H-imidazol-4-one
-
2-amino-5-(4-ethyl-3-methoxyphenyl)-3-methyl-5-(tricyclo[3.3.1.1(3,7)]dec-1-yl)-3,5-dihydro-4H-imidazol-4-one
-
2-amino-5-(4-methoxy-3-methylphenyl)-3-methyl-5-(6-methylbiphenyl-3-yl)-3,5-dihydro-4H-imidazol-4-one
-
2-amino-5-(4-methoxy-3-methylphenyl)-3-methyl-5-[3-(pyridin-3-yl)phenyl]-3,5-dihydro-4H-imidazol-4-one
-
-
2-amino-5-(4-methoxy-3-methylphenyl)-3-methyl-5-[3-(pyrimidin-5-yl)phenyl]-3,5-dihydro-4H-imidazol-4-one
-
2-amino-5-(4-methoxyphenyl)-3-methyl-5-phenyl-3,5-dihydro-4H-imidazol-4-one
-
2-amino-5-(biphenyl-3-yl)-3-methyl-5-(pyridin-4-yl)-3,5-dihydro-4H-imidazol-4-one
-
-
2-amino-5-(biphenyl-3-yl)-5-(3,4-dimethoxyphenyl)-3-methyl-3,5-dihydro-4H-imidazol-4-one
-
2-amino-5-(biphenyl-3-yl)-5-(3-butoxy-4-methoxyphenyl)-3-methyl-3,5-dihydro-4H-imidazol-4-one
-
2-amino-5-(biphenyl-3-yl)-5-(3-chloro-4-methoxyphenyl)-3-methyl-3,5-dihydro-4H-imidazol-4-one
-
2-amino-5-(biphenyl-3-yl)-5-(3-cyclopentyl-4-methoxyphenyl)-3-methyl-3,5-dihydro-4H-imidazol-4-one
-
2-amino-5-(biphenyl-3-yl)-5-(3-ethoxy-4-methoxyphenyl)-3-methyl-3,5-dihydro-4H-imidazol-4-one
-
2-amino-5-(biphenyl-3-yl)-5-(3-ethoxy-4-propoxyphenyl)-3-methyl-3,5-dihydro-4H-imidazol-4-one
-
2-amino-5-(biphenyl-3-yl)-5-(3-fluoro-4-methoxyphenyl)-3-methyl-3,5-dihydro-4H-imidazol-4-one
-
2-amino-5-(biphenyl-3-yl)-5-(4-methoxy-3-methylphenyl)-3-methyl-3,5-dihydro-4H-imidazol-4-one
-
2-amino-5-(biphenyl-3-yl)-5-[3-(cyclopentyloxy)-4-methoxyphenyl]-3-methyl-3,5-dihydro-4H-imidazol-4-one
-
2-amino-5-(biphenyl-3-yl)-5-[4-methoxy-3-(propan-2-yloxy)phenyl]-3-methyl-3,5-dihydro-4H-imidazol-4-one
-
2-amino-5-(biphenyl-3-yl)-5-[4-methoxy-3-(trifluoromethyl)phenyl]-3-methyl-3,5-dihydro-4H-imidazol-4-one
-
2-amino-5-[2-fluoro-3-(pyrimidin-5-yl)phenyl]-3-methyl-5-[4-(trifluoromethoxy)phenyl]-3,5-dihydro-4H-imidazol-4-one
-
2-amino-5-[3-(2-fluoropyridin-3-yl)phenyl]-5-(4-methoxy-3-methylphenyl)-3-methyl-3,5-dihydro-4H-imidazol-4-one
2-amino-5-[3-(2-methoxypyridin-3-yl)phenyl]-3-methyl-5-[4-(trifluoromethoxy)phenyl]-3,5-dihydro-4H-imidazol-4-one
-
2-amino-5-[3-(6-fluoropyridin-3-yl)phenyl]-3-methyl-5-[4-(trifluoromethoxy)phenyl]-3,5-dihydro-4H-imidazol-4-one
-
2-amino-5-[3-(6-methoxypyridin-3-yl)phenyl]-3-methyl-5-[4-(trifluoromethoxy)phenyl]-3,5-dihydro-4H-imidazol-4-one
-
2-amino-5-[3-fluoro-5-(pyrimidin-5-yl)phenyl]-3-methyl-5-[4-(trifluoromethoxy)phenyl]-3,5-dihydro-4H-imidazol-4-one
-
2-amino-5-[4-fluoro-3-(2-fluoropyridin-3-yl)phenyl]-5-(4-methoxy-3-methylphenyl)-3-methyl-3,5-dihydro-4H-imidazol-4-one
-
2-amino-5-[4-fluoro-3-(pyrimidin-5-yl)phenyl]-3-methyl-5-[4-(trifluoromethoxy)phenyl]-3,5-dihydro-4H-imidazol-4-one
-
2-amino-5-[4-fluoro-3-(pyrimidin-5-yl)phenyl]-5-(4-methoxy-3-methylphenyl)-3-methyl-3,5-dihydro-4H-imidazol-4-one
-
2-deoxy-4-O-beta-D-glucopyranuronosyl-6-O-sulfo-2-(sulfoamino)-beta-D-glucopyranose
-
IC50: 0.000053 mg/ml
2-[(3-cyano-4,5,6,7-tetrahydro-1-benzothiophen-2-yl)amino]-2-oxoethyl [(4,6-diphenylpyrimidin-2-yl)sulfanyl]acetate
-
75% inhibition at 0.1 mM
2-[(3-cyano-4,6-diphenylpyridin-2-yl)sulfanyl]-N-(3-nitrophenyl)acetamide
-
complete inhibition at 0.1 mM
2-[(4-methyl-5-[2-[(4-methylphenyl)amino]-2-oxoethyl]-4H-1,2,4-triazol-3-yl)sulfanyl]-N-(4-phenyl-1,3-thiazol-2-yl)acetamide
-
83% inhibition at 0.1 mM
2-[(6-[[4,6-di(piperidin-1-yl)-1,3,5-triazin-2-yl]amino]-1,3-benzothiazol-2-yl)sulfanyl]-N-(2-fluorophenyl)acetamide
-
90% inhibition at 0.1 mM
2-[[2-amino-6-([2-(2-chlorophenyl)-5-[4-(pentyloxy)phenyl]-1H-pyrrol-1-yl]methyl)pyridin-3-yl]amino]ethanol
-
-
2-[[2-amino-6-([2-(2-chlorophenyl)-5-[4-(pentyloxy)phenyl]-1H-pyrrol-1-yl]methyl)pyridin-3-yl]oxy]ethanol
-
1.7% inhibition at 0.0125 mM
2-[[2-amino-6-([2-(2-chlorophenyl)-5-[4-(pyrimidin-5-yloxy)phenyl]-1H-pyrrol-1-yl]methyl)pyridin-3-yl]amino]ethanol
-
8.46% inhibition at 0.0125 mM
2-[[2-amino-6-([2-(2-chlorophenyl)-5-[4-(pyrimidin-5-yloxy)phenyl]-1H-pyrrol-1-yl]methyl)pyridin-3-yl]oxy]ethanol
-
5.43% inhibition at 0.0125 mM
2-[[3-cyano-4-(4-fluorophenyl)-6-phenylpyridin-2-yl]sulfanyl]-N-(tricyclo[3.3.1.1(3,7)]dec-1-yl)acetamide
-
45% inhibition at 0.1 mM
2-[[3-cyano-6-(4-fluorophenyl)-4-phenylpyridin-2-yl]sulfanyl]-N-(5-ethyl-1,3,4-thiadiazol-2-yl)acetamide
-
80% inhibition at 0.1 mM
2-[[4-(4-chlorophenyl)-3-cyano-6-(4-methoxyphenyl)pyridin-2-yl]sulfanyl]-N-(naphthalen-2-yl)-N-phenylacetamide
-
68% inhibition at 0.1 mM
2-[[4-benzyl-5-(1H-indol-3-ylmethyl)-4H-1,2,4-triazol-3-yl]sulfanyl]-1-(1H-indol-3-yl)ethanone
-
75% inhibition at 0.1 mM
3-(3H-imidazo[4,5-c]pyridin-2-yl)-5H-dibenzo[b,e][1,4]diazepin-11(10H)-one
-
-
3-(5-(4-fluorophenyl)-1H-imidazol-2-yl)-5H dibenzo[b,e][1,4]diazepin-11(10H)-one
-
-
3-(5-(pyridin-4-yl)-1H-imidazol-2-yl)-5H dibenzo[b,e][1,4]-diazepin-11(10H)-one
-
-
3-(6-(2-acetylphenyl)-2-aminoquinolin-3-yl)-N-(3,3-dimethylbutyl)-2-methylpropanamide
-
EC50 value for cell assay 11 nM
3-(6-fluoro-1H-benzo[d]imidazol-2-yl)-5H-dibenzo[b,e][1,4]diazepin-11(10H)-one
-
-
3-(benzylsulfanyl)-6-(5-chloro-3-methyl-1-phenyl-1H-pyrazol-4-yl)-6,7-dihydro[1,2,4]triazino[5,6-d][3,1]benzoxazepine
-
48% inhibition at 0.1 mM
3-(butylsulfonyl)-N-[(2S,3R)-1-(3,5-difluorophenyl)-4-[(3-ethylbenzyl)amino]-3-hydroxybutan-2-yl]-N2-(3,3,3-trifluoropropanoyl)-D-alaninamide
-
-
3-(butylsulfonyl)-N-[(2S,3R)-1-(3,5-difluorophenyl)-4-[(3-ethylbenzyl)amino]-3-hydroxybutan-2-yl]-N2-(methoxyacetyl)-D-alaninamide
-
-
3-(butylsulfonyl)-N-[(2S,3R)-1-(3,5-difluorophenyl)-4-[(3-ethylbenzyl)amino]-3-hydroxybutan-2-yl]-N2-(pyridin-3-ylacetyl)-D-alaninamide
-
-
3-(butylsulfonyl)-N-[(2S,3R)-1-(3,5-difluorophenyl)-4-[(3-ethylbenzyl)amino]-3-hydroxybutan-2-yl]-N2-(pyridin-4-ylacetyl)-D-alaninamide
-
-
3-(butylsulfonyl)-N2-(3-cyanopropanoyl)-N-[(2S,3R)-1-(3,5-difluorophenyl)-4-[(3-ethylbenzyl)amino]-3-hydroxybutan-2-yl]-D-alaninamide
-
-
3-(butylsulfonyl)-N2-(cyclopropylcarbonyl)-N-[(2S,3R)-1-(3,5-difluorophenyl)-4-[(3-ethylbenzyl)amino]-3-hydroxybutan-2-yl]-D-alaninamide
-
-
3-(cyclohexylsulfonyl)-N-[(2S,3R)-3-hydroxy-4-[(3-methoxybenzyl)amino]-1-phenylbutan-2-yl]propanamide
-
-
3-(dibutylsulfamoyl)-N-[(2S,3R)-3-hydroxy-4-[(3-methoxybenzyl)amino]-1-phenylbutan-2-yl]propanamide
-
-
3-(dipropylsulfamoyl)-N-[(2S,3R)-3-hydroxy-4-[(3-methoxybenzyl)amino]-1-phenylbutan-2-yl]propanamide
-
-
3-(heptan-4-ylsulfonyl)-N-[(2S,3R)-3-hydroxy-4-[(3-methoxybenzyl)amino]-1-phenylbutan-2-yl]propanamide
-
-
3-carbamoyl-1-[(3-m-tolylcarbamoyl-phenylcarbamoyl)-methyl]-pyridinium chloride
-
44% inhibition at 0.05 mM
3-carbamoyl-1-[(3-p-tolylcarbamoyl-phenylcarbamoyl)-methyl]-pyridinium chloride
-
69% inhibition at 0.05 mM
3-carbamoyl-1-[[3-(4-chloro-phenylcarbamoyl)-phenylcarbamoyl]-methyl]-pyridinium chloride
-
64% inhibition at 0.05 mM
3-carbamoyl-1-[[3-(4-methoxy-phenylcarbamoyl)-phenylcarbamoyl]-methyl]-pyridinium chloride
-
complete inhibition at 0.05 mM
3-carbamoyl-1-[[3-(4-methoxy-phenylsulfamoyl)-phenylcarbamoyl]-methyl]-pyridinium chloride
-
34% inhibition at 0.05 mM
3-carbamoyl-1-[[3-(4-methyl-benzoylamino)-phenylcarbamoyl]-methyl]-pyridinium chloride
-
24% inhibition at 0.05 mM
3-carbamoyl-1-[[3-(toluene-4-sulfonylamino)-phenylcarbamoyl]-methyl]-pyridinium chloride
-
4% inhibition at 0.05 mM
3-chloro-N-[(2R)-1-([1-(3,5-difluorophenyl)-4-[(3-ethylbenzyl)amino]-3-hydroxybutan-2-yl]amino)-3-(heptan-4-ylsulfonyl)-1-oxopropan-2-yl]benzamide
-
-
3-phenethylcarbamoyl-1-[(3-m-tolylcarbamoyl-phenylcarbamoyl)-methyl]-pyridinium chloride
-
58% inhibition at 0.05 mM
3-phenethylcarbamoyl-1-[(3-p-tolylcarbamoyl-phenylcarbamoyl)-methyl]-pyridinium chloride
-
72% inhibition at 0.05 mM
3-phenethylcarbamoyl-1-[[3-(toluene-4-sulfonylamino)-phenylcarbamoyl]-methyl]-pyridinium chloride
-
36% inhibition at 0.05 mM
3-[(2H-tetrazol-5-ylcarbonyl)amino]-L-alanyl-L-valyl-N-((1S,2R)-1-benzyl-3-[(3,5-di-2H-tetrazol-5-ylphenyl)amino]-2-hydroxy-3-oxopropyl)-L-leucinamide
-
0.0002 mM, complete inhibition, IC50: 1.2 nM
3-[(2H-tetrazol-5-ylcarbonyl)amino]-L-alanyl-L-valyl-N-((1S,2R)-1-benzyl-3-[(3,5-dicarboxyphenyl)amino]-2-hydroxy-3-oxopropyl)-L-leucinamide
-
0.0002 mM, 98.1% inhibition, IC50: 3.9 nM
3-[(2H-tetrazol-5-ylcarbonyl)amino]-L-alanyl-L-valyl-N-((1S,2R)-1-benzyl-3-[(3-carbamoylphenyl)amino]-2-hydroxy-3-oxopropyl)-L-leucinamide
-
0.0002 mM, 78.1% inhibition
3-[(2H-tetrazol-5-ylcarbonyl)amino]-L-alanyl-L-valyl-N-((1S,2R)-1-benzyl-3-[(3-carboxyphenyl)amino]-2-hydroxy-3-oxopropyl)-L-leucinamide
-
0.002 mM, 87.1% inhibition, IC50: 8.2 nM
3-[(2H-tetrazol-5-ylcarbonyl)amino]-L-alanyl-L-valyl-N-[(1S,2R)-1-benzyl-2-hydroxy-3-oxo-3-([3-(2H-tetrazol-5-yl)phenyl]amino)propyl]-L-leucinamide
-
0.0002 mM, 98.1% inhibition, IC50: 4.8 nM
3-[(2H-tetrazol-5-ylcarbonyl)amino]-L-alanyl-L-valyl-N-[(1S,2R)-1-benzyl-2-hydroxy-3-oxo-3-([3-(5-oxo-4,5-dihydro-1,2,4-oxadiazol-3-yl)phenyl]amino)propyl]-L-leucinamide
-
0.0002 mM, 94.2% inhibition, IC50: 6.6 nM
3-[(2H-tetrazol-5-ylcarbonyl)amino]-L-alanyl-L-valyl-N-[(1S,2R)-1-benzyl-2-hydroxy-3-oxo-3-([3-(5-thioxo-4,5-dihydro-1,2,4-oxadiazol-3-yl)phenyl]amino)propyl]-L-leucinamide
-
0.0002 mM, 97.2% inhibition, IC50: 6.4 nM
3-[(2H-tetrazol-5-ylcarbonyl)amino]alanyl-L-valyl-N-(1-benzyl-2-hydroxy-3-oxo-3-[[3-(2H-tetrazol-5-yl)phenyl]amino]propyl)leucinamide
-
-
3-[(2H-tetrazol-5-ylcarbonyl)amino]alanyl-L-valyl-N-[1-benzyl-3-[(3,5-di-2H-tetrazol-5-ylphenyl)amino]-2-hydroxy-3-oxopropyl]leucinamide
-
-
3-[2-amino-6-(phenylcarbonyl)quinazolin-3(4H)-yl]-N-cyclohexyl-N-methylpropanamide
-
-
3-[5-[(1R)-1-amino-1-methyl-2-phenylethyl]-1,3,4-oxadiazol-2-yl]-N-[1-(4-fluorophenyl)ethyl]-5-[methyl(methylsulfonyl)amino]benzamide
-
-
3-[[(5-fluoro-2,6-dioxo-1,2,3,6-tetrahydropyrimidin-4-yl)carbonyl]amino]alanyl-L-valyl-N-[(1S)-1-benzyl-2-hydroxy-3-oxo-3-[[3-(2H-tetrazol-5-yl)phenyl]amino]propyl]phenylalaninamide
-
-
3-[[2-amino-6-([2-(2-chlorophenyl)-5-[4-(pentyloxy)phenyl]-1H-pyrrol-1-yl]methyl)pyridin-3-yl]amino]propan-1-ol
-
-
3-[[2-amino-6-([2-(2-chlorophenyl)-5-[4-(pentyloxy)phenyl]-1H-pyrrol-1-yl]methyl)pyridin-3-yl]oxy]propan-1-ol
-
47% inhibition at 0.0125 mM
4-(2-amino-6-phenoxyquinazolin-3(4H)-yl)-N,4-dicyclohexyl-N-methylbutanamide
-
-
4-(4-[1-[(6-aminopyridin-2-yl)methyl]-5-(2-chlorophenyl)-1H-pyrrol-2-yl]phenoxy)butanenitrile
-
-
4-(cyclohexylamino)-1-(4-fluorobenzyl)-8-[(2'-methylbiphenyl-4-yl)methyl]-1,3,8-triazaspiro[4.5]dec-3-en-2-one
-
-
4-(dipropylsulfamoyl)-N-[(2S,3R)-3-hydroxy-4-[(3-methoxybenzyl)amino]-1-phenylbutan-2-yl]butanamide
-
-
4-bromo-N-[(4-bromophenyl)sulfonyl]-N-[1-(3,4-dichlorobenzyl)-1H-pyrazol-4-yl]benzenesulfonamide
-
50% inhibition at 0.1 mM
4-[1-(4-methoxyphenyl)-2-[4-(trifluoromethyl)phenyl]ethyl]-1-methyl-1H-imidazol-2-amine
-
-
4-[1-[(6-aminopyridin-2-yl)methyl]-5-phenyl-1H-pyrrol-2-yl]-N-(prop-2-en-1-yl)benzamide
-
6.2% inhibition at 0.0125 mM
4-[1-[(6-aminopyridin-2-yl)methyl]-5-phenyl-1H-pyrrol-2-yl]-N-(propan-2-yl)benzamide
-
6.58% inhibition at 0.0125 mM
4-[1-[(6-aminopyridin-2-yl)methyl]-5-phenyl-1H-pyrrol-2-yl]-N-butylbenzamide
-
45% inhibition at 0.0125 mM
4-[1-[(6-aminopyridin-2-yl)methyl]-5-phenyl-1H-pyrrol-2-yl]-N-cyclobutylbenzamide
-
38.4% inhibition at 0.0125 mM
4-[1-[(6-aminopyridin-2-yl)methyl]-5-phenyl-1H-pyrrol-2-yl]-N-cyclopropylbenzamide
-
10.6% inhibition at 0.0125 mM
4-[1-[(6-aminopyridin-2-yl)methyl]-5-phenyl-1H-pyrrol-2-yl]-N-ethylbenzamide
-
36% inhibition at 0.0125 mM
4-[1-[(6-aminopyridin-2-yl)methyl]-5-phenyl-1H-pyrrol-2-yl]-N-propylbenzamide
-
28% inhibition at 0.0125 mM
4-[2-(2-methoxy-5-nitrophenyl)-1-(4-methoxyphenyl)ethyl]-1-methyl-1H-imidazol-2-amine
-
-
4-[4-fluoro-5-methoxy-2-[4-(trifluoromethyl)phenyl]-2,3-dihydro-1H-inden-1-yl]-1-methyl-1H-imidazol-2-amine
-
highly active BACE-1 inhibitor
4-[5-methoxy-2-(2-methoxy-5-nitrophenyl)-2,3-dihydro-1H-inden-1-yl]-1-methyl-1H-imidazol-2-amine
-
-
4-[5-methoxy-2-[4-(trifluoromethyl)phenyl]-2,3-dihydro-1H-inden-1-yl]-1-methyl-1H-imidazol-2-amine
-
-
4-[8-benzyl-4-(cyclohexylamino)-2-oxo-1,3,8-triazaspiro[4.5]dec-3-en-1-yl]benzamide
-
-
5-[2-amino-4-(4-methoxy-3-methylphenyl)-1-methyl-5-oxo-4,5-dihydro-1H-imidazol-4-yl]biphenyl-2-carbonitrile
-
5-[2-amino-4-(biphenyl-3-yl)-1-methyl-5-oxo-4,5-dihydro-1H-imidazol-4-yl]-2-methoxybenzonitrile
-
6,7-furano-5,8a-dimethoxy hydrocoumaric acid methyl ester
-
inhibits 57.2% of the BACE1 activity at a concentration of 1 mM
6,7-furano-5-methoxy hydrocoumaric acid
-
-
6,7-furano-5-methoxy hydrocoumaric acid methyl ester
-
-
6,7-furano-5-prenyloxy hydrocoumaric acid
-
-
6,7-furano-5-prenyloxy hydrocoumaric acid methyl ester
-
-
6,7-furano-8,8a-dimethoxy hydrocoumaric acid methyl ester
-
inhibits 48.3% of the BACE1 activity at a concentration of 1 mM
6,7-furano-8-methoxy hydrocoumaric acid
-
-
6,7-furano-8-methoxy hydrocoumaric acid methyl ester
-
inhibits 36.4% of the BACE1 activity at a concentration of 1 mM
6,7-furano-8a-methoxy-5-prenyloxy hydrocoumaric acid
-
-
6,7-furano-8a-methoxy-5-prenyloxy hydrocoumaric acid methyl ester
-
competitive-type inhibitor
6-([2-(2-chlorophenyl)-5-[4-(1,3-thiazol-2-yloxy)phenyl]-1H-pyrrol-1-yl]methyl)pyridin-2-amine
-
3.4% inhibition at 0.0125 mM
6-([2-(2-chlorophenyl)-5-[4-(hexyloxy)phenyl]-1H-pyrrol-1-yl]methyl)pyridin-2-amine
-
13% inhibition at 0.0125 mM
6-([2-(2-chlorophenyl)-5-[4-(pentyloxy)phenyl]-1H-pyrrol-1-yl]methyl)pyridin-2-amine
-
31% inhibition at 0.0125 mM
6-([2-(2-chlorophenyl)-5-[4-(pyrazin-2-yloxy)phenyl]-1H-pyrrol-1-yl]methyl)pyridin-2-amine
-
46.6% inhibition at 0.0125 mM
6-([2-(2-chlorophenyl)-5-[4-(pyridazin-3-yloxy)phenyl]-1H-pyrrol-1-yl]methyl)pyridin-2-amine
-
10.4% inhibition at 0.0125 mM
6-([2-(2-chlorophenyl)-5-[4-(pyridin-2-yloxy)phenyl]-1H-pyrrol-1-yl]methyl)pyridin-2-amine
-
6.61% inhibition at 0.0125 mM
6-([2-(2-chlorophenyl)-5-[4-(pyridin-3-yloxy)phenyl]-1H-pyrrol-1-yl]methyl)pyridin-2-amine
-
7.1% inhibition at 0.0125 mM
6-([2-(2-chlorophenyl)-5-[4-(pyridin-4-yloxy)phenyl]-1H-pyrrol-1-yl]methyl)pyridin-2-amine
-
7.22% inhibition at 0.0125 mM
6-([2-(2-chlorophenyl)-5-[4-(pyrimidin-2-yloxy)phenyl]-1H-pyrrol-1-yl]methyl)pyridin-2-amine
-
9.7% inhibition at 0.0125 mM
6-[(2,5-diphenyl-1H-pyrrol-1-yl)methyl]pyridin-2-amine
-
15% inhibition at 0.0125 mM
6-[[2-(2-chlorophenyl)-5-(4-methoxyphenyl)-1H-pyrrol-1-yl]methyl]pyridin-2-amine
-
30% inhibition at 0.0125 mM
6-[[2-(2-chlorophenyl)-5-(4-phenoxyphenyl)-1H-pyrrol-1-yl]methyl]pyridin-2-amine
-
16% inhibition at 0.0125 mM
6-[[2-(2-chlorophenyl)-5-(4-propoxyphenyl)-1H-pyrrol-1-yl]methyl]pyridin-2-amine
-
48% inhibition at 0.0125 mM
6-[[2-(4-butoxyphenyl)-5-(2-chlorophenyl)-1H-pyrrol-1-yl]methyl]pyridin-2-amine
-
31% inhibition at 0.0125 mM
7-phloroethol
-
significant BACE1 inhibition in a dose-dependent manner
8,8-diphenyl-2,3,4,8-tetrahydroimidazo[1,5-a]pyrimidin-6-amine
-
-
8-(biphenyl-4-ylmethyl)-4-(cyclohexylamino)-1-(4-fluorobenzyl)-1,3,8-triazaspiro[4.5]dec-3-en-2-one
-
-
8-benzyl-4-(cyclohexylamino)-1-(3-fluorophenyl)-1,3,8-triazaspiro[4.5]dec-3-en-2-one
-
-
benzyl 1-(3-acetoxypropyl)-5-((2S,3R)-4-(cyclopropylamino)-3-hydroxy-1-phenylbutan-2-ylcarbamoyl)-2,4,6-trimethyl-1,4-dihydropyridine-3-carboxylate
-
-
benzyl 5-((2S,3R)-4-(cyclopropylamino)-3-hydroxy-1-phenylbutan-2-ylcarbamoyl)-1-(2-(dimethylamino)-2-oxoethyl)-2,4,6-trimethyl-1,4-dihydropyridine-3-carboxylate
-
-
benzyl 5-((2S,3R)-4-(cyclopropylamino)-3-hydroxy-1-phenylbutan-2-ylcarbamoyl)-1-(2-(isopropyl(methyl)amino)-2-oxoethyl)-2,4,6-trimethyl-1,4-dihydropyridine-3-carboxylate
-
-
benzyl 5-((2S,3R)-4-(cyclopropylamino)-3-hydroxy-1-phenylbutan-2-ylcarbamoyl)-1-(2-ethoxy-2-oxoethyl)-2,4,6-trimethyl-1,4-dihydropyridine-3-carboxylate
-
-
benzyl 5-((2S,3R)-4-(cyclopropylamino)-3-hydroxy-1-phenylbutan-2-ylcarbamoyl)-1-(2-isopropoxy-2-oxoethyl)-2,4,6-trimethyl-1,4-dihydropyridine-3-carboxylate
-
-
benzyl 5-((2S,3R)-4-(cyclopropylamino)-3-hydroxy-1-phenylbutan-2-ylcarbamoyl)-1-(2-isopropoxy-2-oxoethyl)-2,4-dimethyl-1,4-dihydropyridine-3-carboxylate
-
-
benzyl 5-((2S,3R)-4-(cyclopropylamino)-3-hydroxy-1-phenylbutan-2-ylcarbamoyl)-1-(2-methoxy-2-oxoethyl)-2,4,6-trimethyl-1,4-dihydropyridine-3-carboxylate
-
-
benzyl 5-((2S,3R)-4-(cyclopropylamino)-3-hydroxy-1-phenylbutan-2-ylcarbamoyl)-2,4,6-trimethyl-1-(2-morpholino-2-oxoethyl)-1,4-dihydropyridine-3-carboxylate
-
-
benzyl 5-((2S,3R)-4-(cyclopropylamino)-3-hydroxy-1-phenylbutan-2-ylcarbamoyl)-2,4,6-trimethyl-1-(methylsulfonyl)-1,4-dihydropyridine-3-carboxylate
-
-
benzyl 5-((2S,3R)-4-(cyclopropylamino)-3-hydroxy-1-phenylbutan-2-ylcarbamoyl)-2,6-dimethyl-1-(methylsulfonyl)-4-phenyl-1,4-dihydropyridine-3-carboxylate
-
-
benzyl 5-((2S,3R)-4-(cyclopropylamino)-3-hydroxy-1-phenylbutan-2-ylcarbamoyl)-2,6-dimethyl-1-(methylsulfonyl)-4-propyl-1,4-dihydropyridine-3-carboxylate
-
-
benzyl 5-((2S,3R)-4-(cyclopropylamino)-3-hydroxy-1-phenylbutan-2-ylcarbamoyl)-4-ethyl-2,6-dimethyl-1-(methylsulfonyl)-1,4-dihydropyridine-3-carboxylate
-
-
benzyl 5-((2S,3R)-4-(cyclopropylamino)-3-hydroxy-1-phenylbutan-2-ylcarbamoyl)-4-isopropyl-2,6-dimethyl-1-(methylsulfonyl)-1,4-dihydropyridine-3-carboxylate
-
-
benzyl [(2S)-1-([(2S,3R)-1-(3,5-difluorophenyl)-4-[(3-ethylbenzyl)amino]-3-hydroxybutan-2-yl]amino)-3-(heptan-4-ylsulfonyl)-1-oxopropan-2-yl]carbamate
-
-
benzyl [2-([1-benzyl-2-hydroxy-3-[(3-methoxybenzyl)amino]propyl]amino)-2-oxo-1-[[(1-propylbutyl)sulfonyl]methyl]ethyl]carbamate
-
-
beta-secretase inhibitor IV
-
complete inhibition at 0.001 mM
cis-4-[(13S)-15-amino-13-cyclohexyl-11-oxo-2-oxa-10,14,16-triazatetracyclo[12.5.3.1(3,7).0(17,21)]tricosa-1(19),3(23),4,6,15,17,20-heptaen-10-yl]cyclohexanecarboxylic acid
-
-
dieckol
-
significant BACE1 inhibition in a dose-dependent manner
dioxinodehydroeckol
-
significant BACE1 inhibition in a dose-dependent manner
eckol
-
significant BACE1 inhibition in a dose-dependent manner
EVD(statine)VAEF
-
IC50: 0.000651 mM
EVE(statine)VAEF
-
IC50: 0.00045 mM
EVG(statine)VAEF
-
IC50: 0.005319 mM
EVL(statine)VAEF
-
IC50: 0.000265 mM
EVNLAAEF
-
Leu in the transition state isostere, i.e. OM99-2, IC50: 0.0000016 mM
EVW(statine)VAEF
-
IC50: 0.00754 mM
EVY(statine)VAEF
-
IC50: 0.000118 mM
heparin
-
leads to increased autocatalytic cleavage of beta-secretase and a subsequent loss of enzyme activity in vitro
heparin sulfate
-
heparin sulfate analogue derived from porcine mucosal intestinal heparin are effective beta-secretase inhibitors, but have negligible activity as anticoagulants or as inhibitors of other aspartyl proteases structurally related to beta-secretase. The structure of the polysaccharide is important for the interaction with beta-secretase, not simply the level of sulfation or charge
isopropyl 2-(3-((2S,3R)-3-hydroxy-4-(3-methoxyphenylamino)-1-phenylbutan-2-ylcarbamoyl)-5-((R)-1-phenylethylcarbamoyl)-4-propylpyridin-1(4H)-yl)acetate
-
-
isopropyl 2-(3-((2S,3R)-4-(cyclopropylamino)-3-hydroxy-1-phenylbutan-2-ylcarbamoyl)-4-methyl-5-((R)-1-phenylethylcarbamoyl)pyridin-1(4H)-yl) acetate
-
-
isopropyl 2-(3-((2S,3R)-4-(cyclopropylamino)-3-hydroxy-1-phenylbutan-2-ylcarbamoyl)-5-((R)-1-phenylethylcarbamoyl)-4-propylpyridin-1(4H)-yl)acetate
-
-
isopropyl 2-(3-acetyl-5-((2S,3R)-3-hydroxy-4-(3-methoxybenzylamino)-1-phenyl butan-2-ylcarbamoyl)-2,6-dimethyl-4-propylpyridin-1(4H)-yl)acetate
-
-
isopropyl 2-(3-acetyl-5-((2S,3R)-3-hydroxy-4-(3-methoxybenzylamino)-1-phenylbutan-2-ylcarbamoyl)-2,4-dimethylpyridin-1(4H)-yl)acetate
-
-
isopropyl 2-(3-acetyl-5-((2S,3R)-3-hydroxy-4-(3-methoxyphenylamino)-1-phenylbutan-2-ylcarbamoyl)-2,6-dimethyl-4-propylpyridin-1(4H)-yl)acetate
-
-
isopropyl 2-(3-acetyl-5-((2S,3R)-4-(3-fluorophenylamino)-3-hydroxy-1-phenylbutan-2-ylcarbamoyl)-2,4,6-trimethylpyridin-1(4H)-yl)acetate
-
-
isopropyl 2-(3-acetyl-5-((2S,3R)-4-(3-fluorophenylamino)-3-hydroxy-1-phenylbutan-2-ylcarbamoyl)-2,4-dimethylpyridin-1(4H)-yl)acetate
-
-
isopropyl 2-(3-acetyl-5-((2S,3R)-4-(3-fluorophenylamino)-3-hydroxy-1-phenylbutan-2-ylcarbamoyl)-2,6-dimethyl-4-propylpyridin-1(4H)-yl)acetate
-
-
isopropyl 2-(3-acetyl-5-((2S,3R)-4-(cyclopropylamino)-3-hydroxy-1-phenylbutan-2-ylcarbamoyl)-2,4,6-trimethylpyridin-1(4H)-yl)acetate
-
-
isopropyl 2-(3-acetyl-5-((2S,3R)-4-(cyclopropylamino)-3-hydroxy-1-phenylbutan-2-ylcarbamoyl)-2,6-dimethyl-4-propylpyridin-1(4H)-yl)acetate
-
-
KTEEISEVN(statine)VAEF
-
0.000055 mM
kuwanon
-
prenylated flavone from the stem bark of Morus lhou, noncompetitive
kuwanon A
-
prenylated flavone from the stem bark of Morus lhou, noncompetitive
L-alpha-glutamyl-L-leucyl-N-[(2S,5S,8S,14R)-2-carboxy-5-(carboxymethoxy)-13-hydroxy-11,16-dimethyl-13-oxido-4,7,10-trioxo-1-phenyl-8-(propan-2-yl)-3,6,9-triaza-13-lambda5-phosphaheptadecan-14-yl]-L-alpha-asparagine
-
-
L-alpha-glutamyl-L-valyl-N-((1S,2R)-1-benzyl-3-[(3,5-di-2H-tetrazol-5-ylphenyl)amino]-2-hydroxy-3-oxopropyl)-L-leucinamide
-
0.002 mM, 99.7% inhibition
L-alpha-glutamyl-L-valyl-N-((1S,2R)-1-benzyl-3-[(3,5-dicarboxyphenyl)amino]-2-hydroxy-3-oxopropyl)-L-leucinamide
-
0.002 mM, 98.3% inhibition
L-alpha-glutamyl-L-valyl-N-((1S,2R)-1-benzyl-3-[(3-carbamoylphenyl)amino]-2-hydroxy-3-oxopropyl)-L-leucinamide
L-alpha-glutamyl-L-valyl-N-((1S,2R)-1-benzyl-3-[(3-carboxyphenyl)amino]-2-hydroxy-3-oxopropyl)-L-leucinamide
-
0.002 mM, 83.7% inhibition
L-alpha-glutamyl-L-valyl-N-[(1S,2R)-1-benzyl-2-hydroxy-3-([3-(4-methyl-5-thioxo-4,5-dihydro-1H-1,2,4-triazol-3-yl)phenyl]amino)-3-oxopropyl]-L-leucinamide
-
0.002 mM, 74.2% inhibition
L-alpha-glutamyl-L-valyl-N-[(1S,2R)-1-benzyl-2-hydroxy-3-oxo-3-([3-(2H-tetrazol-5-yl)phenyl]amino)propyl]-L-leucinamide
-
0.002 mM, 92.2% inhibition
L-alpha-glutamyl-L-valyl-N-[(1S,2R)-1-benzyl-2-hydroxy-3-oxo-3-([3-(5-oxo-4,5-dihydro-1,2,4-oxadiazol-3-yl)phenyl]amino)propyl]-L-leucinamide
-
0.002 mM, 94.4% inhibition
L-alpha-glutamyl-L-valyl-N-[(1S,2R)-1-benzyl-2-hydroxy-3-oxo-3-([3-(5-oxo-4,5-dihydro-1,2,4-thiadiazol-3-yl)phenyl]amino)propyl]-L-leucinamide
-
0.002 mM, 91.9% inhibition
L-alpha-glutamyl-L-valyl-N-[(1S,2R)-1-benzyl-2-hydroxy-3-oxo-3-([3-(5-thioxo-4,5-dihydro-1,2,4-oxadiazol-3-yl)phenyl]amino)propyl]-L-leucinamide
-
-
Lys-Thr-Glu-Glu-Ile-Ser-Glu-Val-Asn-(statine)-Val-Ala-Glu-Phe-OH
-
-
Lys-Thr-Glu-Glu-Ile-Ser-Glu-Val-Asn-Sta-Val-Ala-Glu-Phe
-
complete inhibition at 0.1 mM
Lys-Thr-Glu-Glu-Ile-Ser-Glu-Val-Asn-[statine(3S,4S)]-Val-Ala-Glu-Phe-OH
-
-
methyl [(2S)-1-([(2S,3R)-1-(3,5-difluorophenyl)-4-[(3-ethylbenzyl)amino]-3-hydroxybutan-2-yl]amino)-3-(heptan-4-ylsulfonyl)-1-oxopropan-2-yl]carbamate
-
-
morusin
-
prenylated flavone from the stem bark of Morus lhou, noncompetitive
N'-[(2S,3R)-1-(3,5-difluorophenyl)-3-hydroxy-4-[(3-iodobenzyl)amino]butan-2-yl]-5-methyl-N,N-dipropylbenzene-1,3-dicarboxamide
-
-
N'-[(2S,3R)-3-hydroxy-4-[(3-iodobenzyl)amino]-1-phenylbutan-2-yl]-N,N-dipropylbenzene-1,3-dicarboxamide
-
-
N'-[(2S,3R)-3-hydroxy-4-[(3-methoxybenzyl)amino]-1-phenylbutan-2-yl]-N,N-dipropylbenzene-1,3-dicarboxamide
-
-
N,N'-bis(3-cyano-4,5,6,7,8,9-hexahydrocycloocta[b]thiophen-2-yl)-2,2,3,3,4,4,5,5-octafluorohexanediamide
-
87% inhibition at 0.1 mM
N-((1S,2R)-1-benzyl-3-cyclopropylamino-2-hydroxy-propyl)-5-(methanesulfonyl-methyl-amino)-N'-((R)-1-phenyl-ethyl)-isophthalamide
N-(2-methyl-5-[(6-phenylpyrimidin-4-yl)amino]phenyl)methanesulfonamide
-
-
N-(2-methylpropyl)-N2-([17-[(methylsulfonyl)(propyl)amino]-2-oxo-3-azatricyclo[13.3.1.16,10]icosa-1(19),6(20),7,9,15,17-hexaen-4-yl]methyl)-L-norleucinamide
-
-
N-(4-([4-(cyclohexylamino)-1-(3-fluorophenyl)-2-oxo-1,3,8-triazaspiro[4.5]dec-3-en-8-yl]methyl)phenyl)acetamide
-
-
N-(4-fluorophenyl)-11-oxo-10,11-dihydro-5H-dibenzo[b,e]-[1,4]diazepine-3-carboxamide
-
-
N-(4-[1-[(6-aminopyridin-2-yl)methyl]-5-(2-chlorophenyl)-1H-pyrrol-2-yl]phenyl)pyrimidin-5-amine
-
9.8% inhibition at 0.0125 mM
N-(5-([6-(4-(N,N-dimethyl)aminophenyl)pyrimidin-4-yl]amino)-2-methylphenyl)-N-methylmethanesulfonamide
-
-
N-(5-[[6-(2,3-dihydro-1,4-benzodioxin-6-yl)pyrimidin-4-yl]amino]-2-methylphenyl)-N-methylmethanesulfonamide
-
-
N-(tert-butoxycarbonyl)-L-isoleucyl-N-[(4S,5S,7R)-5-hydroxy-2,7-dimethyl-8-[(2-methylpropyl)amino]-8-oxooctan-4-yl]-L-phenylalaninamide
-
no inhibition at 0.01 mg/ml
N-(tert-butoxycarbonyl)-L-isoleucyl-N-[(4S,5S,7R)-8-(benzylamino)-5-hydroxy-2,7-dimethyl-8-oxooctan-4-yl]-L-phenylalaninamide
-
no inhibition at 0.01 mg/ml
N-(tert-butoxycarbonyl)-L-leucyl-N-[(4S,5S,7R)-5-hydroxy-2,7-dimethyl-8-[(2-methylpropyl)amino]-8-oxooctan-4-yl]-L-phenylalaninamide
-
54.57% inhibition at 0.01 mg/ml
N-(tert-butoxycarbonyl)-L-leucyl-N-[(4S,5S,7R)-8-(benzylamino)-5-hydroxy-2,7-dimethyl-8-oxooctan-4-yl]-L-phenylalaninamide
-
0.91% inhibition at 0.01 mg/ml
N-(tert-butoxycarbonyl)-L-valyl-N-[(4S,5S,7R)-5-hydroxy-2,7-dimethyl-8-[(2-methylpropyl)amino]-8-oxooctan-4-yl]-L-phenylalaninamide
-
no inhibition at 0.01 mg/ml
N-(tert-butoxycarbonyl)-L-valyl-N-[(4S,5S,7R)-8-(benzylamino)-5-hydroxy-2,7-dimethyl-8-oxooctan-4-yl]-L-phenylalaninamide
-
no inhibition at 0.01 mg/ml
N-(tert-butoxycarbonyl)valyl-N-[(2S,4R)-2-hydroxy-4-methyl-5-([(1S)-2-methyl-1-[(1-methylethyl)carbamoyl]propyl]amino)-1-(2-methylpropyl)-5-oxopentyl]-L-methioninamide
-
-
N-acetyl-beta-alanyl-3-(butylsulfonyl)-N-[(2S,3R)-1-(3,5-difluorophenyl)-4-[(3-ethylbenzyl)amino]-3-hydroxybutan-2-yl]-D-alaninamide
-
-
N-acetyl-L-alanyl-N-[(4S,5S,7R)-8-(butylamino)-5-hydroxy-2,7-dimethyl-8-oxooctan-4-yl]-L-methioninamide
-
-
N-acetyl-L-leucyl-N-[(4S,5S,7R)-8-(butylamino)-5-hydroxy-2,7-dimethyl-8-oxooctan-4-yl]-L-alaninamide
-
-
N-acetyl-L-leucyl-N-[(4S,5S,7R)-8-(butylamino)-5-hydroxy-2,7-dimethyl-8-oxooctan-4-yl]-L-methioninamide
-
-
N-acetyl-L-valyl-N-[(4S,5S,7R)-8-(butylamino)-5-hydroxy-2,7-dimethyl-8-oxooctan-4-yl]-L-methioninamide
-
-
N-[(1R,2S)-1-benzyl-2-hydroxy-3-[[3-(trifluoromethyl)benzyl]amino]propyl]-3-(1,1-dioxido-1,2-thiazinan-2-yl)-5-(ethylamino)-2-fluorobenzamide
-
-
N-[(1S)-1-[(butylsulfonyl)methyl]-2-([1-(3,5-difluorobenzyl)-3-[(3-ethylbenzyl)amino]-2-hydroxypropyl]amino)-2-oxoethyl]benzamide
-
-
N-[(1S,2R)-1-benzyl-2-hydroxy-3-[(3-ethoxybenzyl)amino]propyl]-5-[methyl(methylsulfonyl)amino]-N'-[(1R)-1-phenylethyl]benzene-1,3-dicarboxamide
-
-
N-[(1Z)-amino(butylamino)methylidene]-2-[2-(2-chlorophenyl)-5-(4-propoxyphenyl)-1H-pyrrol-1-yl]acetamide
-
-
N-[(2R)-1-([1-(3,5-difluorophenyl)-4-[(3-ethylbenzyl)amino]-3-hydroxybutan-2-yl]amino)-3-(heptan-4-ylsulfonyl)-1-oxopropan-2-yl]-2-methylbenzamide
-
-
N-[(2R)-1-([1-(3,5-difluorophenyl)-4-[(3-ethylbenzyl)amino]-3-hydroxybutan-2-yl]amino)-3-(heptan-4-ylsulfonyl)-1-oxopropan-2-yl]-3-hydroxybenzamide
-
-
N-[(2R)-1-([1-(3,5-difluorophenyl)-4-[(3-ethylbenzyl)amino]-3-hydroxybutan-2-yl]amino)-3-(heptan-4-ylsulfonyl)-1-oxopropan-2-yl]-4-(trifluoromethyl)benzamide
-
-
N-[(2R)-1-([1-(3,5-difluorophenyl)-4-[(3-ethylbenzyl)amino]-3-hydroxybutan-2-yl]amino)-3-(heptan-4-ylsulfonyl)-1-oxopropan-2-yl]-4-methoxybenzamide
-
-
N-[(2R)-1-([1-(3,5-difluorophenyl)-4-[(3-ethylbenzyl)amino]-3-hydroxybutan-2-yl]amino)-3-(heptan-4-ylsulfonyl)-1-oxopropan-2-yl]-4-methylbenzamide
-
-
N-[(2R)-1-([1-(3,5-difluorophenyl)-4-[(3-ethylbenzyl)amino]-3-hydroxybutan-2-yl]amino)-3-(heptan-4-ylsulfonyl)-1-oxopropan-2-yl]benzamide
-
-
N-[(2R)-1-([1-(3,5-difluorophenyl)-4-[(3-ethylbenzyl)amino]-3-hydroxybutan-2-yl]amino)-3-(heptan-4-ylsulfonyl)-1-oxopropan-2-yl]pyridine-2-carboxamide
-
-
N-[(2R)-2-amino-1-benzyl-3-fluoropropyl]-2-[[(2-methylcyclopropyl)methyl]amino]-6-[methyl[(1-methylethyl)sulfonyl]amino]pyridine-4-carboxamide
-
-
N-[(2S)-1-([(4S,5S,7R)-5-hydroxy-2,7-dimethyl-8-[(2-methylpropyl)amino]-8-oxooctan-4-yl]amino)-1-oxo-3-phenylpropan-2-yl]naphthalene-1-carboxamide
-
no inhibition at 0.01 mg/ml
N-[(2S)-1-([(4S,5S,7R)-5-hydroxy-2,7-dimethyl-8-[(2-methylpropyl)amino]-8-oxooctan-4-yl]amino)-3-(4-nitrophenyl)-1-oxopropan-2-yl]naphthalene-1-carboxamide
-
no inhibition at 0.01 mg/ml
N-[(2S)-3-(butylsulfonyl)-1-([(2S,3R)-1-(3,5-difluorophenyl)-4-[(3-ethylbenzyl)amino]-3-hydroxybutan-2-yl]amino)-1-oxopropan-2-yl]-1H-imidazole-2-carboxamide
-
-
N-[(2S)-3-(butylsulfonyl)-1-([(2S,3R)-1-(3,5-difluorophenyl)-4-[(3-ethylbenzyl)amino]-3-hydroxybutan-2-yl]amino)-1-oxopropan-2-yl]-4-hydroxypyridine-3-carboxamide
-
-
N-[(2S)-3-(butylsulfonyl)-1-([(2S,3R)-1-(3,5-difluorophenyl)-4-[(3-ethylbenzyl)amino]-3-hydroxybutan-2-yl]amino)-1-oxopropan-2-yl]-5-methyl-1H-pyrazole-3-carboxamide
-
-
N-[(2S)-3-(butylsulfonyl)-1-([(2S,3R)-1-(3,5-difluorophenyl)-4-[(3-ethylbenzyl)amino]-3-hydroxybutan-2-yl]amino)-1-oxopropan-2-yl]pyrazine-2-carboxamide
-
-
N-[(2S)-3-(butylsulfonyl)-1-([(2S,3R)-1-(3,5-difluorophenyl)-4-[(3-ethylbenzyl)amino]-3-hydroxybutan-2-yl]amino)-1-oxopropan-2-yl]pyridine-3-carboxamide
-
-
N-[(2S)-3-(butylsulfonyl)-1-([(2S,3R)-1-(3,5-difluorophenyl)-4-[(3-ethylbenzyl)amino]-3-hydroxybutan-2-yl]amino)-1-oxopropan-2-yl]pyridine-4-carboxamide
-
-
N-[(2S,3R)-1-(3,5-difluorophenyl)-3-hydroxy-4-[(3-iodobenzyl)amino]butan-2-yl]-3-methylbenzamide
-
-
N-[(2S,3R)-3-hydroxy-4-[(3-methoxybenzyl)amino]-1-phenylbutan-2-yl]-3-(phenylsulfonyl)propanamide
-
-
N-[(2S,3R)-3-hydroxy-4-[(3-methoxybenzyl)amino]-1-phenylbutan-2-yl]-3-(piperidin-1-ylsulfonyl)propanamide
-
-
N-[(2S,3R)-3-hydroxy-4-[(3-methoxybenzyl)amino]-1-phenylbutan-2-yl]-3-[(3-methylbutyl)sulfamoyl]propanamide
-
-
N-[(2S,3R)-3-hydroxy-4-[(3-methoxybenzyl)amino]-1-phenylbutan-2-yl]-3-[(3-methylbutyl)sulfonyl]propanamide
-
-
N-[(2S,3R)-3-hydroxy-4-[(3-methoxybenzyl)amino]-1-phenylbutan-2-yl]-4-(phenylsulfonyl)butanamide
-
-
N-[(2S,3R)-3-hydroxy-4-[(3-methoxybenzyl)amino]-1-phenylbutan-2-yl]-4-(piperidin-1-ylsulfonyl)butanamide
-
-
N-[(2S,3S)-4-(cyclopropylamino)-3-hydroxy-1-phenylbutan-2-yl]-N'-[(1R)-1-(4-fluorophenyl)ethyl]-5-[(methylsulfonyl)amino]benzene-1,3-dicarboxamide
-
-
N-[(2S,4R)-2-hydroxy-4-methyl-5-([(1S)-2-methyl-1-[(2-methylpropyl)carbamoyl]propyl]amino)-1-(2-methylpropyl)-5-oxopentyl]-5-[methyl(methylsulfonyl)amino]-N'-(1-phenylethyl)benzene-1,3-dicarboxamide
-
-
N-[(3S,6S,13R)-13-[(3-[[(2S)-1-[[(1S)-1-(carboxymethoxy)-2-[[(1S)-1-carboxy-2-phenylethyl]amino]-2-oxoethyl]amino]-3-methyl-1-oxobutan-2-yl]amino]-2-methyl-3-oxopropyl)(hydroxy)phosphoryl]-3-(carboxymethyl)-2,5-dioxo-1,4-diazacyclotridecan-6-yl]-L-alpha-glutamine
-
-
N-[(4S)-4-[(1R)-1-hydroxy-2-([1-[3-(propan-2-yl)phenyl]cyclopropyl]amino)ethyl]-2-oxo-11-oxa-3,16-diazatricyclo[15.3.1.1(6,10)]docosa-1(21),6(22),7,9,17,19-hexaen-19-yl]-N-methylpropane-1-sulfonamide
-
-
N-[(4S)-4-[(1R)-1-hydroxy-2-[[3-(propan-2-yl)benzyl]amino]ethyl]-2-oxo-11-oxa-3,16-diazatricyclo[15.3.1.1(6,10)]docosa-1(21),6(22),7,9,17,19-hexaen-19-yl]-N-methylpropane-1-sulfonamide
-
-
N-[(4S,5S,7R)-2-[7-(1-benzylpiperidin-4-yl)]methylcarbamoyl-5-hydroxy-2-methyloct-4-yl]-N'-[(R)-1-(4-fluorophenyl)ethyl-5-methyl(methylsulfonyl)amino]isophthalamide
-
-
N-[(4S,5S,7R)-5-hydroxy-2,7-dimethyl-8-[(2-methylpropyl)amino]-8-oxooctan-4-yl]-4-nitro-Nalpha-(4-nitrobenzoyl)-L-phenylalaninamide
-
10.48% inhibition at 0.01 mg/ml
N-[(4S,5S,7R)-5-hydroxy-2,7-dimethyl-8-[(2-methylpropyl)amino]-8-oxooctan-4-yl]-4-nitro-Nalpha-[(2Z)-3-phenylprop-2-enoyl]-L-phenylalaninamide
-
37.22% inhibition at 0.01 mg/ml
N-[(4S,5S,7R)-5-hydroxy-2,7-dimethyl-8-[(2-methylpropyl)amino]-8-oxooctan-4-yl]-4-nitro-Nalpha-[(2Z)-3-[4-(trifluoromethyl)phenyl]prop-2-enoyl]-L-phenylalaninamide
-
0.13% inhibition at 0.01 mg/ml
N-[(4S,5S,7R)-5-hydroxy-2,7-dimethyl-8-[(2-methylpropyl)amino]-8-oxooctan-4-yl]-Nalpha-(4-nitrobenzoyl)-L-phenylalaninamide
-
1.47% inhibition at 0.01 mg/ml
N-[(4S,5S,7R)-5-hydroxy-2,7-dimethyl-8-[(2-methylpropyl)amino]-8-oxooctan-4-yl]-Nalpha-[(2Z)-3-phenylprop-2-enoyl]-L-phenylalaninamide
-
22.83% inhibition at 0.01 mg/ml
N-[(4S,5S,7R)-5-hydroxy-2,7-dimethyl-8-[(2-methylpropyl)amino]-8-oxooctan-4-yl]-Nalpha-[(2Z)-3-[4-(trifluoromethyl)phenyl]prop-2-enoyl]-L-phenylalaninamide
-
59.66% inhibition at 0.01 mg/ml
N-[(4S,5S,7R)-8-(benzylamino)-5-hydroxy-2,7-dimethyl-8-oxooctan-4-yl]-Nalpha-(tert-butoxycarbonyl)-L-phenylalaninamide
-
22.96% inhibition at 0.01 mg/ml
N-[(5R)-5-amino-5-methyl-4,16-dioxo-14-phenyl-3-oxa-15-azatricyclo[15.3.1.17,11]docosa-1(21),7(22),8,10,17,19-hexaen-19-yl]-N-methylmethanesulfonamide
-
-
N-[(Z)-[(4,6-dimethylpyrimidin-2-yl)amino][(3-nitrophenyl)amino]methylidene]-10H-phenothiazine-10-carboxamide
-
80% inhibition at 0.1 mM
N-[1-(3,5-difluorobenzyl)-2-hydroxy-3-[(3-iodobenzyl)amino]propyl]-5-methyl-N'-propylbenzene-1,3-dicarboxamide
-
-
N-[1-(3,5-difluorobenzyl)-2-hydroxy-3-[(3-methoxybenzyl)amino]propyl]-5-methyl-N'-propylbenzene-1,3-dicarboxamide
-
-
N-[2-(3,4-dimethoxyphenyl)ethyl]-2-[(6-[[4,6-di(piperidin-1-yl)-1,3,5-triazin-2-yl]amino]-1,3-benzothiazol-2-yl)sulfanyl]acetamide
-
80% inhibition at 0.1 mM
N-[5-(2,3-dichlorobenzyl)-1,3-thiazol-2-yl]-4-([[4-phenyl-5-(pyridin-4-yl)-4H-1,2,4-triazol-3-yl]sulfanyl]methyl)benzamide
-
78% inhibition at 0.1 mM
N1-[1-(3,5-difluorobenzyl)-2-hydroxy-3-[(3-methoxybenzyl)amino]propyl]-N3-propylbenzene-1,3,5-tricarboxamide
-
-
N1-[1-(3,5-difluorobenzyl)-3-[(3-ethylbenzyl)amino]-2-hydroxypropyl]-N3-propylbenzene-1,3,5-tricarboxamide
-
-
N2-acetyl-3-(butylsulfonyl)-N-[(2S,3R)-1-(3,5-difluorophenyl)-4-[(3-ethylbenzyl)amino]-3-hydroxybutan-2-yl]-D-alaninamide
-
-
N2-[(2R,4S)-5-[[N-[[(2,5-dimethyl-1,3-oxazol-4-yl)methoxy]carbonyl]-3-(methylsulfonyl)-L-alanyl]amino]-4-hydroxy-2,7-dimethyloctanoyl]-N-(2-methylpropyl)-L-valinamide
-
-
N2-[(2R,4S)-5-[[N-[[(3,5-dimethyl-1H-pyrazol-1-yl)methoxy]carbonyl]-3-(methylsulfonyl)-L-alanyl]amino]-4-hydroxy-2,7-dimethyloctanoyl]-N-(2-methylpropyl)-L-valinamide
-
-
N3-((2S,3R)-4-(cyclopropylamino)-3-hydroxy-1-phenylbutan-2-yl)-2,4,6-trimethyl-1-(methylsulfonyl)-N5-((R)-1-phenylethyl)-1,4-dihydropyridine-3,5-dicarboxamide
-
-
N3-((2S,3R)-4-(cyclopropylamino)-3-hydroxy-1-phenylbutan-2-yl)-4-ethyl-2,6-dimethyl-1-(methylsulfonyl)-N5-((R)-1-phenylethyl)-1,4-dihydropyridine-3,5-dicarboxamide
-
-
Nalpha-(1,3-benzodioxol-5-ylcarbonyl)-N-[(4S,5S,7R)-5-hydroxy-2,7-dimethyl-8-[(2-methylpropyl)amino]-8-oxooctan-4-yl]-4-nitro-L-phenylalaninamide
-
40.29% inhibition at 0.01 mg/ml
Nalpha-(1,3-benzodioxol-5-ylcarbonyl)-N-[(4S,5S,7R)-5-hydroxy-2,7-dimethyl-8-[(2-methylpropyl)amino]-8-oxooctan-4-yl]-L-phenylalaninamide
-
16.2% inhibition at 0.01 mg/ml
Nalpha-(2,4-dichlorobenzoyl)-N-[(4S,5S,7R)-5-hydroxy-2,7-dimethyl-8-[(2-methylpropyl)amino]-8-oxooctan-4-yl]-4-nitro-L-phenylalaninamide
-
22.23% inhibition at 0.01 mg/ml
Nalpha-(2,4-dichlorobenzoyl)-N-[(4S,5S,7R)-5-hydroxy-2,7-dimethyl-8-[(2-methylpropyl)amino]-8-oxooctan-4-yl]-L-phenylalaninamide
-
20.26% inhibition at 0.01 mg/ml
Nalpha-(3,4-dimethoxybenzoyl)-N-[(4S,5S,7R)-5-hydroxy-2,7-dimethyl-8-[(2-methylpropyl)amino]-8-oxooctan-4-yl]-4-nitro-L-phenylalaninamide
-
18.3% inhibition at 0.01 mg/ml
Nalpha-(3,5-dinitrobenzoyl)-N-[(4S,5S,7R)-5-hydroxy-2,7-dimethyl-8-[(2-methylpropyl)amino]-8-oxooctan-4-yl]-4-nitro-L-phenylalaninamide
-
7.61% inhibition at 0.01 mg/ml
Nalpha-(3,5-dinitrobenzoyl)-N-[(4S,5S,7R)-5-hydroxy-2,7-dimethyl-8-[(2-methylpropyl)amino]-8-oxooctan-4-yl]-L-phenylalaninamide
-
0.91% inhibition at 0.01 mg/ml
Nalpha-(3-chlorobenzoyl)-N-[(4S,5S,7R)-5-hydroxy-2,7-dimethyl-8-[(2-methylpropyl)amino]-8-oxooctan-4-yl]-4-nitro-L-phenylalaninamide
-
25.66% inhibition at 0.01 mg/ml
Nalpha-(3-chlorobenzoyl)-N-[(4S,5S,7R)-5-hydroxy-2,7-dimethyl-8-[(2-methylpropyl)amino]-8-oxooctan-4-yl]-L-phenylalaninamide
-
16.92% inhibition at 0.01 mg/ml
Nalpha-(tert-butoxycarbonyl)-N-[(4S,5S,7R)-5-hydroxy-2,7-dimethyl-8-[(2-methylpropyl)amino]-8-oxooctan-4-yl]-4-nitro-L-phenylalaninamide
-
30.06% inhibition at 0.01 mg/ml
Nalpha-(tert-butoxycarbonyl)-N-[(4S,5S,7R)-5-hydroxy-2,7-dimethyl-8-[(2-methylpropyl)amino]-8-oxooctan-4-yl]-L-phenylalaninamide
-
25.76% inhibition at 0.01 mg/ml
Nalpha-benzoyl-N-[(4S,5S,7R)-5-hydroxy-2,7-dimethyl-8-[(2-methylpropyl)amino]-8-oxooctan-4-yl]-L-phenylalaninamide
-
11.2% inhibition at 0.01 mg/ml
pepstatin A
-
less potent inhibitor
phlorofurofucoeckol-A
-
significant BACE1 inhibition in a dose-dependent manner
phloroglucinol
-
significant BACE1 inhibition in a dose-dependent manner
pyridin-3-ylmethyl [(2S)-1-([(2S,3R)-1-(3,5-difluorophenyl)-4-[(3-ethylbenzyl)amino]-3-hydroxybutan-2-yl]amino)-3-(heptan-4-ylsulfonyl)-1-oxopropan-2-yl]carbamate
-
-
pyridin-4-ylmethyl [(2S)-1-([(2S,3R)-1-(3,5-difluorophenyl)-4-[(3-ethylbenzyl)amino]-3-hydroxybutan-2-yl]amino)-3-(heptan-4-ylsulfonyl)-1-oxopropan-2-yl]carbamate
-
-
quercetin
-
significant BACE1 inhibition in a dose-dependent manner
S-(tetrahydrofuran-3-yl) [(2S)-3-(butylsulfonyl)-1-([(2S,3R)-1-(3,5-difluorophenyl)-4-[(3-ethylbenzyl)amino]-3-hydroxybutan-2-yl]amino)-1-oxopropan-2-yl]carbamothioate
-
-
tert-butyl 5-((2S,3R)-3-hydroxy-4-(3-methoxyphenylamino)-1-phenylbutan-2-ylcarbamoyl)-1-(2-isopropoxy-2-oxoethyl)-4-propyl-1,4-dihydropyridine-3-carboxylate
-
-
tert-butyl 5-((2S,3R)-4-(cyclopropylamino)-3-hydroxy-1-phenylbutan-2-ylcarbamoyl)-1-(2-isopropoxy-2-oxoethyl)-4-methyl-1,4-dihydropyridine-3-carboxylate
-
-
tert-butyl 5-((2S,3R)-4-(cyclopropylamino)-3-hydroxy-1-phenylbutan-2-ylcarbamoyl)-1-(2-isopropoxy-2-oxoethyl)-4-propyl-1,4-dihydropyridine-3-carboxylate
-
-
tert-butyl [(2S)-1-[[(4S,5S,7R)-8-(benzylamino)-5-hydroxy-2,7-dimethyl-8-oxooctan-4-yl]amino]-3-hydroxy-1-oxopropan-2-yl]carbamate
-
50.53% inhibition at 0.01 mg/ml
trans-4-[(13S)-15-amino-13-cyclohexyl-11-oxo-2-oxa-10,14,16-triazatetracyclo[12.5.3.1(3,7).0(17,21)]tricosa-1(19),3(23),4,6,15,17,20-heptaen-10-yl]cyclohexanecarboxylic acid
-
-
triphloroethol A
-
significant BACE1 inhibition in a dose-dependent manner
[(1R,2R,4R,5S,6S)-2-hydroxy-7-sulfo-4-[(sulfooxy)methyl]-3-oxa-7-azabicyclo[4.1.0]hept-5-yl 2-O-sulfo-beta-D-glucopyranosiduronic acid]n
-
IC50: 0.000031 mg/ml
[(2R,4S,5S)-5-[N-(3,4-dimethoxy)benzoyl-L-phenylalanylamido]-4-hydroxy-2,7-dimethyloctan] N'-isobutyl amide
-
14.66% inhibition at 0.01 mg/ml
[2-(acetylamino)-2-deoxy-4-O-(2-O-sulfo-beta-D-glucopyranuronosyl)-beta-D-glucopyranose]n
-
IC50: 0.00041 mg/ml
[2-(acetylamino)-2-deoxy-4-O-beta-D-glucopyranuronosyl-6-O-sulfo-beta-D-glucopyranose]n
-
IC50: 0.000091 mg/ml
[2-(acetylamino)-2-deoxy-6-O-sulfo-4-O-(2-O-sulfo-beta-D-glucopyranuronosyl)-beta-D-glucopyranose]n
-
IC50: 0.000031 mg/ml
[2-amino-2-deoxy-6-O-sulfo-4-O-(2-O-sulfo-beta-D-glucopyranuronosyl)-beta-D-glucopyranose]n
-
IC50: 0.000159 mg/ml
[2-deoxy-2-(butanoylamino)-6-O-sulfo-4-O-(2-O-sulfo-beta-D-glucopyranuronosyl)-beta-D-glucopyranose]n
-
IC50: 0.000055 mg/ml
[2-deoxy-2-(propanoylamino)-6-O-sulfo-4-O-(2-O-sulfo-beta-D-glucopyranuronosyl)-beta-D-glucopyranose]n
-
IC50: 0.000053 mg/ml
[2-deoxy-2-(sulfoamino)-4-O-(2-O-sulfo-beta-D-glucopyranuronosyl)-beta-D-glucopyranose]n
-
IC50: 0.0001 mg/ml
[2-deoxy-4-O-(2,3-di-O-sulfo-beta-D-glucopyranuronosyl)-6-O-sulfo-2-(sulfoamino)-beta-D-glucopyranose]n
-
IC50: 0.000053 mg/ml
[2-deoxy-6-O-sulfo-2-(sulfoamino)-4-O-(2-O-sulfo-beta-D-glucopyranuronosyl)-beta-D-glucopyranose]n
-
porcine mucosal intestinal heparin, IC50: 0.000028 mg/ml
[3-([1-benzyl-2-hydroxy-3-[(1-methylethyl)amino]propyl]carbamoyl)-5-[(1-phenylethyl)carbamoyl]phenyl]methylsulfamic acid
-
-
[3-([1-benzyl-2-hydroxy-3-[(3-methylbenzyl)amino]propyl]carbamoyl)-5-[[(2,5-dimethyl-1,3-oxazol-4-yl)methyl]carbamoyl]phenyl]methylsulfamic acid
-
-
[3-[(1-[1-hydroxy-2-[(3-methoxybenzyl)amino]ethyl]-3-methylbutyl)carbamoyl]-5-[(1-phenylethyl)carbamoyl]phenyl]methylsulfamic acid
-
-
OM99-2
-
OM99-2
pH dependence of BACE1 activity in solution with and without OM99-2 shown, surface representation in the active site cleft with superimposed OM99-2 at pH 5 shown by crystallization, active and inactive structures determined
2-amino-5-[3-(2-fluoropyridin-3-yl)phenyl]-5-(4-methoxy-3-methylphenyl)-3-methyl-3,5-dihydro-4H-imidazol-4-one
-
-
2-amino-5-[3-(2-fluoropyridin-3-yl)phenyl]-5-(4-methoxy-3-methylphenyl)-3-methyl-3,5-dihydro-4H-imidazol-4-one
-
imperatorin
-
-
imperatorin
-
strongest inhibition of BACE1 activity
L-alpha-glutamyl-L-valyl-N-((1S,2R)-1-benzyl-3-[(3-carbamoylphenyl)amino]-2-hydroxy-3-oxopropyl)-L-leucinamide
-
0.002 mM, 29.2% inhibition
L-alpha-glutamyl-L-valyl-N-((1S,2R)-1-benzyl-3-[(3-carbamoylphenyl)amino]-2-hydroxy-3-oxopropyl)-L-leucinamide
-
0.002 mM, 62.1% inhibition
N-((1S,2R)-1-benzyl-3-cyclopropylamino-2-hydroxy-propyl)-5-(methanesulfonyl-methyl-amino)-N'-((R)-1-phenyl-ethyl)-isophthalamide
-
beta-secretase inhibitor IV
N-((1S,2R)-1-benzyl-3-cyclopropylamino-2-hydroxy-propyl)-5-(methanesulfonyl-methyl-amino)-N'-((R)-1-phenyl-ethyl)-isophthalamide
-
beta-secretase inhibitor IV, potent inhibitor
OM00-3
-
-
OM00-3
-
Glu-Leu-Asp-Leu*Ala-Val-Glu-Phe, the asterisk denotes a hydxoxyethelene transition state isostere
OM99-2
-
-
OM99-2
-
Glu-Val-Asn-Leu*Ala-Ala-Glu-Phe, the asterisk denotes a hydxoxyethelene transition state isostere
OM99-2
-
complete inhibition at 0.0001 nM
OM99-2
-
i.e. Glu-Val-Asn-(S)-CH(OH)CH2-Leu-Ala-Glu-Phe-OH
OM99-2
-
i.e. Glu-Val-Asn-[(2R,4S,5S)-5-amino-4-hydroxy-2,7-dimethyl-octanoyl]-Ala-Glu-Phe-OH, potent inhibitor
additional information
design of selective non-peptidic small molecule inhibitors of beta-secretase BACE1, substitution of a thiophene ring for the key pyrrole nucleus in a series of substituted acylguanidines performed
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additional information
isophthalic-type aromatic residues at the P2 position and an HMC isostere at the P1 position used as lead compounds for generation of novel inhibitors against beta-secretase BACE1, development of novel inhibitors against beta-secretase BACE1 studied, novel nonpeptidic and small-sized BACE1 inhibitors possessing a 2,6-pyridinedicarboxylic, chelidamic or chelidonic residue at the P2 position described, inhibitory activities summarized
-
additional information
membrane excitability normalized by BACE1 inhibitor GL189 in Alzheimer disease patients reveals association between BACE1 and regulatory role on voltage-gated sodium channel by cleavage of beta2 subunit
-
additional information
-
membrane excitability normalized by BACE1 inhibitor GL189 in Alzheimer disease patients reveals association between BACE1 and regulatory role on voltage-gated sodium channel by cleavage of beta2 subunit
-
additional information
structures of BACE1 inhibitors containing a tetrazole ring at the P4 position indicated, inhibitory activities summarized
-
additional information
a pyrrolidinyl side group at the P3' and P4' positions of the inhibitors are favored for strong inhibition and a small aromatic group at the P4 position is also essential to the potency
-
additional information
presence of a flavanone moiety in the amentoflavone biflavonoid is advantageous for inhibitory activity
-
additional information
BACE1 inhibitors possessing a chelidonic or 2,6-pyridinedicarboxylic scaffold at the P2 position. Small-sized and hydrophobic residues at the P2 and P3 positions are preferable for BACE1 inhibition. The membrane permeability of these non-peptidic BACE1 inhibitors is similar to that of peptidic compounds
-
additional information
not inhibited by 0.005 mM (+)-canadine, (+)-corydaline, (+)-tetrahydropalmatine, (+)-corydine, (+)-bulbocapnine, (+)-corypalmine, (-)-sinoacutine, and (+)-N-methyllaurotetanine
-
additional information
-
overview on first generation inhibitors, inhibitor design
-
additional information
-
strategies for inhibitor design
-
additional information
-
strategies for inhibitor design
-
additional information
-
murine BACE1 in amyloid precursor protein transgenic mouse models should exhibit similar pharmacological and enzymatic profiles to those of human BACE1 and should thus be useful in the development of BACE inhibitors for the treatment of Alzheimer's disease
-
additional information
-
cholesterol depletion within the cellular context inhibits both beta-secretase and gamma-secretase additively and independently from each other. The parallel and additive inhibition may indicate an intrinsic cross-talk between Alzheimer disease-related amyloid precursor protein processing, amyloid precursor protein function, and lipid biology
-
additional information
-
cyclodextrin does not affect the protein levels of BACE I
-
additional information
-
gamma-secretase affects BACE1 expression and induces an increase in protein levels in Alzheimer's disease
-
additional information
-
in presenilin 1 mutants I143T or G384A after treatment with apoptosis-inducing agents, increasing levels of p53 protein are enhanced. Treatment with a beta-secretase inhibitor counteracts the increases in the p53 protein levels
-
additional information
-
in presenilin 1 mutants I143T or G384A, acceleration of apoptosis, elevation of caspase 3/7 activity, and significant increases in caspase-4, caspase-8, and caspase-9 activities during apoptosis are observed,. Treatment with a beta-secretase inhibitor significantly attenuates the effects of the presenilin 1 mutants on caspase 3/7 activation and recovers cell viability
-
additional information
-
in wild-type as well as transgenic Tg2576 mice, no effect on BACE-1 activity can be observed by standardized Ginkgo biloba extract EGb761, a flavonol fraction or a terpenelactone fraction from Ginkgo biloba leaf
-
additional information
-
neither standardized Ginkgo biloba extract EGb761, a flavonol fraction or a terpenelactone fraction from Ginkgo biloba leaf affect BACE-1 activity in vitro or in Neuro-2a cells
-
additional information
-
not inhibited by xanthoxol
-
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Abscess
Hidradenitis Suppurativa: Proposal of Classification in Two Endotypes with Two-Step Cluster Analysis.
Acute Kidney Injury
Targeted gamma-secretase inhibition of Notch signaling activation in acute renal injury.
Acute Lung Injury
Gamma-Secretase Inhibitors Attenuate Neurotrauma and Neurogenic Acute Lung Injury in Rats by Rescuing the Accumulation of Hypertrophic Microglia.
Adenocarcinoma
Essential role of Notch signaling in apoptosis of human pancreatic tumoral cells mediated by exosomal nanoparticles.
Adenocarcinoma
Gamma-secretase complexes regulate the responses of human pancreatic ductal adenocarcinoma cells to taxanes.
Adenocarcinoma
Inhibition of gamma-secretase activity inhibits tumor progression in a mouse model of pancreatic ductal adenocarcinoma.
Adenocarcinoma
Pathogenesis of Barrett's esophagus: bile acids inhibit the Notch signaling pathway with induction of CDX2 gene expression in human esophageal cells.
Adenocarcinoma of Lung
Notch pathway activity identifies cells with cancer stem cell-like properties and correlates with worse survival in lung adenocarcinoma.
Albuminuria
The pathogenic role of notch activation in podocytes.
Alzheimer Disease
(S)-N-(5-Chlorothiophene-2-sulfonyl)-beta,beta-diethylalaninol a Notch-1-sparing gamma-secretase inhibitor.
Alzheimer Disease
1,3-Oxazines as BACE1 and/or BACE2 inhibitors: a patent evaluation (WO2012156284).
Alzheimer Disease
1,4-Oxazine ?-Secretase 1 (BACE1) Inhibitors: From Hit Generation to Orally Bioavailable Brain Penetrant Leads.
Alzheimer Disease
1-(3',4'-Dichloro-2-fluoro[1,1'-biphenyl]-4-yl)-cyclopropanecarboxylic acid (CHF5074), a novel gamma-secretase modulator, reduces brain beta-amyloid pathology in a transgenic mouse model of Alzheimer's disease without causing peripheral toxicity.
Alzheimer Disease
2,6-Disubstituted N-arylsulfonyl piperidines as gamma-secretase inhibitors.
Alzheimer Disease
3-Substituted gem-cyclohexane sulfone based gamma-secretase inhibitors for Alzheimer's disease: conformational analysis and biological activity.
Alzheimer Disease
3K3A-activated protein C blocks amyloidogenic BACE1 pathway and improves functional outcome in mice.
Alzheimer Disease
4-substituted cyclohexyl sulfones as potent, orally active gamma-secretase inhibitors.
Alzheimer Disease
6beta-acetoxy nortropane regulated processing of amyloid precursor protein in CHOm1 cells and rat brain.
Alzheimer Disease
7,8-dihydroxyflavone, a small-molecule TrkB agonist, reverses memory deficits and BACE1 elevation in a mouse model of Alzheimer's disease.
Alzheimer Disease
?-Secretase activity in rat astrocytes: translational block of BACE1 and modulation of BACE2 expression.
Alzheimer Disease
?-secretase BACE1 is required for normal cochlear function.
Alzheimer Disease
?-Secretase BACE1 Regulates Hippocampal and Reconstituted M-Currents in a ?-Subunit-Like Fashion.
Alzheimer Disease
?-Secretase1 biological markers for Alzheimer's disease: state-of-art of validation and qualification.
Alzheimer Disease
?-Secretase: its biology as a therapeutic target in diseases.
Alzheimer Disease
?-site amyloid precursor protein-cleaving enzyme 1(BACE1) inhibitor treatment induces A?5-X peptides through alternative amyloid precursor protein cleavage.
Alzheimer Disease
?-Site APP-cleaving enzyme 1 (BACE1) cleaves cerebellar Na+ channel ?4-subunit and promotes Purkinje cell firing by slowing the decay of resurgent Na+ current.
Alzheimer Disease
?-Site APP-cleaving enzyme 1 trafficking and Alzheimer's disease pathogenesis.
Alzheimer Disease
A Canine Model to Evaluate Efficacy and Safety of ?-Secretase Inhibitors and Modulators.
Alzheimer Disease
A Case of Early-Onset Alzheimer's Disease Mimicking Schizophrenia in a Patient with Presenilin 1 Mutation (S170P).
Alzheimer Disease
A Close Look at BACE1 Inhibitors for Alzheimer's Disease Treatment.
Alzheimer Disease
A continuous time-resolved fluorescence assay for identification of BACE1 inhibitors.
Alzheimer Disease
A copper-binding site in the cytoplasmic domain of BACE1 identifies a possible link to metal homoeostasis and oxidative stress in Alzheimer's disease.
Alzheimer Disease
A founder mutation in presenilin 1 causing early-onset Alzheimer disease in unrelated Caribbean Hispanic families.
Alzheimer Disease
A function for EHD family proteins in unidirectional retrograde dendritic transport of BACE1 and Alzheimer's disease A? production.
Alzheimer Disease
A further presenilin 1 mutation in the exon 8 cluster in familial Alzheimer's disease.
Alzheimer Disease
A G-Rich element forms a G-quadruplex and regulates BACE1 mRNA alternative splicing.
Alzheimer Disease
A gamma-secretase inhibitor blocks Notch signaling in vivo and causes a severe neurogenic phenotype in zebrafish.
Alzheimer Disease
A Glycosaminoglycan Extract from Portunus pelagicus Inhibits BACE1, the ? Secretase Implicated in Alzheimer's Disease.
Alzheimer Disease
A GPCR/secretase complex regulates beta- and gamma-secretase specificity for Abeta production and contributes to AD pathogenesis.
Alzheimer Disease
A helix-to-coil transition at the epsilon-cut site in the transmembrane dimer of the amyloid precursor protein is required for proteolysis.
Alzheimer Disease
A Hypothesis and Evidence That Mercury May be an Etiological Factor in Alzheimer's Disease.
Alzheimer Disease
A Method for Induced-Fit Docking, Scoring, and Ranking of Flexible Ligands. Application to Peptidic and Pseudopeptidic beta-secretase (BACE 1) Inhibitors.
Alzheimer Disease
A Miniaturized 1536-Well Format gamma-Secretase Assay *
Alzheimer Disease
A molecular dynamics study of the BACE1 conformational change from Apo to closed form induced by hydroxyethylamine derived compounds.
Alzheimer Disease
A multifactorial model of pathology for age of onset heterogeneity in familial Alzheimer's disease.
Alzheimer Disease
A mutation in Alzheimer's disease destroying a splice acceptor site in the presenilin-1 gene.
Alzheimer Disease
A myristoylated calcium-binding protein that preferentially interacts with the Alzheimer's disease presenilin 2 protein.
Alzheimer Disease
A new and simple approach for genotyping Alzheimer's disease presenilin-1 mutant knock-in mice.
Alzheimer Disease
A New Decision Tree to Solve the Puzzle of Alzheimer's Disease Pathogenesis Through Standard Diagnosis Scoring System.
Alzheimer Disease
A New Presenilin 1 (Psen1) Mutation (p.Cys263Trp) as a Cause of Both Early and Late-Onset Alzheimer's Disease in a Large Italian Family.
Alzheimer Disease
A new presenilin Alzheimer's disease case confirms the helical alignment of pathogenic mutations in transmembrane domain 5.
Alzheimer Disease
A new series of potent benzodiazepine gamma-secretase inhibitors.
Alzheimer Disease
A nine-transmembrane domain topology for presenilin 1.
Alzheimer Disease
A noncompetitive BACE1 inhibitor TAK-070 ameliorates Abeta pathology and behavioral deficits in a mouse model of Alzheimer's disease.
Alzheimer Disease
A novel Abeta isoform pattern in CSF reflects gamma-secretase inhibition in Alzheimer disease.
Alzheimer Disease
A novel Leu171Pro mutation in presenilin-1 gene in a Mexican family with early onset Alzheimer disease.
Alzheimer Disease
A novel missense mutation (G209R) in exon 8 of the presenilin 1 gene in a Japanese family with presenile familial Alzheimer's disease. Mutation in brief no. 254. Online.
Alzheimer Disease
A novel missense mutation in the presenilin-1 gene in a familial Alzheimer's disease pedigree with abundant amyloid angiopathy.
Alzheimer Disease
A novel mutation (G217D) in the Presenilin 1 gene ( PSEN1) in a Japanese family: presenile dementia and parkinsonism are associated with cotton wool plaques in the cortex and striatum.
Alzheimer Disease
A novel mutation (L250V) in the presenilin 1 gene in a Japanese familial Alzheimer's disease with myoclonus and generalized convulsion.
Alzheimer Disease
A novel mutation (Thr116Ile) in the presenilin 1 gene in a patient with early-onset Alzheimer's disease.
Alzheimer Disease
A novel mutation (V89L) in the presenilin 1 gene in a family with early onset Alzheimer's disease and marked behavioural disturbances.
Alzheimer Disease
A novel mutation in PSEN1 (p.Arg41Ser) in an Argentinian woman with early onset Parkinsonism.
Alzheimer Disease
A novel mutation in the PSEN2 gene (T430M) associated with variable expression in a family with early-onset Alzheimer disease.
Alzheimer Disease
A novel mutation of presenilin 1 in familial Alzheimer's disease in Israel detected by denaturing gradient gel electrophoresis.
Alzheimer Disease
A novel pathogenic mutation (Leu262Phe) found in the presenilin 1 gene in early-onset Alzheimer's disease.
Alzheimer Disease
A novel Polish presenilin-1 mutation (P117L) is associated with familial Alzheimer's disease and leads to death as early as the age of 28 years.
Alzheimer Disease
A novel presenilin 1 deletion (p.L166del) associated with early onset familial Alzheimer's disease.
Alzheimer Disease
A novel presenilin 1 duplication mutation (Ile168dup) causing Alzheimer's disease associated with myoclonus, seizures and pyramidal features.
Alzheimer Disease
A novel presenilin 1 L166H mutation in a pseudo-sporadic case of early-onset Alzheimer's disease.
Alzheimer Disease
A novel presenilin 1 missense mutation (L153V) segregating with early-onset autosomal dominant Alzheimer's disease.
Alzheimer Disease
A novel presenilin 1 mutation (Ala275Val) as cause of early-onset familial Alzheimer disease.
Alzheimer Disease
A novel presenilin 1 mutation (F388L) identified in a Chinese family with early-onset Alzheimer's disease.
Alzheimer Disease
A novel presenilin 1 mutation (L174 M) in a large Cuban family with early onset Alzheimer disease.
Alzheimer Disease
A novel presenilin 1 mutation (L282F) in familial Alzheimer's disease.
Alzheimer Disease
A novel presenilin 1 mutation (Leu166Arg) associated with early-onset Alzheimer disease.
Alzheimer Disease
A novel presenilin 1 mutation (Ser169del) in a Chinese family with early-onset Alzheimer's disease.
Alzheimer Disease
A novel presenilin 1 mutation (V261L) associated with presenile Alzheimer's disease and spastic paraparesis.
Alzheimer Disease
A novel presenilin 1 mutation (Y154N) in a patient with early onset Alzheimer's disease with spastic paraparesis.
Alzheimer Disease
A Novel Presenilin 1 Mutation in Early-Onset Alzheimer's Disease With Prominent Frontal Features.
Alzheimer Disease
A novel presenilin 1 mutation resulting in familial Alzheimer's disease with an onset age of 29 years.
Alzheimer Disease
A novel presenilin 1 mutation, I202F occurring at a previously predicted pathogenic site causing autosomal dominant Alzheimer's disease.
Alzheimer Disease
A novel presenilin mutation (M233V) causing very early onset Alzheimer's disease with Lewy bodies.
Alzheimer Disease
A novel presenilin-1 mutation (Leu85Pro) in early-onset Alzheimer disease with spastic paraparesis.
Alzheimer Disease
A novel presenilin-2 splice variant in human Alzheimer's disease brain tissue.
Alzheimer Disease
A novel PSEN1 gene mutation (L235R) associated with familial early-onset Alzheimer's disease.
Alzheimer Disease
A novel PSEN1 H163P mutation in a patient with early-onset Alzheimer's disease: clinical, neuroimaging, and neuropathological findings.
Alzheimer Disease
A Novel PSEN1 K311R Mutation Discovered in Chinese Families with Late-Onset Alzheimer's Disease Affects Amyloid-? Production and Tau Phosphorylation.
Alzheimer Disease
A novel PSENEN mutation in a patient with complaints of memory loss and a family history of dementia.
Alzheimer Disease
A novel role for {gamma}-secretase: selective regulation of spontaneous neurotransmitter release from hippocampal neurons.
Alzheimer Disease
A novel sorting nexin modulates endocytic trafficking and alpha-secretase cleavage of the amyloid precursor protein.
Alzheimer Disease
A novel substrate for analyzing Alzheimer's disease gamma-secretase.
Alzheimer Disease
A novel V272D presenilin mutation associated with logopenia, disorientation, and apraxia in an autosomal-dominant Alzheimer's disease family.
Alzheimer Disease
A Nuclear Function for the Presenilin 1 Neuronal Partner NPRAP/?-Catenin.
Alzheimer Disease
A pathogenic presenilin-1 deletion causes abberrant Abeta 42 production in the absence of congophilic amyloid plaques.
Alzheimer Disease
A pathogenic PSEN1 Trp165Cys mutation associated with early-onset Alzheimer's disease.
Alzheimer Disease
A pathogenic PSEN2 p.His169Asn mutation associated with early-onset Alzheimer's disease.
Alzheimer Disease
A patient with posterior cortical atrophy possesses a novel mutation in the presenilin 1 gene.
Alzheimer Disease
A pedigree with a novel presenilin 1 mutation at a residue that is not conserved in presenilin 2.
Alzheimer Disease
A physicochemical descriptor based method for effective and rapid screening of dual inhibitors against BACE-1 and GSK-3? as targets for Alzheimer's disease.
Alzheimer Disease
A PM7 dynamic residue-ligand interactions energy landscape of the BACE1 inhibitory pathway by hydroxyethylamine compounds. Part I: The flap closure process.
Alzheimer Disease
A Polish pedigree with Alzheimer's disease determined by a novel mutation in exon 12 of the presenilin 1 gene: clinical and molecular characterization.
Alzheimer Disease
A polymorphism in the presenilin 1 gene does not modify risk for Alzheimer's disease in a cohort with sporadic early onset.
Alzheimer Disease
A presenilin 1 mutation (Arg278Ser) associated with early onset Alzheimer's disease and spastic paraparesis.
Alzheimer Disease
A presenilin 1 mutation (L420R) in a family with early onset Alzheimer disease, seizures and cotton wool plaques, but not spastic paraparesis.
Alzheimer Disease
A presenilin 1 mutation in the first case of Alzheimer's disease.
Alzheimer Disease
A presenilin 1 mutation in the first case of Alzheimer's disease: revisited.
Alzheimer Disease
A presenilin-1 mutation (T245P) in transmembrane domain 6 causes early onset Alzheimer's disease.
Alzheimer Disease
A presenilin-1 mutation causes Alzheimer disease without affecting Notch signaling.
Alzheimer Disease
A presenilin-1 mutation identified in familial Alzheimer disease with cotton wool plaques causes a nearly complete loss of gamma-secretase activity.
Alzheimer Disease
A presenilin-1 mutation in a Japanese family with Alzheimer's disease and distinctive abnormalities on cranial MRI.
Alzheimer Disease
A presenilin-1 mutation renders neurons vulnerable to isoflurane toxicity.
Alzheimer Disease
A presenilin-1 Thr116Asn substitution in a family with early-onset Alzheimer's disease.
Alzheimer Disease
A presenilin-1 truncating mutation is present in two cases with autopsy-confirmed early-onset Alzheimer disease.
Alzheimer Disease
A presenilin-1-dependent gamma-secretase-like protease mediates release of Notch intracellular domain.
Alzheimer Disease
A presenilin-1/gamma-secretase cleavage releases the E-cadherin intracellular domain and regulates disassembly of adherens junctions.
Alzheimer Disease
A promising, novel, and unique BACE1 inhibitor emerges in the quest to prevent Alzheimer's disease.
Alzheimer Disease
A protective role of the low density lipoprotein receptor-related protein against amyloid beta-protein toxicity.
Alzheimer Disease
A quantitative autoradiographic study of [3H]cAMP binding to cytosolic and particulate protein kinase A in post-mortem brain staged for Alzheimer's disease neurofibrillary changes and amyloid deposits.
Alzheimer Disease
A Rare Variation in the 3' Untranslated Region of the Presenilin 2 Gene Is Linked to Alzheimer's Disease.
Alzheimer Disease
A reversible form of lysine acetylation in the ER and Golgi lumen controls the molecular stabilization of BACE1.
Alzheimer Disease
A Review of the Familial Alzheimer's Disease Locus PRESENILIN 2 and Its Relationship to PRESENILIN 1.
Alzheimer Disease
A RIP tide in neuronal signal transduction.
Alzheimer Disease
A secreted type of beta1,6 N-acetylglucosaminyltransferase V (GnT-V), a novel angiogenesis inducer, is regulated by gamma-secretase.
Alzheimer Disease
A sensitive and quantitative assay for measuring cleavage of presenilin substrates.
Alzheimer Disease
A strategy focused on MAPT, APP, NCSTN and BACE1 to build blood classifiers for Alzheimer's disease.
Alzheimer Disease
A Study On Cytogenetic And Molecular Analysis Of Presenilin 1 (Ps1) Gene In Alzheimer's Disease.
Alzheimer Disease
A surface plasmon resonance-based biosensor with full-length BACE1 in a reconstituted membrane.
Alzheimer Disease
A synthetic substrate assay for the gamma-secretase of the beta-A4 amyloid of Alzheimer's disease.
Alzheimer Disease
A system for enhancing genome-wide coexpression dynamics study.
Alzheimer Disease
A systematic review on anti-Alzheimer's disease activity of prescription Kangen-karyu.
Alzheimer Disease
A therapeutic antibody targeting BACE1 inhibits amyloid-? production in vivo.
Alzheimer Disease
A unifying model for functional difference and redundancy of presenilin-1 and -2 in cell apoptosis and differentiation.
Alzheimer Disease
A variant of Alzheimer's disease with spastic paraparesis and unusual plaques due to deletion of exon 9 of presenilin 1.
Alzheimer Disease
A? reduction in BACE1 heterozygous null 5XFAD mice is associated with transgenic APP level.
Alzheimer Disease
A?42 oligomers modulate ?-secretase through an XBP-1s-dependent pathway involving HRD1.
Alzheimer Disease
A?42/A?40 Ratios of Presenilin 1 Mutations Correlate with Clinical Onset of Alzheimer's Disease.
Alzheimer Disease
A?43-producing PS1 FAD mutants cause altered substrate interactions and respond to ?-secretase modulation.
Alzheimer Disease
A?PP/PS1 Transgenic Mice Show Sex Differences in the Cerebellum Associated with Aging.
Alzheimer Disease
Aberrant accentuation of neurofibrillary degeneration in the hippocampus of Alzheimer's disease with amyloid precursor protein 717 and presenilin-1 gene mutations.
Alzheimer Disease
Aberrant amyloid precursor protein (APP) processing in hereditary forms of Alzheimer disease caused by APP familial Alzheimer disease mutations can be rescued by mutations in the APP GxxxG motif.
Alzheimer Disease
Aberrant expressions of pathogenic phenotype in Alzheimer's diseased transgenic mice carrying NSE-controlled APPsw.
Alzheimer Disease
Aberrant induction of Par-4 is involved in apoptosis of hippocampal neurons in presenilin-1 M146V mutant knock-in mice.
Alzheimer Disease
Aberrant presenilin-1 expression downregulates LDL receptor-related protein (LRP): is LRP central to Alzheimer's disease pathogenesis?
Alzheimer Disease
Aberrant splicing in the presenilin-1 intron 4 mutation causes presenile Alzheimer's disease by increased Abeta42 secretion.
Alzheimer Disease
Abeta 17-42 in Alzheimer's disease activates JNK and caspase-8 leading to neuronal apoptosis.
Alzheimer Disease
Abeta deposition and related pathology in an APP x PS1 transgenic mouse model of Alzheimer's disease.
Alzheimer Disease
Abeta42-lowering nonsteroidal anti-inflammatory drugs preserve intramembrane cleavage of the amyloid precursor protein (APP) and ErbB-4 receptor and signaling through the APP intracellular domain.
Alzheimer Disease
Abnormal blood vessel development in mice lacking presenilin-1.
Alzheimer Disease
Abnormal cross-talk between mutant presenilin 1 (I143T, G384A) and glycosphingolipid biosynthesis.
Alzheimer Disease
Abnormal gel-electrophoretic behavior of presenilin 1 and it's fragment.
Alzheimer Disease
Accelerated acquisition of permeability barrier function in the skin of presenilin-1-deficient embryos.
Alzheimer Disease
Accelerated Alzheimer-type phenotype in transgenic mice carrying both mutant amyloid precursor protein and presenilin 1 transgenes.
Alzheimer Disease
Accelerated amyloid deposition in the brains of transgenic mice coexpressing mutant presenilin 1 and amyloid precursor proteins.
Alzheimer Disease
Accelerated long-term forgetting is a BACE1 inhibitor-reversible incipient cognitive phenotype in Alzheimer's disease model mice.
Alzheimer Disease
Accumulation of murine amyloidbeta42 in a gene-dosage-dependent manner in PS1 'knock-in' mice.
Alzheimer Disease
Accurate determination of carboxyl-terminal fragment of Presenilin 1 in various tissues from rat and cell lines.
Alzheimer Disease
Activating transcription factor 6 reduces A?1-42 and restores memory in Alzheimer's disease model mice.
Alzheimer Disease
Activation of beta2-adrenergic receptor stimulates gamma-secretase activity and accelerates amyloid plaque formation.
Alzheimer Disease
Activation of Liver X Receptor Decreases BACE1 Expression and Activity by Reducing Membrane Cholesterol Levels.
Alzheimer Disease
Activation of PKR causes amyloid ß-peptide accumulation via de-repression of BACE1 expression.
Alzheimer Disease
Activity of gamma-secretase on substrates other than APP.
Alzheimer Disease
Activity-induced convergence of APP and BACE-1 in acidic microdomains via an endocytosis-dependent pathway.
Alzheimer Disease
Acute gamma-secretase inhibition improves contextual fear conditioning in the Tg2576 mouse model of Alzheimer's disease.
Alzheimer Disease
Acylguanidine inhibitors of beta-secretase: optimization of the pyrrole ring substituents extending into the S1 and S3 substrate binding pockets.
Alzheimer Disease
Acylguanidines as small-molecule beta-secretase inhibitors.
Alzheimer Disease
ADAM10 is the physiologically relevant, constitutive alpha-secretase of the amyloid precursor protein in primary neurons.
Alzheimer Disease
ADAM19 is tightly associated with constitutive Alzheimer's disease APP alpha-secretase in A172 cells.
Alzheimer Disease
ADAM19/adamalysin 19 structure, function, and role as a putative target in tumors and inflammatory diseases.
Alzheimer Disease
ADAMs family members as amyloid precursor protein alpha-secretases.
Alzheimer Disease
Additive effects of PS1 and APP mutations on secretion of the 42-residue amyloid beta-protein.
Alzheimer Disease
Age-dependent impairment of spine morphology and synaptic plasticity in hippocampal CA1 neurons of a presenilin 1 transgenic mouse model of Alzheimer's disease.
Alzheimer Disease
Age-Dependent, Non-Cell-Autonomous Deposition of Amyloid from Synthesis of ?-Amyloid by Cells Other Than Excitatory Neurons.
Alzheimer Disease
Age-related amyloid beta deposition in transgenic mice overexpressing both Alzheimer mutant presenilin 1 and amyloid beta precursor protein Swedish mutant is not associated with global neuronal loss.
Alzheimer Disease
Age-related impairment of cerebral blood flow response to KATP channel opener in Alzheimer's disease mice with presenilin-1 mutation.
Alzheimer Disease
Age-related progressive synaptic dysfunction: the critical role of presenilin 1.
Alzheimer Disease
Age-related vascular pathology in transgenic mice expressing presenilin 1-associated familial Alzheimer's disease mutations.
Alzheimer Disease
Akt activity in presenilin 1 wild-type and mutation transfected human SH-SY5Y neuroblastoma cells after serum deprivation and high glucose stress.
Alzheimer Disease
Alcadein cleavages by APP {alpha}-and {gamma}-secretases generate small peptides p3-Alcs indicating Alzheimer disease-related {gamma}-secretase dysfunction.
Alzheimer Disease
Alleles at the Nicastrin locus modify presenilin 1- deficiency phenotype.
Alzheimer Disease
Allosteric inhibition of BACE1 by an exosite-binding antibody.
Alzheimer Disease
Allosteric Modulation of Intact ?-Secretase Structural Dynamics.
Alzheimer Disease
Alpha, beta-and gamma-secretases in Alzheimer's disease.
Alzheimer Disease
alpha- and beta-secretase: profound changes in Alzheimer's disease.
Alzheimer Disease
Alpha-secretase activation--an approach to Alzheimer's disease therapy.
Alzheimer Disease
Alpha-Secretase ADAM10 Regulation: Insights into Alzheimer's Disease Treatment.
Alzheimer Disease
Alpha-secretase as a therapeutic target.
Alzheimer Disease
alpha-secretase in Alzheimer's disease: molecular identity, regulation and therapeutic potential.
Alzheimer Disease
alpha-secretase mediated conversion of the Amyloid Precursor Protein derived membrane stub C99 to C83 limits Abeta generation.
Alzheimer Disease
Alpha-secretase-derived product of beta-amyloid precursor protein is decreased by presenilin 1 mutations linked to familial Alzheimer's disease.
Alzheimer Disease
Alteration in brain presenilin 1 mRNA expression in early onset familial Alzheimer's disease.
Alzheimer Disease
Alteration in brain presenilin-1 mRNA expression in sporadic Alzheimer's disease.
Alzheimer Disease
Alteration of BACE1-dependent NRG1/ErbB4 signaling and schizophrenia-like phenotypes in BACE1-null mice.
Alzheimer Disease
Alterations in behavior, amyloid beta-42, caspase-3, and Cox-2 in mutant PS2 transgenic mouse model of Alzheimer's disease.
Alzheimer Disease
Alterations in excitotoxicity and prostaglandin metabolism in a transgenic mouse model of Alzheimer's disease.
Alzheimer Disease
Alterations in presenilin 1 processing by amyloid-beta peptide in the rat retina.
Alzheimer Disease
Alterations in Striatal microRNA-mRNA Networks Contribute to Neuroinflammation in Multiple System Atrophy.
Alzheimer Disease
Altered amyloid-beta metabolism and deposition in genomic-based beta-secretase transgenic mice.
Alzheimer Disease
Altered beta-secretase enzyme kinetics and levels of both BACE1 and BACE2 in the Alzheimer's disease brain.
Alzheimer Disease
Altered binding of mutated presenilin with cytoskeleton-interacting proteins.
Alzheimer Disease
Altered calcium homeostasis and mitochondrial dysfunction in cortical synaptic compartments of presenilin-1 mutant mice.
Alzheimer Disease
Altered Cholesterol Intracellular Trafficking and the Development of Pathological Hallmarks of Sporadic AD.
Alzheimer Disease
Altered expression of apolipoprotein E, amyloid precursor protein and presenilin-1 is associated with chronic reactive gliosis in rat cortical tissue.
Alzheimer Disease
Altered morphological and electrophysiological properties of Cajal-Retzius cells in cerebral cortex of embryonic Presenilin-1 knockout mice.
Alzheimer Disease
Alternative cleavage of Alzheimer-associated presenilins during apoptosis by a caspase-3 family protease.
Alzheimer Disease
Alternative processing of ?-secretase substrates in common forms of mild cognitive impairment and Alzheimer's disease: evidence for ?-secretase dysfunction.
Alzheimer Disease
Alternative splicing in a presenilin 2 variant associated with Alzheimer disease.
Alzheimer Disease
Alternative splicing in the N-terminus of Alzheimer's presenilin 1.
Alzheimer Disease
Alzheimer disease Abeta production in the absence of S-palmitoylation-dependent targeting of BACE1 to lipid rafts.
Alzheimer Disease
Alzheimer disease gamma-secretase: a complex story of GxGD-type presenilin proteases.
Alzheimer Disease
Alzheimer disease: BACE1 branches out.
Alzheimer Disease
Alzheimer disease: BACE1 inhibition could block CSF tau increase.
Alzheimer Disease
Alzheimer disease: BACE1 inhibitor reduces ?-amyloid production in humans.
Alzheimer Disease
Alzheimer disease: BACE1 inhibitors block new A? plaque formation.
Alzheimer Disease
Alzheimer disease: update on basic mechanisms.
Alzheimer Disease
Alzheimer presenilins in the nuclear membrane, interphase kinetochores, and centrosomes suggest a role in chromosome segregation.
Alzheimer Disease
Alzheimer's beta-secretase, beta-site amyloid precursor protein-cleaving enzyme, is responsible for cleavage secretion of a Golgi-resident sialyltransferase.
Alzheimer Disease
Alzheimer's Disease and Hippocampal Adult Neurogenesis; Exploring Shared Mechanisms.
Alzheimer Disease
Alzheimer's disease and Notch signaling.
Alzheimer Disease
Alzheimer's Disease Associated Presenilin 1 and 2 Genes Dysregulation in Neonatal Lymphocytes Following Perinatal Asphyxia.
Alzheimer Disease
Alzheimer's disease associated presenilin 1 interacts with HC5 and ZETA, subunits of the catalytic 20S proteasome.
Alzheimer Disease
Alzheimer's disease associated presenilin-1 holoprotein and its 18-20 kDa C-terminal fragment are death substrates for proteases of the caspase family.
Alzheimer Disease
Alzheimer's disease beta-secretase BACE1 is not a neuron-specific enzyme.
Alzheimer Disease
Alzheimer's disease BIN1 coding variants increase intracellular A? levels by interfering with BACE1 recycling.
Alzheimer Disease
Alzheimer's disease due to an intronic presenilin-1 (PSEN1 intron 4) mutation: A clinicopathological study.
Alzheimer Disease
Alzheimer's disease phenotypes and genotypes associated with mutations in presenilin 2.
Alzheimer Disease
Alzheimer's disease presenilin-1 exon 9 deletion and L250S mutations sensitize SH-SY5Y neuroblastoma cells to hyperosmotic stress-induced apoptosis.
Alzheimer Disease
Alzheimer's disease presenilin-1 expression modulates the assembly of neurofilaments.
Alzheimer Disease
Alzheimer's Disease Presenilin-1 Mutation Sensitizes Neurons to Impaired Autophagy Flux and Propofol Neurotoxicity: Role of Calcium Dysregulation.
Alzheimer Disease
Alzheimer's disease with spastic paresis and cotton wool type plaques.
Alzheimer Disease
Alzheimer's Disease, Drosophila melanogaster and Polyphenols.
Alzheimer Disease
Alzheimer's disease-associated presenilins 1 and 2: accelerated amyloid fibril formation of mutant 410 Cys-->Tyr and 141 Asn-->Ile peptides.
Alzheimer Disease
Alzheimer's disease-causing proline substitutions lead to presenilin 1 aggregation and malfunction.
Alzheimer Disease
Alzheimer's disease-like alterations in peripheral cells from presenilin-1 transgenic mice.
Alzheimer Disease
Alzheimer's disease-linked mutations in presenilin-1 result in a drastic loss of activity in purified ?-secretase complexes.
Alzheimer Disease
Alzheimer's disease-related gene expression in the brain of senescence accelerated mouse.
Alzheimer Disease
Alzheimer's disease. Closing in on gamma-secretase.
Alzheimer Disease
Alzheimer's disease. In search of gamma-secretase.
Alzheimer Disease
Alzheimer's disease. Molecular consequences of presenilin-1 mutation.
Alzheimer Disease
Alzheimer's Disease: APP, Gamma Secretase, APOE, CLU, CR1, PICALM, ABCA7, BIN1, CD2AP, CD33, EPHA1, and MS4A2, and Their Relationships with Herpes Simplex, C. Pneumoniae, Other Suspect Pathogens, and the Immune System.
Alzheimer Disease
Alzheimer's disease: from pathology to therapeutic approaches.
Alzheimer Disease
Alzheimer's disease: genetic studies and transgenic models.
Alzheimer Disease
Alzheimer's disease: Selectively tuning gamma-secretase.
Alzheimer Disease
Alzheimer's presenilin 1 causes chromosome missegregation and aneuploidy.
Alzheimer Disease
Alzheimer's presenilin 1 is a putative membrane receptor for rab GDP dissociation inhibitor.
Alzheimer Disease
Alzheimer's presenilin 1 modulates sorting of APP and its carboxyl-terminal fragments in cerebral neurons in vivo.
Alzheimer Disease
Alzheimer's presenilin mutation sensitizes neural cells to apoptosis induced by trophic factor withdrawal and amyloid beta-peptide: involvement of calcium and oxyradicals.
Alzheimer Disease
Alzheimer's PS-1 mutation perturbs calcium homeostasis and sensitizes PC12 cells to death induced by amyloid beta-peptide.
Alzheimer Disease
Alzheimer's secretases regulate voltage-gated sodium channels.
Alzheimer Disease
Alzheimer-associated C allele of the promoter polymorphism -22C>T causes a critical neuron-specific decrease of presenilin 1 expression.
Alzheimer Disease
Alzheimer-associated presenilin-2 confers increased sensitivity to apoptosis in PC12 cells.
Alzheimer Disease
Ameliorative effects of a non-competitive BACE1 inhibitor TAK-070 on A? peptide levels and impaired learning behavior in aged rats.
Alzheimer Disease
American Chemical Society - 240th national meeting - chemistry for preventing and combating disease: part 1.
Alzheimer Disease
Amino-terminally truncated Abeta peptide species are the main component of cotton wool plaques.
Alzheimer Disease
Aminomethyl-Derived Beta Secretase (BACE1) Inhibitors: Engaging Gly230 without an Anilide Functionality.
Alzheimer Disease
Amyloid ? aggregation inhibitory activity of triterpene saponins from the cactus Stenocereus pruinosus.
Alzheimer Disease
Amyloid ? production along the neuronal secretory pathway: Dangerous liaisons in the Golgi?
Alzheimer Disease
Amyloid ?-protein oligomers upregulate the ?-secretase, BACE1, through a post-translational mechanism involving its altered subcellular distribution in neurons.
Alzheimer Disease
Amyloid angiopathy and variability in amyloid beta deposition is determined by mutation position in presenilin-1-linked Alzheimer's disease.
Alzheimer Disease
Amyloid angiopathy in a Volga German family with Alzheimer's disease and a presenilin-2 mutation (N141I).
Alzheimer Disease
Amyloid at the cutting edge: activation of alpha-secretase prevents amyloidogenesis in an Alzheimer disease mouse model.
Alzheimer Disease
Amyloid beta secretase gene (BACE) is neither mutated in nor associated with early-onset Alzheimer's disease.
Alzheimer Disease
Amyloid beta-protein precursor juxtamembrane domain regulates specificity of gamma-secretase-dependent cleavages.
Alzheimer Disease
Amyloid precursor protein associates with a nicastrin-dependent docking site on the presenilin 1-gamma-secretase complex in cells demonstrated by fluorescence lifetime imaging.
Alzheimer Disease
Amyloid precursor protein gene analysis in familial Alzheimer's disease cases: a lack of mutations in exons 16 and 17.
Alzheimer Disease
Amyloid precursor protein heat shock response in lymphoblastoid cell lines bearing presenilin-1 mutations.
Alzheimer Disease
Amyloid precursor protein processing in human neurons with an allelic series of the PSEN1 intron 4 deletion mutation and total presenilin-1 knockout.
Alzheimer Disease
Amyloid precursor protein selective gamma-secretase inhibitors for treatment of Alzheimer's disease.
Alzheimer Disease
Amyloid precursor protein, presenilins, and alpha-synuclein: molecular pathogenesis and pharmacological applications in Alzheimer's disease.
Alzheimer Disease
Amyloid protein-mediated differential DNA methylation status regulates gene expression in Alzheimer's disease model cell line.
Alzheimer Disease
Amyloid-? precursor protein processing and oxidative stress are altered in human iPSC-derived neuron and astrocyte co-cultures carrying presenillin-1 gene mutations following spontaneous differentiation.
Alzheimer Disease
Amyloid-beta reduction by memapsin 2 (beta-secretase) immunization.
Alzheimer Disease
Amyloid-beta, BACE, and oxidative stress in Alzheimer's disease, a commentary on "The different aggregation state of beta-amyloid 1-42 mediates different effects on oxidative stress, neurodegeneration and BACE-1 expression".
Alzheimer Disease
Amyloid-dependent triosephosphate isomerase nitrotyrosination induces glycation and tau fibrillation.
Alzheimer Disease
Amyloidogenic processing of human amyloid precursor protein in hippocampal neurons devoid of cathepsin D.
Alzheimer Disease
An aberrant sugar modification of BACE1 blocks its lysosomal targeting in Alzheimer's disease.
Alzheimer Disease
An alternative spliced mouse presenilin-2 mRNA encodes a novel gamma-secretase inhibitor.
Alzheimer Disease
An Alzheimer's disease-linked PS1 variant rescues the developmental abnormalities of PS1-deficient embryos.
Alzheimer Disease
An APP inhibitory domain containing the Flemish mutation residue modulates gamma-secretase activity for Abeta production.
Alzheimer Disease
An atomic structure of human ?-secretase.
Alzheimer Disease
An empirical model of gamma-secretase activity.
Alzheimer Disease
An exo-cell assay for examining real-time gamma-secretase activity and inhibition.
Alzheimer Disease
An intronic polymorphism in the presenilin-1 gene does not influence the amount or molecular form of the amyloid beta protein deposited in Alzheimer's disease.
Alzheimer Disease
An NSAID-like compound, FT-9, preferentially inhibits gamma-secretase cleavage of APP compared to its effect on APLP1.
Alzheimer Disease
An Orally Available BACE1 Inhibitor That Affords Robust CNS A? Reduction without Cardiovascular Liabilities.
Alzheimer Disease
Anagliptin protects neuronal cells against endogenous amyloid ? (A?)-induced cytotoxicity and apoptosis.
Alzheimer Disease
Analysis of alteration of p75NTR processing and signalling by PS2 mutation and gamma-secretase inhibition.
Alzheimer Disease
Analysis of presenilin 1 and presenilin 2 expression and processing by newly developed monoclonal antibodies.
Alzheimer Disease
Analysis of the 5' sequence, genomic structure, and alternative splicing of the presenilin-1 gene (PSEN1) associated with early onset Alzheimer disease.
Alzheimer Disease
Angela R.: a familial Alzheimer's disease case in the days of Auguste D.
Alzheimer Disease
Antisense inhibition at the beta-secretase-site of beta-amyloid precursor protein reduces cerebral amyloid and acetyl cholinesterase activity in Tg2576.
Alzheimer Disease
Antisense-induced reduction of presenilin 1 expression selectively increases the production of amyloid beta42 in transfected cells.
Alzheimer Disease
AP-2 reduces amyloidogenesis by promoting BACE1 trafficking and degradation in neurons.
Alzheimer Disease
Apolipoprotein E and amyloidogenesis.
Alzheimer Disease
Apolipoprotein E and intronic polymorphism of presenilin 1 and alpha-1-antichymotrypsin in Alzheimer's disease and vascular dementia.
Alzheimer Disease
Apolipoprotein E and presenilin-1 allelic variation and Alzheimer's disease in India.
Alzheimer Disease
Apolipoprotein E and presenilin-1 genotypes in Huntington's disease.
Alzheimer Disease
Apolipoprotein Eepsilon4 modifies Alzheimer's disease onset in an E280A PS1 kindred.
Alzheimer Disease
Apoptogenic interactions of plasmalemmal type-1 VDAC and A? peptides via GxxxG motifs induce Alzheimer's disease - a basic model of apoptosis?
Alzheimer Disease
Apoptotic proteolytic cleavage of the presenilins by caspases.
Alzheimer Disease
APP and BACE1 miRNA genetic variability has no major role in risk for Alzheimer disease.
Alzheimer Disease
APP processing and amyloid deposition in mice haplo-insufficient for presenilin 1.
Alzheimer Disease
APP substitutions V715F and L720P alter PS1 conformation and differentially affect Abeta and AICD generation.
Alzheimer Disease
APP transgenic mice and their application to drug discovery.
Alzheimer Disease
APP, PSEN1, and PSEN2 mutations in early-onset Alzheimer disease: A genetic screening study of familial and sporadic cases.
Alzheimer Disease
Application of a Bioinformatics-Based Approach to Identify Novel Putative in vivo BACE1 Substrates.
Alzheimer Disease
Application of BACE1 immobilized enzyme reactor for the characterization of multifunctional alkaloids from Corydalis cava (Fumariaceae) as Alzheimer's disease targets.
Alzheimer Disease
Application of molecular framework-based data-mining method in the search for beta-secretase 1 inhibitors through drug repurposing.
Alzheimer Disease
Application of quantitative LC-MS surrogate peptide methodology in the analysis of the amyloid beta peptide (Abeta) biosynthetic intermediate protein APP-betaCTF.
Alzheimer Disease
Approaches for detecting lysosomal alkalinization and impaired degradation in fresh and cultured RPE cells: evidence for a role in retinal degenerations.
Alzheimer Disease
Aryl sulfones: a new class of gamma-secretase inhibitors.
Alzheimer Disease
Aspartate mutations in presenilin and gamma-secretase inhibitors both impair notch1 proteolysis and nuclear translocation with relative preservation of notch1 signaling.
Alzheimer Disease
Aspartic proteases involved in Alzheimer's disease.
Alzheimer Disease
Aspartyl protease inhibitor pepstatin binds to the presenilins of Alzheimer's disease.
Alzheimer Disease
Assembly, maturation, and trafficking of the gamma-secretase complex in Alzheimer's disease.
Alzheimer Disease
Assembly, trafficking and function of gamma-secretase.
Alzheimer Disease
Association between a PS-1 intronic polymorphism and late onset Alzheimer's disease.
Alzheimer Disease
Association between presenilin 1 intronic polymorphism and late onset Alzheimer's disease in the North Chinese population.
Alzheimer Disease
Association between presenilin-1 Glu318Gly mutation and familial Alzheimer's disease in the Australian population.
Alzheimer Disease
Association between the presenilin-1 mutation Glu318Gly and complaints of memory impairment.
Alzheimer Disease
Association of a presenilin 1 S170F mutation with a novel Alzheimer disease molecular phenotype.
Alzheimer Disease
Association of apolipoprotein E genotype and intronic polymorphism of the presenilin-1 gene with Alzheimer's disease in elderly Taiwan Chinese.
Alzheimer Disease
Association of BACE1 gene polymorphism with Alzheimer's disease in Asian populations: meta-analysis including Korean samples.
Alzheimer Disease
Association of presenilin-1 polymorphism with cerebral amyloid angiopathy in the elderly.
Alzheimer Disease
Association of PS1 1/2, ACE I/D, and LRP C/T polymorphisms with Alzheimer's disease in the Chinese population: a meta-analysis of case-control studies.
Alzheimer Disease
Association of variants within APOE, SORL1, RUNX1, BACE1 and ALDH18A1 with dementia in Alzheimer's disease in subjects with Down syndrome.
Alzheimer Disease
Association study and meta-analysis of Alzheimer's disease risk and presenilin-1 intronic polymorphism.
Alzheimer Disease
Association study between Alzheimer's disease and genes involved in Abeta biosynthesis, aggregation and degradation: suggestive results with BACE1.
Alzheimer Disease
Associations Between Biomarkers and Age in the Presenilin 1 E280A Autosomal Dominant Alzheimer Disease Kindred: A Cross-sectional Study.
Alzheimer Disease
Astragaloside IV, a Natural PPAR? Agonist, Reduces A? Production in Alzheimer's Disease Through Inhibition of BACE1.
Alzheimer Disease
Asymptomatic Carriers of Presenilin-1 E318G Variant Show no Cerebrospinal Fluid Biochemical Signs Suggestive of Alzheimer's disease in a Family with Late-onset Dementia.
Alzheimer Disease
At the frontline of Alzheimer's disease treatment: gamma-secretase inhibitor/modulator mechanism.
Alzheimer Disease
ATF4 regulates gamma-secretase activity during amino acid imbalance.
Alzheimer Disease
Attenuated presenilin-1 endoproteolysis enhances store-operated calcium currents in neuronal cells.
Alzheimer Disease
Attitudes and knowledge about genetic testing before and after finding the disease-causing mutation among individuals at high risk for familial, early-onset Alzheimer's disease.
Alzheimer Disease
Atypical early-onset Alzheimer's disease caused by the Iranian APP mutation.
Alzheimer Disease
Atypical presentation of a novel Presenilin 1 R377W mutation: sporadic, late-onset Alzheimer disease with epilepsy and frontotemporal atrophy.
Alzheimer Disease
Autophagy impairment stimulates PS1 expression and gamma-secretase activity.
Alzheimer Disease
Autophagy Induction by Bexarotene Promotes Mitophagy in Presenilin 1 Familial Alzheimer's Disease iPSC-Derived Neural Stem Cells.
Alzheimer Disease
Autophagy-mediated Regulation of BACE1 Protein Trafficking and Degradation.
Alzheimer Disease
Autopsy-confirmed familial early-onset Alzheimer disease caused by the l153V presenilin 1 mutation.
Alzheimer Disease
Avoidance of Apoptosis in Alzheimer's Disease.
Alzheimer Disease
Axonal and Schwann Cell BACE1 Is Equally Required for Remyelination of Peripheral Nerves.
Alzheimer Disease
Axonal BACE1 dynamics and targeting in hippocampal neurons: a role for Rab11 GTPase.
Alzheimer Disease
AZD3293: Pharmacokinetic and Pharmacodynamic Effects in Healthy Subjects and Patients with Alzheimer's Disease.
Alzheimer Disease
BACE inhibitor treatment of mice induces hyperactivity in a Seizure-related gene 6 family dependent manner without altering learning and memory.
Alzheimer Disease
BACE-1 and ?-Secretase as Therapeutic Targets for Alzheimer's Disease.
Alzheimer Disease
BACE-1 hydroxyethylamine inhibitors using novel edge-to-face interaction with Arg-296.
Alzheimer Disease
BACE-1 inhibitors part 1: identification of novel hydroxy ethylamines (HEAs).
Alzheimer Disease
BACE-1 Inhibitors: From Recent Single-Target Molecules to Multitarget Compounds for Alzheimer's Disease.
Alzheimer Disease
BACE-1 is expressed in the blood-brain barrier endothelium and is upregulated in a murine model of Alzheimer's disease.
Alzheimer Disease
BACE1 (?-secretase) inhibitors for the treatment of Alzheimer's disease.
Alzheimer Disease
BACE1 (beta-secretase) transgenic and knockout mice: identification of neurochemical deficits and behavioral changes.
Alzheimer Disease
BACE1 across species: a comparison of the in vivo consequences of BACE1 deletion in mice and rats.
Alzheimer Disease
BACE1 activity in cerebrospinal fluid and its relation to markers of AD pathology.
Alzheimer Disease
BACE1 activity is modulated by cell-associated sphingosine-1-phosphate.
Alzheimer Disease
BACE1 activity regulates cell surface contactin-2 levels.
Alzheimer Disease
BACE1 and BACE2 enzymatic activities in Alzheimer's disease.
Alzheimer Disease
BACE1 and Other Alzheimer's-Related Biomarkers in Cerebrospinal Fluid and Plasma Distinguish Alzheimer's Disease Patients from Cognitively-Impaired Neurosyphilis Patients.
Alzheimer Disease
BACE1 and presenilin/?-secretase regulate proteolytic processing of KCNE1 and 2, auxiliary subunits of voltage-gated potassium channels.
Alzheimer Disease
BACE1 and presenilin: two unusual aspartyl proteases involved in Alzheimer's disease.
Alzheimer Disease
BACE1 as a Potential Biomarker for Alzheimer's Disease.
Alzheimer Disease
BACE1 as a Therapeutic Target in Alzheimer's Disease: Rationale and Current Status.
Alzheimer Disease
BACE1 controls synaptic function through modulating release of synaptic vesicles.
Alzheimer Disease
BACE1 Deficiency Causes Abnormal Neuronal Clustering in the Dentate Gyrus.
Alzheimer Disease
BACE1 deficiency rescues memory deficits and cholinergic dysfunction in a mouse model of Alzheimer's disease.
Alzheimer Disease
BACE1 deletion in the adult mouse reverses preformed amyloid deposition and improves cognitive functions.
Alzheimer Disease
BACE1 Dynamics Upon Inhibition with a BACE Inhibitor and Correlation to Downstream Alzheimer's Disease Markers in Elderly Healthy Participants.
Alzheimer Disease
BACE1 Elevation is Involved in Amyloid Plaque Development in the Triple Transgenic Model of Alzheimer's Disease: Differential A? Antibody Labeling of Early-Onset Axon Terminal Pathology.
Alzheimer Disease
BACE1 expression and activity: relevance in Alzheimer's disease.
Alzheimer Disease
BACE1 Function and Inhibition: Implications of Intervention in the Amyloid Pathway of Alzheimer's Disease Pathology.
Alzheimer Disease
BACE1 gene deletion: impact on behavioral function in a model of Alzheimer's disease.
Alzheimer Disease
BACE1 gene promoter single-nucleotide polymorphisms in Alzheimer's disease.
Alzheimer Disease
BACE1 gene variants do not influence BACE1 activity, levels of APP or A? isoforms in CSF in Alzheimer's disease.
Alzheimer Disease
BACE1 in Alzheimer's disease.
Alzheimer Disease
BACE1 in the retina: a sensitive biomarker for monitoring early pathological changes in Alzheimer's disease.
Alzheimer Disease
BACE1 inhibition as a therapeutic strategy for Alzheimer's disease.
Alzheimer Disease
BACE1 inhibition induces a specific cerebrospinal fluid ?-amyloid pattern that identifies drug effects in the central nervous system.
Alzheimer Disease
BACE1 inhibition more effectively suppresses initiation than progression of ?-amyloid pathology.
Alzheimer Disease
BACE1 Inhibition Using 2'-OMePS Steric Blocking Antisense Oligonucleotides.
Alzheimer Disease
BACE1 inhibitor drugs in clinical trials for Alzheimer's disease.
Alzheimer Disease
BACE1 inhibitors: Current status and future directions in treating Alzheimer's disease.
Alzheimer Disease
BACE1 is at the crossroad of a toxic vicious cycle involving cellular stress and ?-amyloid production in Alzheimer's disease.
Alzheimer Disease
BACE1 knock-outs display deficits in activity-dependent potentiation of synaptic transmission at mossy fiber to CA3 synapses in the hippocampus.
Alzheimer Disease
BACE1 levels are increased in plasma of Alzheimer's disease patients compared with matched cognitively healthy controls.
Alzheimer Disease
BACE1 levels by APOE genotype in non-demented and Alzheimer's post-mortem brains.
Alzheimer Disease
BACE1 Levels Correlate with Phospho-Tau Levels in Human Cerebrospinal Fluid.
Alzheimer Disease
BACE1 modulates filopodia-like protrusions induced by sodium channel beta4 subunit.
Alzheimer Disease
BACE1 modulates gating of KCNQ1 (Kv7.1) and cardiac delayed rectifier KCNQ1/KCNE1 (IKs).
Alzheimer Disease
BACE1 molecular docking and anti-Alzheimer's disease activities of ginsenosides.
Alzheimer Disease
BACE1 mRNA Expression in Alzheimer's Disease Postmortem Brain Tissue.
Alzheimer Disease
BACE1 partial deletion induces synaptic plasticity deficit in adult mice.
Alzheimer Disease
BACE1 Physiological Functions May Limit Its Use as Therapeutic Target for Alzheimer's Disease.
Alzheimer Disease
BACE1 polymorphisms do not influence platelet membrane beta-secretase activity or genetic susceptibility for Alzheimer's disease in the Northern Irish population.
Alzheimer Disease
BACE1 regulates hippocampal astrogenesis via the Jagged1-Notch pathway.
Alzheimer Disease
BACE1 regulates voltage-gated sodium channels and neuronal activity.
Alzheimer Disease
BACE1 RNA interference improves spatial memory and attenuates A? burden in a streptozotocin-induced tau hyperphosphorylated rat model.
Alzheimer Disease
BACE1 RNAi Restores the Composition of Phosphatidylethanolamine-Derivates Related to Memory Improvement in Aged 3xTg-AD Mice.
Alzheimer Disease
BACE1 role in Alzheimer's disease and other dementias: from the theory to the practice.
Alzheimer Disease
BACE1 structure and function in health and Alzheimer's disease.
Alzheimer Disease
BACE1 SUMOylation increases its stability and escalates the protease activity in Alzheimer's disease.
Alzheimer Disease
BACE1 Translation: At the Crossroads Between Alzheimer's Disease Neurodegeneration and Memory Consolidation.
Alzheimer Disease
BACE1-/- mice exhibit seizure activity that does not correlate with sodium channel level or axonal localization.
Alzheimer Disease
BACE1: from biomarker to Alzheimer's disease therapeutical target.
Alzheimer Disease
BACE1: the beta-secretase enzyme in Alzheimer's disease.
Alzheimer Disease
BACE2 as a new diabetes target: a patent review 2010 - 2012.
Alzheimer Disease
BACE2 degradation is mediated by both the proteasome and lysosome pathways.
Alzheimer Disease
BACE2 distribution in major brain cell types and identification of novel substrates.
Alzheimer Disease
BACE2 is stored in secretory granules of mouse and rat pancreatic beta cells.
Alzheimer Disease
Baculoviruses expressing the human familial Alzheimer's disease presenilin 1 mutation lacking exon 9 increase levels of an amyloid beta-like protein in Sf9 cells.
Alzheimer Disease
BAG-1M co-activates BACE1 transcription through NF-?B and accelerates A? production and memory deficit in Alzheimer's disease mouse model.
Alzheimer Disease
Behavioral and neural network abnormalities in human APP transgenic mice resemble those of App knock-in mice and are modulated by familial Alzheimer's disease mutations but not by inhibition of BACE1.
Alzheimer Disease
Behavioral and neurochemical characterization of transgenic mice carrying the human presenilin-1 gene with or without the leucine-to-proline mutation at codon 235.
Alzheimer Disease
Beneficial effects of the ?-secretase inhibitor GRL-8234 in 5XFAD Alzheimer's transgenic mice lessen during disease progression.
Alzheimer Disease
Benzolactam (BL) enhances sAPP secretion in fibroblasts and in PC12 cells.
Alzheimer Disease
Bepridil and amiodarone simultaneously target the Alzheimer's disease beta- and gamma-secretase via distinct mechanisms.
Alzheimer Disease
beta Subunits of voltage-gated sodium channels are novel substrates of beta-site amyloid precursor protein-cleaving enzyme (BACE1) and gamma-secretase.
Alzheimer Disease
Beta-amyloid mediated nitration of manganese superoxide dismutase: implication for oxidative stress in a APPNLH/NLH X PS-1P264L/P264L double knock-in mouse model of Alzheimer's disease.
Alzheimer Disease
Beta-catenin expression in human neural cell lines following exposure to cytokines and growth factors.
Alzheimer Disease
Beta-galactoside alpha2,6-sialyltransferase I cleavage by BACE1 enhances the sialylation of soluble glycoproteins. A novel regulatory mechanism for alpha2,6-sialylation.
Alzheimer Disease
Beta-Secretase 1 Underlies Reactive Astrocytes and Endothelial Disruption in Neurodegeneration.
Alzheimer Disease
Beta-secretase as a target for Alzheimer's disease drug discovery: an overview of in vitro methods for characterization of inhibitors.
Alzheimer Disease
beta-Secretase inhibitor potency is decreased by aberrant beta-cleavage location of the "Swedish mutant" amyloid precursor protein.
Alzheimer Disease
Beta-secretase processing in the trans-Golgi network preferentially generates truncated amyloid species that accumulate in Alzheimer's disease brain.
Alzheimer Disease
Beta-secretase processing of the Alzheimer's amyloid protein precursor (APP).
Alzheimer Disease
Beta-secretase-1 elevation in transgenic mouse models of Alzheimer's disease is associated with synaptic/axonal pathology and amyloidogenesis: implications for neuritic plaque development.
Alzheimer Disease
Beta-secretase: structure, function, and evolution.
Alzheimer Disease
Beta-site amyloid precursor protein cleaving enzyme 1 (BACE1) as a biological candidate marker of Alzheimer's disease.
Alzheimer Disease
Beta-Site Amyloid Precursor Protein Cleaving Enzyme 1 Inhibition Impairs Synaptic Plasticity via Seizure Protein 6.
Alzheimer Disease
Beta-site amyloid precursor protein cleaving enzyme 1 levels become elevated in neurons around amyloid plaques: implications for Alzheimer's disease pathogenesis.
Alzheimer Disease
Beta-site amyloid precursor protein-cleaving enzyme-1 (BACE1)-mediated changes of endogenous amyloid beta in wild-type and transgenic mice in vivo.
Alzheimer Disease
Beta-site APP cleaving enzyme 1 (BACE1) is increased in remaining neurons in Alzheimer's disease brains.
Alzheimer Disease
Beta-site APP cleaving enzyme up-regulation induced by 4-hydroxynonenal is mediated by stress-activated protein kinases pathways.
Alzheimer Disease
Bidirectional regulation of A? levels by Presenilin 1.
Alzheimer Disease
Binding of F-spondin to amyloid-beta precursor protein: a candidate amyloid-beta precursor protein ligand that modulates amyloid-beta precursor protein cleavage.
Alzheimer Disease
Binding of the positron emission tomography tracer Pittsburgh compound-B reflects the amount of amyloid-beta in Alzheimer's disease brain but not in transgenic mouse brain.
Alzheimer Disease
Binding partners of Alzheimer's disease proteins: are they physiologically relevant?
Alzheimer Disease
Bioactive polycyclic polyprenylated acylphloroglucinols from Hypericum perforatum.
Alzheimer Disease
Biochemical and immunocytochemical characterization of calsenilin in mouse brain.
Alzheimer Disease
Biochemical and structural characterization of the interaction of memapsin 2 (beta-secretase) cytosolic domain with the VHS domain of GGA proteins.
Alzheimer Disease
Biochemical characterization of the gamma-secretase activity that produces beta-amyloid peptides.
Alzheimer Disease
Biochemical properties of endogenous presenilin 1 and presenilin 2 in cultured human B-lymphocytes.
Alzheimer Disease
Biogenesis of gamma-secretase early in the secretory pathway.
Alzheimer Disease
Biological actions and mechanism of action of calbindin in the process of apoptosis.
Alzheimer Disease
Biological Evaluation of Newly Synthesized Biaryl Guanidine Derivatives to Arrest ?-Secretase Enzymatic Activity Involved in Alzheimer's Disease.
Alzheimer Disease
Biomarkers of Alzheimer disease, insulin resistance, and obesity in childhood.
Alzheimer Disease
Blood-brain barrier-penetrating siRNA nanomedicine for Alzheimer's disease therapy.
Alzheimer Disease
Bone Marrow-Derived Macrophages from A?PP/PS1 Mice are Sensitized to the Effects of Inflammatory Stimuli.
Alzheimer Disease
Boom in the development of non-peptidic beta-secretase (BACE1) inhibitors for the treatment of Alzheimer's disease.
Alzheimer Disease
Both N-terminal and C-terminal fragments of presenilin 1 colocalize with neurofibrillary tangles in neurons and dystrophic neurites of senile plaques in Alzheimer's disease.
Alzheimer Disease
Brain 18F-Florbetapir PET/CT Findings in an Early-onset Alzheimer Disease Patient Carrying Presenilin-1 G378E Mutation.
Alzheimer Disease
Brain A? load association and sexual dimorphism of plasma BACE1 concentrations in cognitively normal individuals at risk for AD.
Alzheimer Disease
Brain expression of presenilins in sporadic and early-onset, familial Alzheimer's disease.
Alzheimer Disease
Brain imaging and fluid biomarker analysis in young adults at genetic risk for autosomal dominant Alzheimer's disease in the presenilin 1 E280A kindred: a case-control study.
Alzheimer Disease
Brain Pyroglutamate Amyloid-Beta is Produced by Cathepsin B and is Reduced by the Cysteine Protease Inhibitor E64d, Representing a Potential Alzheimer's Disease Therapeutic.
Alzheimer Disease
Brain-Targeted Delivery of Pre-miR-29b Using Lactoferrin-Stearic Acid-Modified-Chitosan/Polyethyleneimine Polyplexes.
Alzheimer Disease
Brain-wide Cas9-mediated cleavage of a gene causing familial Alzheimer's disease alleviates amyloid-related pathologies in mice.
Alzheimer Disease
Branched Diacylglycerol-Lactones as Potent Protein Kinase C Ligands and alpha-Secretase Activators.
Alzheimer Disease
C-terminal 37 residues of LRP promote the amyloidogenic processing of APP independent of FE65.
Alzheimer Disease
C-terminal maturation fragments of presenilin 1 and 2 control secretion of APP alpha and A beta by human cells and are degraded by proteasome.
Alzheimer Disease
Ca(2+) dysregulation in neurons from transgenic mice expressing mutant presenilin 2.
Alzheimer Disease
Ca(2+) stores and capacitative Ca(2+) entry in human neuroblastoma (SH-SY5Y) cells expressing a familial Alzheimer's disease presenilin-1 mutation.
Alzheimer Disease
CA1 hippocampal neuronal loss in familial Alzheimer's disease presenilin-1 E280A mutation is related to epilepsy.
Alzheimer Disease
Caffeine Reverses Cognitive Impairment and Decreases Brain Amyloid-beta Levels in Aged Alzheimer's Disease Mice.
Alzheimer Disease
Calbindin D28k blocks the proapoptotic actions of mutant presenilin 1: reduced oxidative stress and preserved mitochondrial function.
Alzheimer Disease
Calcium enhances the proteolytic activity of BACE1: An in vitro biophysical and biochemical characterization of the BACE1-calcium interaction.
Alzheimer Disease
Calcium ion transients in neutrophils from patients with sporadic Alzheimer's disease.
Alzheimer Disease
Calpain activation promotes BACE1 expression, amyloid precursor protein processing, and amyloid plaque formation in a transgenic mouse model of Alzheimer disease.
Alzheimer Disease
Calsenilin: a calcium-binding protein that interacts with the presenilins and regulates the levels of a presenilin fragment.
Alzheimer Disease
Capacitative calcium entry induces hippocampal long term potentiation in the absence of presenilin-1.
Alzheimer Disease
Carbon-11-Pittsburgh compound B positron emission tomography imaging of amyloid deposition in presenilin 1 mutation carriers.
Alzheimer Disease
Carboxyl-terminal fragments of presenilin-1 are closely related to cytoskeletal abnormalities in Alzheimer's brains.
Alzheimer Disease
Case-control study of presenilin-1 intronic polymorphism in sporadic early and late onset Alzheimer's disease.
Alzheimer Disease
Casein Kinase 2 dependent phosphorylation of eIF4B regulates BACE1 expression in Alzheimer's disease.
Alzheimer Disease
Cases of Alzheimer's disease due to deletion of exon 9 of the presenilin-1 gene show an unusual but characteristic beta-amyloid pathology known as 'cotton wool' plaques.
Alzheimer Disease
Caspase-4 is partially cleaved by calpain via the impairment of Ca2+ homeostasis under the ER stress.
Alzheimer Disease
Catalytic site-directed gamma-secretase complex inhibitors do not discriminate pharmacologically between Notch S3 and beta-APP cleavages.
Alzheimer Disease
CD147 is a regulatory subunit of the gamma-secretase complex in Alzheimer's disease amyloid beta-peptide production.
Alzheimer Disease
CD147, a gamma-secretase associated protein is upregulated in Alzheimer's disease brain and its cellular trafficking is affected by presenilin-2.
Alzheimer Disease
Cdk5 Protein Inhibition and A?42 Increase BACE1 Protein Level in Primary Neurons by a Post-transcriptional Mechanism: IMPLICATIONS OF CDK5 AS A THERAPEUTIC TARGET FOR ALZHEIMER DISEASE.
Alzheimer Disease
Cell and molecular neurobiology of presenilins: a role for the endoplasmic reticulum in the pathogenesis of Alzheimer's disease?
Alzheimer Disease
Cell cycle-driven neuronal apoptosis specifically linked to amyloid peptide Abeta1-42 exposure is not exacerbated in a mouse model of presenilin-1 familial Alzheimer's disease.
Alzheimer Disease
Cell-type-specific enhancement of amyloid-beta deposition in a novel presenilin-1 mutation (P117L).
Alzheimer Disease
Cellular consequences of the expression of Alzheimer's disease-causing presenilin 1 mutations in human neuroblastoma (SH-SY5Y) cells.
Alzheimer Disease
Ceramide stabilizes beta-site amyloid precursor protein-cleaving enzyme 1 and promotes amyloid beta-peptide biogenesis.
Alzheimer Disease
Cerebellar dysfunction in a family harboring the PSEN1 mutation co-segregating with a Cathepsin D variant p.A58V.
Alzheimer Disease
Cerebral amyloid angiopathy is a pathogenic lesion in Alzheimer's disease due to a novel presenilin 1 mutation.
Alzheimer Disease
Cerebrospinal fluid BACE1 activity and brain amyloid load in Alzheimer's disease.
Alzheimer Disease
Cerebrospinal fluid BACE1 activity and markers of amyloid precursor protein metabolism and axonal degeneration in Alzheimer's disease.
Alzheimer Disease
Cerebrospinal Fluid BACE1 Activity and sA?PP? as Biomarker Candidates of Alzheimer's Disease.
Alzheimer Disease
Cerebrospinal fluid Presenilin-1 increases at asymptomatic stage in genetically determined Alzheimer's disease.
Alzheimer Disease
Challenges in diffusion MRI meta-analysis: A discussion of "Genetic influences on white matter and metabolism abnormal change in Alzheimer's disease: Meta-analysis for neuroimaging research on presenilin 1 mutation".
Alzheimer Disease
Changes in Chemokines and Chemokine Receptors Expression in a Mouse Model of Alzheimer's Disease.
Alzheimer Disease
Changes in Neuropsychiatric Inventory Associated with Semagacestat Treatment of Alzheimer's Disease.
Alzheimer Disease
Changing the course of Alzheimer's disease: anti-amyloid disease-modifying treatments on the horizon.
Alzheimer Disease
Characterisation of cytoskeletal abnormalities in mice transgenic for wild-type human tau and familial Alzheimer's disease mutants of APP and presenilin-1.
Alzheimer Disease
Characterization and molecular profiling of PSEN1 familial Alzheimer's disease iPSC-derived neural progenitors.
Alzheimer Disease
Characterization of alpha 2,6-sialyltransferase cleavage by Alzheimer's beta -secretase (BACE1).
Alzheimer Disease
Characterization of an atypical gamma-secretase complex from hematopoietic origin.
Alzheimer Disease
Characterization of beta-amyloid peptide precursor processing by the yeast Yap3 and Mkc7 proteases.
Alzheimer Disease
Characterization of Cerebrospinal Fluid BACE1 Species.
Alzheimer Disease
Characterization of cognitive deficits in a transgenic mouse model of Alzheimer's disease and effects of donepezil and memantine.
Alzheimer Disease
Characterization of detergent-insoluble complexes containing the familial Alzheimer's disease-associated presenilins.
Alzheimer Disease
Characterization of human presenilin 1 transgenic rats: increased sensitivity to apoptosis in primary neuronal cultures.
Alzheimer Disease
Characterization of human presenilin 1 using N-terminal specific monoclonal antibodies: Evidence that Alzheimer mutations affect proteolytic processing.
Alzheimer Disease
Characterization of mouse Ire1 alpha: cloning, mRNA localization in the brain and functional analysis in a neural cell line.
Alzheimer Disease
Characterization of presenilin complexes from mouse and human brain using Blue Native gel electrophoresis reveals high expression in embryonic brain and minimal change in complex mobility with pathogenic presenilin mutations.
Alzheimer Disease
Characterization of recombinant, soluble beta-secretase from an insect cell expression system.
Alzheimer Disease
Characterization of the Photophysical, Thermodynamic, and Structural Properties of the Terbium(III)-DREAM Complex.
Alzheimer Disease
Characterization of the reconstituted gamma-secretase complex from Sf9 cells co-expressing presenilin 1, nicastrin [correction of nacastrin], aph-1a, and pen-2.
Alzheimer Disease
Chemical cross-linking provides a model of the gamma-secretase complex subunit architecture and evidence for close proximity of the C-terminal fragment of presenilin with APH-1.
Alzheimer Disease
Chemoproteomic profiling reveals that cathepsin D off-target activity drives ocular toxicity of ?-secretase inhibitors.
Alzheimer Disease
CHF5074, a novel gamma-secretase modulator, attenuates brain beta-amyloid pathology and learning deficit in a mouse model of Alzheimer's disease.
Alzheimer Disease
CHF5074, a novel gamma-secretase modulator, restores hippocampal neurogenesis potential and reverses contextual memory deficit in a transgenic mouse model of Alzheimer's disease.
Alzheimer Disease
Chinese Presenilin-1 V97L mutation enhanced Abeta42 levels in SH-SY5Y neuroblastoma cells.
Alzheimer Disease
Cholesterol accumulation in Niemann Pick type C (NPC) model cells causes a shift in APP localization to lipid rafts.
Alzheimer Disease
Cholesterol retention in Alzheimer's brain is responsible for high beta- and gamma-secretase activities and A beta production.
Alzheimer Disease
Cholesterol-depletion corrects APP and BACE1 misstrafficking in NPC1-deficient cells.
Alzheimer Disease
Cholinesterase inhibitors influence APP metabolism in Alzheimer disease patients.
Alzheimer Disease
Choroidal Proteins Involved in Cerebrospinal Fluid Production may be Potential Drug Targets for Alzheimer's Disease Therapy.
Alzheimer Disease
Chromosome 14 familial Alzheimer's disease: the clinical and neuropathological characteristics of a family with a leucine-->serine (L250S) substitution at codon 250 of the presenilin 1 gene.
Alzheimer Disease
Chronic treatment with the gamma-secretase inhibitor LY-411,575 inhibits beta-amyloid peptide production and alters lymphopoiesis and intestinal cell differentiation.
Alzheimer Disease
Chronic Verubecestat Treatment Suppresses Amyloid Accumulation in Advanced Aged Tg2576-A?PPswe Mice Without Inducing Microhemorrhage.
Alzheimer Disease
Chronicles in drug discovery.
Alzheimer Disease
Cleavage of amyloid-beta precursor protein and amyloid-beta precursor-like protein by BACE 1.
Alzheimer Disease
Click Chemistry-mediated Biotinylation Reveals a Function for the Protease BACE1 in Modulating the Neuronal Surface Glycoproteome.
Alzheimer Disease
Clinical and biomarker investigation of a patient with a novel presenilin-1 mutation (A431V) in the mild cognitive impairment stage of Alzheimer's disease.
Alzheimer Disease
Clinical and genetic analysis of a Chilean family with early-onset autosomal dominant Alzheimer's disease.
Alzheimer Disease
Clinical and molecular studies reveal a PSEN1 mutation (L153V) in a Peruvian family with early-onset Alzheimer's disease.
Alzheimer Disease
Clinical and neuropathological findings in a patient with familial Alzheimer disease showing a mutation in the PSEN1 gene.
Alzheimer Disease
Clinical Association of White Matter Hyperintensities Localization in a Mexican Family with Spastic Paraparesis Carrying the PSEN1 A431E Mutation.
Alzheimer Disease
Clinical characterization of a presenilin 1 mutation (F177S) in a family with very early-onset Alzheimer's disease in the third decade of life.
Alzheimer Disease
Clinical features of early-onset Alzheimer disease in a large kindred with an E280A presenilin-1 mutation.
Alzheimer Disease
Clinical Phenotype of G206D Mutation in the Presenilin 1 Gene in Pathologically Confirmed Familial Alzheimer's Disease.
Alzheimer Disease
Clinical phenotypic heterogeneity of Alzheimer's disease associated with mutations of the presenilin-1 gene.
Alzheimer Disease
Clinical Presentation of Early-Onset Alzheimer's Disease as a Result of Mutation in Exon 12 of the PSEN-1 Gene.
Alzheimer Disease
Clinical, imaging, pathological, and biochemical characterization of a novel presenilin 1 mutation (N135Y) causing Alzheimer's disease.
Alzheimer Disease
Clinical, neuropathologic, and biochemical profile of the amyloid precursor protein I716F mutation.
Alzheimer Disease
Clinical, pathological, and biochemical spectrum of Alzheimer disease associated with PS-1 mutations.
Alzheimer Disease
Clinical-Genetic Correlations in Familial Alzheimer's Disease Caused by Presenilin 1 Mutations.
Alzheimer Disease
Clinical-genetic correlations in familial Alzheimer's disease caused by presenilin 1 mutations.
Alzheimer Disease
Clinicopathological correlations and cholinesterase expression in early-onset familial Alzheimer's disease with the presenilin 1 mutation, Leu235Pro.
Alzheimer Disease
Clinicopathological features of familial Alzheimer's disease associated with the M139V mutation in the presenilin 1 gene. Pedigree but not mutation specific age at onset provides evidence for a further genetic factor.
Alzheimer Disease
Cloning and characterization of the presenilin-2 gene promoter.
Alzheimer Disease
Cloning and expression of the rat BACE1 promoter.
Alzheimer Disease
Co-cultures with stem cell-derived human sensory neurons reveal regulators of peripheral myelination.
Alzheimer Disease
Co-expression of nicastrin and presenilin rescues a loss of function mutant of APH-1.
Alzheimer Disease
Cognitive decline in patients with familial Alzheimer's disease associated with E280a presenilin-1 mutation: a longitudinal study.
Alzheimer Disease
Combined association of Presenilin-1 and Apolipoprotein E polymorphisms with maternal meiosis II error in Down syndrome births.
Alzheimer Disease
Combining Dyad Protonation and Active Site Plasticity in BACE-1 Structure-Based Drug Design.
Alzheimer Disease
Combining NMR and X-ray Crystallography in Fragment-Based Drug Discovery: Discovery of Highly Potent and Selective BACE-1 Inhibitors.
Alzheimer Disease
Comparative molecular docking studies of lupeol and lupenone isolated from Pueraria lobata that inhibits BACE1: Probable remedies for Alzheimer's disease.
Alzheimer Disease
Comparative study of the effects of phosphatidylcholine rich in DHA and EPA on Alzheimer's disease and the possible mechanisms in CHO-APP/PS1 cells and SAMP8 mice.
Alzheimer Disease
Comparison of clinical and pathological phenotypes in two ethnically and geographically unrelated pedigrees segregating an equivalent presenilin 1 mutation.
Alzheimer Disease
Complete analysis of the presenilin 1 gene in early onset Alzheimer's disease.
Alzheimer Disease
Complete genomic screen in late-onset familial Alzheimer disease. Evidence for a new locus on chromosome 12.
Alzheimer Disease
Complex translational regulation of BACE1 involves upstream AUGs and stimulatory elements within the 5' untranslated region.
Alzheimer Disease
Computational analysis of Alzheimer-causing mutations in amyloid precursor protein and presenilin 1.
Alzheimer Disease
Computing the Pathogenicity of Alzheimer's Disease Presenilin 1 Mutations.
Alzheimer Disease
Conformational Changes in Transmembrane Domain 4 of Presenilin 1 Are Associated with Altered Amyloid-? 42 Production.
Alzheimer Disease
Conformational Dynamics and Binding Free Energies of Inhibitors of BACE-1: From the Perspective of Protonation Equilibria.
Alzheimer Disease
Conformational dynamics of cathepsin D and binding to a small-molecule BACE1 inhibitor.
Alzheimer Disease
Conformational dynamics of transmembrane domain 3 of presenilin 1 is associated with the trimming activity of ?-secretase.
Alzheimer Disease
Conformational transition in the substrate binding domain of ?-secretase exploited by NMA and its implication in inhibitor recognition: BACE1-myricetin a case study.
Alzheimer Disease
Consequences of Pharmacological BACE Inhibition on Synaptic Structure and Function.
Alzheimer Disease
Conserved residues within the putative active site of gamma-secretase differentially influence enzyme activity and inhibitor binding.
Alzheimer Disease
Continuing strategies for inhibiting Alzheimer's gamma-secretase.
Alzheimer Disease
Contrasting role of presenilin-1 and presenilin-2 in neuronal differentiation in vitro.
Alzheimer Disease
Contribution of the proteasome to the alpha-secretase pathway in Alzheimer's disease.
Alzheimer Disease
Control of amyloid-beta-peptide generation by subcellular trafficking of the beta-amyloid precursor protein and beta-secretase.
Alzheimer Disease
Control of peripheral nerve myelination by the beta-secretase BACE1.
Alzheimer Disease
Convergence of pathology in dementia with Lewy bodies and Alzheimer's disease: a role for the novel interaction of alpha-synuclein and presenilin 1 in disease.
Alzheimer Disease
Conversion of the LXR-agonist TO-901317--from inverse to normal modulation of gamma-secretase by addition of a carboxylic acid and a lipophilic anchor.
Alzheimer Disease
Core Refinement towards Permeable ß-Secretase (BACE-1) Inhibitors with Low hERG Activity.
Alzheimer Disease
Correction for Bao et al., BACE1 SUMOylation increases its stability and escalates the protease activity in Alzheimer's disease.
Alzheimer Disease
Correction: Mild Oxidative Stress Induces Redistribution of BACE1 in Non-Apoptotic Conditions and Promotes the Amyloidogenic Processing of Alzheimer's Disease Amyloid Precursor Protein.
Alzheimer Disease
Correction: MiR-124 acts as a target for Alzheimer's disease by regulating BACE1.
Alzheimer Disease
Cortical atrophy in presymptomatic Alzheimer's disease presenilin 1 mutation carriers.
Alzheimer Disease
Corticobasal Syndrome in a Family with Early-Onset Alzheimer's Disease Linked to a Presenilin-1 Gene Mutation.
Alzheimer Disease
Cotton wool plaques in non-familial late-onset Alzheimer disease.
Alzheimer Disease
cPLA2 and desaturases underlie the tau hyperphosphorylation offset induced by BACE knock-down in neuronal primary cultures.
Alzheimer Disease
Creation of Novel Cores for ?-Secretase (BACE-1) Inhibitors: A Multiparameter Lead Generation Strategy.
Alzheimer Disease
Crystal structure of human BACE2 in complex with a hydroxyethylamine transition-state inhibitor.
Alzheimer Disease
CSF BACE1 activity is increased in CJD and Alzheimer disease other dementias.
Alzheimer Disease
CSF biomarkers for mild cognitive impairment.
Alzheimer Disease
CSF levels of the BACE1 substrate NRG1 correlate with cognition in Alzheimer's disease.
Alzheimer Disease
CSF markers for incipient Alzheimer's disease.
Alzheimer Disease
CSF markers for pathogenic processes in Alzheimer's disease: diagnostic implications and use in clinical neurochemistry.
Alzheimer Disease
CSF Presenilin-1 complexes are increased in Alzheimer's disease.
Alzheimer Disease
CSF studies facilitate DNA diagnosis in familial Alzheimer's disease due to a presenilin-1 mutation.
Alzheimer Disease
Curcumin mediates presenilin-1 activity to reduce ?-amyloid production in a model of Alzheimer's Disease.
Alzheimer Disease
Current and future implications of basic and translational research on amyloid-? peptide production and removal pathways.
Alzheimer Disease
Cyanobacterial peptides as a prototype for the design of potent ?-secretase inhibitors and the development of selective chemical probes for other aspartic proteases.
Alzheimer Disease
Cyclin-dependent kinase-5/p35 phosphorylates Presenilin 1 to regulate carboxy-terminal fragment stability.
Alzheimer Disease
Cyclooxygenase (COX)-2 and COX-1 potentiate beta-amyloid peptide generation through mechanisms that involve gamma-secretase activity.
Alzheimer Disease
Cyclooxygenase-2 and presenilin-1 gene expression induced by interleukin-1beta and amyloid beta 42 peptide is potentiated by hypoxia in primary human neural cells.
Alzheimer Disease
Cysteine proteases are the major beta-secretase in the regulated secretory pathway that provides most of the beta-amyloid in Alzheimer's disease: role of BACE 1 in the constitutive secretory pathway.
Alzheimer Disease
Cytoskeletal alterations differentiate presenilin-1 and sporadic Alzheimer's disease.
Alzheimer Disease
De novo presenilin 1 mutations are rare in clinically sporadic, early onset Alzheimer's disease cases. French Alzheimer's Disease Study Group.
Alzheimer Disease
De Novo PS1 Mutation (Pro436Gln) in a Very Early-Onset Posterior Variant of Alzheimer's Disease Associated with Spasticity: A Case Report.
Alzheimer Disease
Decrease in age-adjusted cerebrospinal fluid beta-secretase activity in Alzheimer's subjects.
Alzheimer Disease
Decrease in brain soluble amyloid precursor protein ? (sAPP?) in Alzheimer's disease cortex.
Alzheimer Disease
Decreased Abeta secretion by cells expressing familial Alzheimer's disease-linked mutant presenilin 1.
Alzheimer Disease
Decreased Deposition of Beta-Amyloid 1-38 and Increased Deposition of Beta-Amyloid 1-42 in Brain Tissue of Presenilin-1 E280A Familial Alzheimer's Disease Patients.
Alzheimer Disease
Decreased nuclear beta-catenin, tau hyperphosphorylation and neurodegeneration in GSK-3beta conditional transgenic mice.
Alzheimer Disease
Decreased plasma cholesterol levels during aging in transgenic mouse models of Alzheimer's disease.
Alzheimer Disease
Deducing the transmembrane domain organization of presenilin-1 in gamma-secretase by cysteine disulfide cross-linking.
Alzheimer Disease
Defects of immune regulation in the presenilin-1 mutant knockin mouse.
Alzheimer Disease
Deficiency of Neuronal p38? MAPK Attenuates Amyloid Pathology in Alzheimer Disease Mouse and Cell Models through Facilitating Lysosomal Degradation of BACE1.
Alzheimer Disease
Deficiency of presenilin-1 inhibits the normal cleavage of amyloid precursor protein.
Alzheimer Disease
Deficiency of the Copper Chaperone for Superoxide Dismutase Increases Amyloid-? Production.
Alzheimer Disease
Deficits in Enrichment-Dependent Neurogenesis and Enhanced Anxiety Behaviors Mediated by Expression of Alzheimer's Disease-Linked Ps1 Variants Are Rescued by Microglial Depletion.
Alzheimer Disease
Degenerative alterations in noradrenergic neurons of the locus coeruleus in Alzheimer's disease.
Alzheimer Disease
Deletion of exons 9 and 10 of the Presenilin 1 gene in a patient with Early-onset Alzheimer Disease generates longer amyloid seeds.
Alzheimer Disease
Deletion of presenilin 1 hydrophilic loop sequence leads to impaired gamma-secretase activity and exacerbated amyloid pathology.
Alzheimer Disease
Deletion of the neuron-specific protein delta-catenin leads to severe cognitive and synaptic dysfunction.
Alzheimer Disease
Delivery of BACE1 siRNA mediated by TARBP-BTP fusion protein reduces ?-amyloid deposits in a transgenic mouse model of Alzheimer's disease.
Alzheimer Disease
Delivery of Quantum Dot-siRNA Nanoplexes in SK-N-SH Cells for BACE1 Gene Silencing and Intracellular Imaging.
Alzheimer Disease
Delivery of siRNA to the mouse brain by systemic injection of targeted exosomes.
Alzheimer Disease
delta-catenin is a nervous system-specific adherens junction protein which undergoes dynamic relocalization during development.
Alzheimer Disease
Delta-catenin is required for the maintenance of neural structure and function in mature cortex in vivo.
Alzheimer Disease
Densin-180 interacts with delta-catenin/neural plakophilin-related armadillo repeat protein at synapses.
Alzheimer Disease
Deposition of BACE-1 Protein in the Brains of APP/PS1 Double Transgenic Mice.
Alzheimer Disease
Deposition of Hyperphosphorylated Tau in Cerebellum of PS1 E280A Alzheimer's Disease.
Alzheimer Disease
Derivation of induced pluripotent stem cells from a familial Alzheimer's disease patient carrying the L282F mutation in presenilin 1.
Alzheimer Disease
Design and synthesis of 1,4-dihydropyridine derivatives as BACE-1 inhibitors.
Alzheimer Disease
Design and synthesis of benzoazepinone-derived cyclic malonamides and aminoamides as potent gamma-secretase inhibitors.
Alzheimer Disease
Design and synthesis of highly potent benzodiazepine gamma-secretase inhibitors: preparation of (2S,3R)-3-(3,4-difluorophenyl)-2-(4-fluorophenyl)-4- hydroxy-N-((3S)-1-methyl-2-oxo-5- phenyl-2,3-dihydro-1H-benzo[e][1,4]-diazepin-3-yl)butyramide by use of an asymmetric Ireland-Claisen rearrangement.
Alzheimer Disease
Design and synthesis of novel arylisoxazole-chromenone carboxamides: Investigation of biological activities associated with Alzheimer's disease.
Alzheimer Disease
Design, synthesis and biological evaluation of tasiamide B derivatives as BACE1 inhibitors.
Alzheimer Disease
Design, Synthesis and Evaluation of 2,4,6-substituted Pyrimidine Derivatives as BACE-1 inhibitor: Plausible lead for Alzheimer's Disease.
Alzheimer Disease
Design, synthesis and in vitro evaluation studies of sulfonyl-amino-acetamides as small molecule BACE-1 inhibitors.
Alzheimer Disease
Design, synthesis and SAR analysis of potent BACE1 inhibitors: Possible lead drug candidates for Alzheimer's disease.
Alzheimer Disease
Design, synthesis, and biological evaluation of a novel class of gamma-secretase modulators with PPARgamma activity.
Alzheimer Disease
Design, synthesis, and evaluation of tetrahydroquinoline and pyrrolidine sulfonamide carbamates as gamma-secretase inhibitors.
Alzheimer Disease
Designing of Selective ?-Secretase Inhibitory Benzenesulfonamides through Comparative In Vitro and In Silico Analysis.
Alzheimer Disease
Destabilization of beta-catenin by mutations in presenilin-1 potentiates neuronal apoptosis.
Alzheimer Disease
Detection of the presenilin 1 COOH-terminal fragment in the extracellular compartment: a release enhanced by apoptosis.
Alzheimer Disease
Detection of the presenilin 1 gene mutation (M139T) in early-onset familial Alzheimer disease in Spain.
Alzheimer Disease
Determination of a cleavage site of presenilin 2 protein in stably transfected SH-SY5Y human neuroblastoma cell lines.
Alzheimer Disease
Determination of a novel gamma-secretase inhibitor in human plasma and cerebrospinal fluid using automated 96 well solid phase extraction and liquid chromatography/tandem mass spectrometry.
Alzheimer Disease
Determination of the active site protonation state of beta-secretase from molecular dynamics simulation and docking experiment: implications for structure-based inhibitor design.
Alzheimer Disease
Determination of the protonation state for the catalytic dyad in ?-secretase when bound to hydroxyethylamine transition state analogue inhibitors: A molecular dynamics simulation study.
Alzheimer Disease
Development and characterization of beta-secretase monolithic micro-immobilized enzyme reactor for on-line high-performance liquid chromatography studies.
Alzheimer Disease
Development and validation of sensitive and selective LC-MS/MS methods for the determination of BMS-708163, a gamma-secretase inhibitor, in plasma and cerebrospinal fluid using deprotonated or formate adduct ions as precursor ions.
Alzheimer Disease
Development of 2-aminooxazoline 3-azaxanthene ?-amyloid cleaving enzyme (BACE) inhibitors with improved selectivity against Cathepsin D.
Alzheimer Disease
Development of a high-throughput assay for screening of gamma-secretase inhibitor with endogenous human, mouse or drosophila gamma-secretase.
Alzheimer Disease
Development of a specific ELISA to measure BACE1 levels in human tissues.
Alzheimer Disease
Development of an efficient enzyme production and structure-based discovery platform for BACE1 inhibitors.
Alzheimer Disease
Development of BACE1 inhibitors for Alzheimer's disease.
Alzheimer Disease
Development of molecular tools for diagnosis of Alzheimer's disease that are based on detection of amyloidogenic proteins.
Alzheimer Disease
Development of semagacestat (LY450139), a functional gamma-secretase inhibitor, for the treatment of Alzheimer's disease.
Alzheimer Disease
Developmental regulation and possible alternative cleavage of presenilin 1 in the rat retina.
Alzheimer Disease
DGGE method for the mutational analysis of the coding and proximal promoter regions of the Alzheimer's disease presenilin-1 gene: two novel mutations.
Alzheimer Disease
Diagnostic accuracy of CERAD total score in a Colombian cohort with mild cognitive impairment and Alzheimer's disease affected by E280A mutation on presenilin-1 gene.
Alzheimer Disease
Dictyostelium possesses highly diverged presenilin/gamma-secretase that regulates growth and cell-fate specification and can accurately process human APP: a system for functional studies of the presenilin/gamma-secretase complex.
Alzheimer Disease
Different clinical phenotypes in siblings with a presenilin-1 P264L mutation.
Alzheimer Disease
Different effects of Alzheimer-associated mutations of presenilin 1 on its processing.
Alzheimer Disease
Differential contribution of the three Aph1 genes to gamma-secretase activity in vivo.
Alzheimer Disease
Differential contributions of ApoE4 and female sex to BACE1 activity and expression mediate A? deposition and learning and memory in mouse models of Alzheimer's disease.
Alzheimer Disease
Differential display analysis of presenilin 1-deficient mouse brains.
Alzheimer Disease
Differential distribution of presenilin-1, Bax, and Bcl-X(L) in Alzheimer's disease and frontotemporal dementia.
Alzheimer Disease
Differential effects of transforming growth factor-beta(s) and glial cell line-derived neurotrophic factor on gene expression of presenilin-1 in human post-mitotic neurons and astrocytes.
Alzheimer Disease
Differential expression of presenilin-alpha and -beta (PSalpha and PSbeta) in Xenopus laevis: embryonic phosphorylation of PSalpha.
Alzheimer Disease
Differential gene expression in ADAM10 and mutant ADAM10 transgenic mice.
Alzheimer Disease
Differential regulation of BACE1 promoter activity by nuclear factor-kappaB in neurons and glia upon exposure to beta-amyloid peptides.
Alzheimer Disease
Differential regulation of neurogenesis in two neurogenic regions of APPswe/PS1dE9 transgenic mice.
Alzheimer Disease
Differential utilization of upstream AUGs in the beta-secretase mRNA suggests that a shunting mechanism regulates translation.
Alzheimer Disease
Differentially expressed genes in transgenic mice carrying human mutant presenilin-2 (N141I): correlation of selenoprotein M with Alzheimer's disease.
Alzheimer Disease
Difluoro ketone peptidomimetics suggest a large S1 pocket for Alzheimer's gamma-secretase: implications for inhibitor design.
Alzheimer Disease
Dimethyl Fumarate Exerts Neuroprotection by Modulating Calcineurin/NFAT1 and NF?B Dependent BACE1 Activity in a Neuronal Model of Alzheimer's Disease.
Alzheimer Disease
Direct association of presenilin-1 with beta-catenin.
Alzheimer Disease
Directed conversion of Alzheimer's disease patient skin fibroblasts into functional neurons.
Alzheimer Disease
Discovery and Early Clinical Development of LY3202626, a Low-Dose, CNS-Penetrant BACE Inhibitor.
Alzheimer Disease
Discovery of (S)-2-((S)-2-(3,5-difluorophenyl)-2-hydroxyacetamido)-N-((S,Z)-3-methyl-4-oxo-4,5-dihydro-3H-benzo[d][1,2]diazepin-5-yl)propanamide (BMS-433796): a gamma-secretase inhibitor with Abeta lowering activity in a transgenic mouse model of Alzheimer's disease.
Alzheimer Disease
Discovery of 2,4,6-trisubstituted N-arylsulfonyl piperidines as gamma-secretase inhibitors.
Alzheimer Disease
Discovery of a novel pharmacological and structural class of gamma secretase modulators derived from the extract of Actaea racemosa.
Alzheimer Disease
Discovery of a Subnanomolar helical D-tridecapeptide inhibitor of gamma-secretase.
Alzheimer Disease
Discovery of an Orally Available, Brain Penetrant BACE1 Inhibitor that Affords Robust CNS A? Reduction.
Alzheimer Disease
Discovery of AZD3839, a potent and selective BACE1 inhibitor clinical candidate for the treatment of Alzheimer disease.
Alzheimer Disease
Discovery of begacestat, a Notch-1-sparing gamma-secretase inhibitor for the treatment of Alzheimer's disease.
Alzheimer Disease
Discovery of gamma-secretase inhibitors efficacious in a transgenic animal model of Alzheimer's disease.
Alzheimer Disease
Discovery of N-ethylpyridine-2-carboxamide derivatives as a novel scaffold for orally active ?-secretase modulators.
Alzheimer Disease
Discovery of novel scaffolds for ?-secretase modulators without an arylimidazole moiety.
Alzheimer Disease
Discovery of potent beta-secretase (bace-1) inhibitors by the synthesis of isophthalamide-containing hybrids.
Alzheimer Disease
Discovery of SCH 900229, a Potent Presenilin 1 Selective ?-Secretase Inhibitor for the Treatment of Alzheimer's Disease.
Alzheimer Disease
Discovery of Sulforaphane as a Potent BACE1 Inhibitor Based on Kinetics and Computational Studies.
Alzheimer Disease
Disease-modifying approach to the treatment of Alzheimer's disease: from alpha-secretase activators to gamma-secretase inhibitors and modulators.
Alzheimer Disease
Disease-related mutations among Caribbean Hispanics with familial dementia.
Alzheimer Disease
Disrupted intracellular calcium regulates BACE1 gene expression via nuclear factor of activated T cells 1 (NFAT 1) signaling.
Alzheimer Disease
Dissecting the many genetic faces of schizophrenia.
Alzheimer Disease
Disturbed activation of endoplasmic reticulum stress transducers by familial Alzheimer's disease-linked presenilin-1 mutations.
Alzheimer Disease
Divalent cation tolerance protein binds to ?-secretase and inhibits the processing of amyloid precursor protein.
Alzheimer Disease
Diverging longitudinal changes in astrocytosis and amyloid PET in autosomal dominant Alzheimer's disease.
Alzheimer Disease
Dll4 signalling through Notch1 regulates formation of tip cells during angiogenesis.
Alzheimer Disease
DNA Damage does not Correlate with Amyloid-beta-Plaques and Neurofibrillary Tangles in Familial Alzheimer's Disease Presenilin-1 [E280A] Mutation.
Alzheimer Disease
DNA methylation of the 5'-untranslated region at +298 and +351 represses BACE1 expression in mouse BV-2 microglial cells.
Alzheimer Disease
DNA microarray profiling of developing PS1-deficient mouse brain reveals complex and coregulated expression changes.
Alzheimer Disease
Docking, molecular dynamics, binding energy-MM-PBSA studies of naphthofuran derivatives to identify potential dual inhibitors against BACE-1 and GSK-3?.
Alzheimer Disease
Does oxybutynin alter plaques, amyloid beta peptides and behavior in a mouse model of Alzheimer's disease?
Alzheimer Disease
Dopa Responsive Parkinsonism in an Early Onset Alzheimer's Disease Patient with a Presenilin 1 Mutation (A434T).
Alzheimer Disease
Dose-dependent inhibition of BACE-1 by the monoterpenoid 2,3,4,4-tetramethyl-5-methylenecyclopent-2-enone in cellular and mouse models of Alzheimer's disease.
Alzheimer Disease
Downregulated miR-29c correlates with increased BACE1 expression in sporadic Alzheimer's disease.
Alzheimer Disease
Driving force to detect Alzheimer's disease biomarkers: application of a thioflavine T@Er-MOF ratiometric fluorescent sensor for smart detection of presenilin 1, amyloid ?-protein and acetylcholine.
Alzheimer Disease
Dual inhibition of BACE1 and A? aggregation by ?-ecdysone: Application of a phytoecdysteroid scaffold in Alzheimer's disease therapeutics.
Alzheimer Disease
Dual roles of proteasome in the metabolism of presenilin 1.
Alzheimer Disease
Dual Signal Amplification Electrochemical Biosensor for Monitoring the Activity and Inhibition of the Alzheimer's Related Protease ?-Secretase.
Alzheimer Disease
Dual Task Abilities as a Possible Preclinical Marker of Alzheimer's Disease in Carriers of the E280A Presenilin-1 Mutation.
Alzheimer Disease
Dual-target compounds for Alzheimer's disease: Natural and synthetic AChE and BACE-1 dual-inhibitors and their structure-activity relationship (SAR).
Alzheimer Disease
Dual-target-directed 1,3-diphenylurea derivatives: BACE 1 inhibitor and metal chelator against Alzheimer's disease.
Alzheimer Disease
Dynamic Nature of presenilin1/?-Secretase: Implication for Alzheimer's Disease Pathogenesis.
Alzheimer Disease
Dynamic presenilin 1 and synaptotagmin 1 interaction modulates exocytosis and amyloid ? production.
Alzheimer Disease
Dynamics of Abeta turnover and deposition in different beta-amyloid precursor protein transgenic mouse models following gamma-secretase inhibition.
Alzheimer Disease
Dynamics of {beta}-amyloid reductions in brain, cerebrospinal fluid, and plasma of {beta}-amyloid precursor protein transgenic mice treated with a {gamma}-secretase inhibitor.
Alzheimer Disease
Dyrk1A-mediated phosphorylation of Presenilin 1: a functional link between Down syndrome and Alzheimer's disease.
Alzheimer Disease
Dysregulated IP3 signaling in cortical neurons of knock-in mice expressing an Alzheimer's-linked mutation in presenilin1 results in exaggerated Ca2+ signals and altered membrane excitability.
Alzheimer Disease
Dysregulation of SREBP2 induces BACE1 expression.
Alzheimer Disease
E280A PS-1 mutation causes Alzheimer's disease but age of onset is not modified by ApoE alleles.
Alzheimer Disease
Ear2 deletion causes early memory and learning deficits in APP/PS1 mice.
Alzheimer Disease
Early onset Alzheimer's disease - a case study.
Alzheimer Disease
Early onset familial Alzheimer Disease with spastic paraparesis, dysarthria, and seizures and N135S mutation in PSEN1.
Alzheimer Disease
Early psychiatrics symptoms in familial Alzheimer's disease with presenilin 1 mutation (I83T).
Alzheimer Disease
Early structural changes in individuals at risk of familial Alzheimer's disease: a volumetry and magnetization transfer MR imaging study.
Alzheimer Disease
Early-onset Alzheimer disease in an Italian family with presenilin-1 double mutation E318G and G394V.
Alzheimer Disease
Early-onset Alzheimer's disease caused by a novel mutation at codon 219 of the presenilin-1 gene.
Alzheimer Disease
Early-onset Alzheimer's disease due to mutations of the presenilin-1 gene on chromosome 14: a 7-year follow-up of a patient with a mutation at codon 139.
Alzheimer Disease
Early-onset Alzheimer's disease with a de novo mutation in the presenilin 1 gene.
Alzheimer Disease
Early-onset Alzheimer's disease with a presenilin-1 mutation at the site corresponding to the Volga German presenilin-2 mutation.
Alzheimer Disease
Early-onset Alzheimer's disease with presenilin-1 M139V mutation: clinical, neuropsychological and neuropathological study.
Alzheimer Disease
Early-onset amyloid deposition and cognitive deficits in transgenic mice expressing a double mutant form of amyloid precursor protein 695.
Alzheimer Disease
Early-Onset Familial Alzheimer Disease Variant PSEN2 N141I Heterozygosity is Associated with Altered Microglia Phenotype.
Alzheimer Disease
Early-onset familial Alzheimer's disease related to presenilin 1 mutation resembling autosomal dominant spinocerebellar ataxia.
Alzheimer Disease
Editorial: Implications for BACE1 Inhibitor Clinical Trials: Adult Conditional BACE1 Knockout Mice Exhibit Axonal Organization Defects in the Hippocampus.
Alzheimer Disease
EEG and Granular Osmiophilic Elements in Early-Onset Alzheimer's Disease.
Alzheimer Disease
EEG, Activity, and Sleep Architecture in a Transgenic A?PPSWE/PSEN1A246E Alzheimer's Disease Mouse.
Alzheimer Disease
Effect of a dominant-negative form of ADAM10 in a mouse model of Alzheimer's disease.
Alzheimer Disease
Effect of gamma-secretase inhibitors on muscarinic receptor-mediated calcium signaling in human salivary epithelial cells.
Alzheimer Disease
Effect of glycogen synthase kinase 3 ?-mediated presenilin 1 phosphorylation on amyloid ? production is negatively regulated by insulin receptor cleavage.
Alzheimer Disease
Effect of heparin on APP metabolism and Abeta production in cortical neurons.
Alzheimer Disease
Effect of sampling on BACE-1 ligands binding free energy predictions via MM-PBSA calculations.
Alzheimer Disease
Effect of the protonation state of the titratable residues on the inhibitor affinity to BACE-1.
Alzheimer Disease
Effects of a gamma-secretase inhibitor in a randomized study of patients with Alzheimer disease.
Alzheimer Disease
Effects of an inhibitor of alpha-secretase, which metabolizes the amyloid peptide precursor, on memory formation in rats.
Alzheimer Disease
Effects of curcuminoids identified in rhizomes of Curcuma longa on BACE-1 inhibitory and behavioral activity and lifespan of Alzheimer's disease Drosophila models.
Alzheimer Disease
Effects of gamma-secretase inhibition on the amyloid beta isoform pattern in a mouse model of Alzheimer's disease.
Alzheimer Disease
Effects of human presenilin 1 isoforms on proliferation and survival of rat pheochromocytoma cell line PC12.
Alzheimer Disease
Effects of long-term treatment with pioglitazone on cognition and glucose metabolism of PS1-KI, 3xTg-AD, and wild-type mice.
Alzheimer Disease
Effects of Mild and Severe Oxidative Stress on BACE1 Expression and APP Amyloidogenic Processing.
Alzheimer Disease
Effects of presenilin N-terminal fragments on production of amyloid beta peptide and accumulation of endogenous presenilins.
Alzheimer Disease
Effects of progesterone administration and APPswe+PSEN1Deltae9 mutation for cognitive performance of mid-aged mice.
Alzheimer Disease
Effects of RNA interference-mediated silencing of gamma-secretase complex components on cell sensitivity to caspase-3 activation.
Alzheimer Disease
Effects of short-term Western diet on cerebral oxidative stress and diabetes related factors in APP x PS1 knock-in mice.
Alzheimer Disease
Efficacy of SPI-1865, a novel gamma-secretase modulator, in multiple rodent models.
Alzheimer Disease
Egr-1 upregulates the Alzheimer's disease presenilin-2 gene in neuronal cells.
Alzheimer Disease
EHT0202 in Alzheimer's Disease: A 3-Month, Randomized, Placebo-Controlled, Double-Blind Study.
Alzheimer Disease
Electric Stimulation of Neurogenesis Improves Behavioral Recovery After Focal Ischemia in Aged Rats.
Alzheimer Disease
Electroacupuncture ameliorates beta-amyloid pathology and cognitive impairment in Alzheimer disease via a novel mechanism involving activation of TFEB (transcription factor EB).
Alzheimer Disease
Electrophoretic separation and immunoblotting of a?(1-40) and a? (1-42).
Alzheimer Disease
Elevated A?42 in Aged, Non-demented Individuals with Cerebral Atherosclerosis.
Alzheimer Disease
Elevated cellular cholesterol in Familial Alzheimer's presenilin 1 mutation is associated with lipid raft localization of ?-amyloid precursor protein.
Alzheimer Disease
Elevated cerebrospinal fluid BACE1 activity in incipient Alzheimer disease.
Alzheimer Disease
Elucidation of the BACE1 Regulating Factor GGA3 in Alzheimer's Disease.
Alzheimer Disease
Employing a superior BACE1 cleavage sequence to probe cellular APP processing.
Alzheimer Disease
Encompassing receptor flexibility in virtual screening using ensemble docking-based hybrid QSAR: discovery of novel phytochemicals for BACE1 inhibition.
Alzheimer Disease
Endogenous APP accumulates in synapses after BACE1 inhibition.
Alzheimer Disease
Endogenous presenilin 1 redistributes to the surface of lamellipodia upon adhesion of Jurkat cells to a collagen matrix.
Alzheimer Disease
Endogenous presenilin-1 targets to endocytic rather than biosynthetic compartments.
Alzheimer Disease
Endoproteolysis of beta-secretase (beta-site amyloid precursor protein-cleaving enzyme) within its catalytic domain. A potential mechanism for regulation.
Alzheimer Disease
Endoproteolysis of presenilin in vitro: inhibition by gamma-secretase inhibitors.
Alzheimer Disease
Endoproteolysis of the ER stress transducer ATF6 in the presence of functionally inactive presenilins.
Alzheimer Disease
Endoproteolytic processing and stabilization of wild-type and mutant presenilin.
Alzheimer Disease
Enhanced accumulation of phosphorylated alpha-synuclein and elevated beta-amyloid 42/40 ratio caused by expression of the presenilin-1 deltaT440 mutant associated with familial Lewy body disease and variant Alzheimer's disease.
Alzheimer Disease
Enhanced brain activity may precede the diagnosis of Alzheimer's disease by 30 years.
Alzheimer Disease
Enhanced delivery of gamma-secretase inhibitor DAPT into the brain via an ascorbic acid mediated strategy.
Alzheimer Disease
Enhanced production and oligomerization of the 42-residue amyloid beta-protein by Chinese hamster ovary cells stably expressing mutant presenilins.
Alzheimer Disease
Enhanced synaptic potentiation in transgenic mice expressing presenilin 1 familial Alzheimer's disease mutation is normalized with a benzodiazepine.
Alzheimer Disease
Enhancement of activation of caspases by presenilin 1 gene mutations and its inhibition by secretase inhibitors.
Alzheimer Disease
Enhancement of alpha-secretase cleavage of amyloid precursor protein by a metalloendopeptidase nardilysin.
Alzheimer Disease
Enhancement of amyloid beta 42 secretion by 28 different presenilin 1 mutations of familial Alzheimer's disease.
Alzheimer Disease
Enhancement of BACE1 Activity by p25/Cdk5-Mediated Phosphorylation in Alzheimer's Disease.
Alzheimer Disease
Enrichment of presenilin 1 peptides in neuronal large dense-core and somatodendritic clathrin-coated vesicles.
Alzheimer Disease
Environmental exposures and the etiopathogenesis of Alzheimer's disease: The potential role of BACE1 as a critical neurotoxic target.
Alzheimer Disease
Enzymic properties of recombinant BACE2.
Alzheimer Disease
Epicatechin Plus Treadmill Exercise are Neuroprotective Against Moderate-stage Amyloid Precursor Protein/Presenilin 1 Mice.
Alzheimer Disease
Epidermal Growth Factor Receptor and Notch Pathways Participate in the Tumor Suppressor Function of {gamma}-Secretase.
Alzheimer Disease
Epigenetic Changes and Its Intervention in Age-Related Neurodegenerative Diseases.
Alzheimer Disease
Epigenetic regulation of BACE1 in Alzheimer's disease patients and in transgenic mice.
Alzheimer Disease
ER stress is not elevated in the 5XFAD mouse model of Alzheimer's disease.
Alzheimer Disease
ERK1/2 is an endogenous negative regulator of the gamma-secretase activity.
Alzheimer Disease
Establishing the relationship between in vitro potency, pharmacokinetic and pharmacodynamic parameters in a series of orally available, hydroxyethylamine-derived ?-secretase inhibitors.
Alzheimer Disease
Estimating diagnostic accuracy for clustered ordinal diagnostic groups in the three-class case-Application to the early diagnosis of Alzheimer disease.
Alzheimer Disease
Estimation of the genetic contribution of presenilin-1 and -2 mutations in a population-based study of presenile Alzheimer disease.
Alzheimer Disease
Estrogens stabilize mitochondrial function and protect neural cells against the pro-apoptotic action of mutant presenilin-1.
Alzheimer Disease
Etazolate improves performance in a foraging and homing task in aged rats.
Alzheimer Disease
Evaluation of an Allosteric BACE Inhibitor Peptide to Identify Mimetics that Can Interact with the Loop F Region of the Enzyme and Prevent APP Cleavage.
Alzheimer Disease
Evaluation of polymorphisms in the presenilin-1 gene and the butyrylcholinesterase gene as risk factors in sporadic Alzheimer's disease.
Alzheimer Disease
Event-related potential markers of brain changes in preclinical familial Alzheimer disease.
Alzheimer Disease
Evidence for a six-transmembrane domain structure of presenilin 1.
Alzheimer Disease
Evidence for natural antisense transcript-mediated inhibition of microRNA function.
Alzheimer Disease
Evidence for phosphorylation and oligomeric assembly of presenilin 1.
Alzheimer Disease
Evidence for presenilin-1 involvement in amyloid angiopathy in the Alzheimer's disease-affected brain.
Alzheimer Disease
Evidence for the involvement of calbindin D28k in the presenilin 1 model of Alzheimer's disease.
Alzheimer Disease
Evidence that Abeta42 plasma levels in presenilin-1 mutation carriers do not allow for prediction of their clinical phenotype.
Alzheimer Disease
Evidence that gamma-secretase mediates oxidative stress-induced beta-secretase expression in Alzheimer's disease.
Alzheimer Disease
Ex vivo occupancy of gamma-secretase inhibitors correlates with brain beta-amyloid peptide reduction in Tg2576 mice.
Alzheimer Disease
Exacerbation of psoriatic skin lesions in a patient with Alzheimer disease receiving gamma-secretase inhibitor.
Alzheimer Disease
Excess of nicastrin in brain results in heterozygosity having no effect on endogenous APP processing and amyloid peptide levels in vivo.
Alzheimer Disease
Exclusively targeting beta-secretase to lipid rafts by GPI-anchor addition up-regulates beta-site processing of the amyloid precursor protein.
Alzheimer Disease
Exercise-mediated alteration of hippocampal Dicer mRNA and miRNAs is associated with lower BACE1 gene expression and A?1-42 in female 3xTg-AD mice.
Alzheimer Disease
Existing plaques and neuritic abnormalities in APP:PS1 mice are not affected by administration of the gamma-secretase inhibitor LY-411575.
Alzheimer Disease
Exome sequencing identifies 2 novel presenilin 1 mutations (p.L166V and p.S230R) in British early-onset Alzheimer's disease.
Alzheimer Disease
Exploring the chemical space of gamma-secretase modulators.
Alzheimer Disease
Expressing mRNAs for presenilin-1 and amyloid precursor protein (APP-695) from same neuronal populations in rat hippocampus.
Alzheimer Disease
Expression analysis of BACE2 in brain and peripheral tissues.
Alzheimer Disease
Expression analysis of human ?-secretase in transgenic tomato fruits.
Alzheimer Disease
Expression and activity of beta-site amyloid precursor protein cleaving enzyme in Alzheimer's disease.
Alzheimer Disease
Expression and analysis of presenilin 1 in a human neuronal system: localization in cell bodies and dendrites.
Alzheimer Disease
Expression of ?-site APP-cleaving enzyme 1 in the hippocampal tissue of an insulin-resistant rat model of Alzheimer's disease.
Alzheimer Disease
Expression of a noncoding RNA is elevated in Alzheimer's disease and drives rapid feed-forward regulation of beta-secretase.
Alzheimer Disease
Expression of Alzheimer's disease risk genes in ischemic brain degeneration.
Alzheimer Disease
Expression of Amyloid-Associated miRNAs in Both the Forebrain Cortex and Hippocampus of Middle-Aged Rat.
Alzheimer Disease
Expression of familial Alzheimer disease presenilin 1 gene attenuates vesicle traffic and reduces peptide secretion in cultured astrocytes devoid of pathologic tissue environment.
Alzheimer Disease
Expression of presenilin 1 and 2 (PS1 and PS2) in human and murine tissues.
Alzheimer Disease
Expression of presenilin 1 mRNA in rat peripheral organs and brain.
Alzheimer Disease
Expression of presenilin-1 and -2 mRNAs in rat and Alzheimer's disease brains.
Alzheimer Disease
Expression of the Alzheimer protease BACE1 is suppressed via its 5'-untranslated region.
Alzheimer Disease
Expression of the Alzheimer's Disease Mutations A?PP695sw and PSEN1M146I in Double-Transgenic Göttingen Minipigs.
Alzheimer Disease
Expressions of amyloid precursor protein, synaptophysin and presenilin-1 in the different areas of the developing cerebellum of rat.
Alzheimer Disease
Extreme cerebrospinal fluid amyloid beta levels identify family with late-onset Alzheimer's disease presenilin 1 mutation.
Alzheimer Disease
F175S change and a novel polymorphism in presenilin-1 gene in late-onset familial Alzheimer's disease.
Alzheimer Disease
Facilitation of glutamate, but not GABA, release in Familial Alzheimer's APP mutant Knock-in rats with increased ?-cleavage of APP.
Alzheimer Disease
FAD mutations in presenilin-1 or amyloid precursor protein decrease the efficacy of a gamma-secretase inhibitor: evidence for direct involvement of PS1 in the gamma-secretase cleavage complex.
Alzheimer Disease
Familial Alzheimer disease presenilin-1 mutations alter the active site conformation of ?-secretase.
Alzheimer Disease
Familial Alzheimer's disease co-segregates with a Met146I1e substitution in presenilin-1.
Alzheimer Disease
Familial Alzheimer's disease coding mutations reduce Presenilin-1 expression in a novel genomic locus reporter model.
Alzheimer Disease
Familial Alzheimer's disease genes in Japanese.
Alzheimer Disease
Familial Alzheimer's Disease Lymphocytes Respond Differently Than Sporadic Cells to Oxidative Stress: Upregulated p53-p21 Signaling Linked with Presenilin 1 Mutants.
Alzheimer Disease
Familial Alzheimer's Disease Mutations in Presenilin 1 Do Not Alter Levels of the Secreted Amyloid-beta Protein Precursor Generated by beta-Secretase Cleavage.
Alzheimer Disease
Familial Alzheimer's disease mutations in presenilin 1 do not alter levels of the secreted amyloid-beta protein precursor generated by beta-secretase cleavage.
Alzheimer Disease
Familial Alzheimer's Disease Mutations in PSEN1 Lead to Premature Human Stem Cell Neurogenesis.
Alzheimer Disease
Familial Alzheimer's disease mutations inhibit gamma-secretase-mediated liberation of beta-amyloid precursor protein carboxy-terminal fragment.
Alzheimer Disease
Familial Alzheimer's Disease Mutations within the Amyloid Precursor Protein Alter the Aggregation and Conformation of the Amyloid-? Peptide.
Alzheimer Disease
Familial Alzheimer's disease presenilin 1 mutation M146V increases gamma secretase cutting of p75NTR in vitro.
Alzheimer Disease
Familial Alzheimer's disease presenilin 1 mutations cause alterations in the conformation of presenilin and interactions with amyloid precursor protein.
Alzheimer Disease
Familial Alzheimer's disease presenilin-1 mutants potentiate cell cycle arrest.
Alzheimer Disease
Familial Alzheimer's disease presenilin-2 mutants affect Ca2+ homeostasis and brain network excitability.
Alzheimer Disease
Familial Alzheimer's disease-linked presenilin 1 variants elevate Abeta1-42/1-40 ratio in vitro and in vivo.
Alzheimer Disease
Familial Alzheimer's disease-linked presenilin-1 mutation M146V affects store-operated calcium entry: does gain look like loss?
Alzheimer Disease
Familial Alzheimer's disease: oxidative stress, beta-amyloid, presenilins, and cell death.
Alzheimer Disease
Familial cases presenting very early onset autosomal dominant Alzheimer's disease with I143T in presenilin-1 gene: implication for genotype-phenotype correlation.
Alzheimer Disease
Familial Creutzfeldt-Jakob disease in a patient carrying both a presenilin 1 missense substitution and a prion protein gene insertion.
Alzheimer Disease
Familial dementia with frontotemporal features associated with M146V presenilin-1 mutation.
Alzheimer Disease
Familial frontotemporal dementia-associated presenilin-1 c.548G>T mutation causes decreased mRNA expression and reduced presenilin function in knock-in mice.
Alzheimer Disease
Fatty acids increase presenilin-1 levels and [gamma]-secretase activity in PSwt-1 cells.
Alzheimer Disease
Fe65 stimulates proteolytic liberation of the beta-amyloid precursor protein intracellular domain.
Alzheimer Disease
Female preclinical presenilin-1 mutation carriers unaware of their genetic status have higher levels of depression than their non-mutation carrying kin.
Alzheimer Disease
Fenchylamine sulfonamide inhibitors of amyloid beta peptide production by the gamma-secretase proteolytic pathway: potential small-molecule therapeutic agents for the treatment of Alzheimer's disease.
Alzheimer Disease
Fibroblasts from FAD-linked presenilin 1 mutations display a normal unfolded protein response but overproduce Abeta42 in response to tunicamycin.
Alzheimer Disease
Flavonoid-mediated presenilin-1 phosphorylation reduces Alzheimer's disease beta-amyloid production.
Alzheimer Disease
Flavonols and flavones as BACE-1 inhibitors: structure-activity relationship in cell-free, cell-based and in silico studies reveal novel pharmacophore features.
Alzheimer Disease
Florbetapir PET analysis of amyloid-? deposition in the presenilin 1 E280A autosomal dominant Alzheimer's disease kindred: a cross-sectional study.
Alzheimer Disease
Flotillins bind to the Dileucine Sorting Motif of BACE1 and influence its endosomal Sorting.
Alzheimer Disease
Forebrain degeneration and ventricle enlargement caused by double knockout of Alzheimer's presenilin-1 and presenilin-2.
Alzheimer Disease
Forebrain depletion of Rheb GTPase elicits spatial memory deficits in mice.
Alzheimer Disease
Formation of stable complexes between two Alzheimer's disease gene products: presenilin-2 and beta-amyloid precursor protein.
Alzheimer Disease
Formation of Tau Inclusions in Knock-in Mice with Familial Alzheimer Disease (FAD) Mutation of Presenilin 1 (PS1).
Alzheimer Disease
Founder effect for the Ala431Glu mutation of the presenilin 1 gene causing early-onset Alzheimer's disease in Mexican families.
Alzheimer Disease
Fragment-Based Discovery of Nonpeptidic BACE-1 Inhibitors Using Tethering.
Alzheimer Disease
Fragment-guided approach to incorporating structural information into a CoMFA study: BACE-1 as an example.
Alzheimer Disease
Frequency and clinicopathological characteristics of presenilin 1 Gly206Ala mutation in Puerto Rican Hispanics with dementia.
Alzheimer Disease
From BACE1 inhibitor to multifunctionality of tryptoline and tryptamine triazole derivatives for Alzheimer's disease.
Alzheimer Disease
From presenilinase to gamma-secretase, cleave to capacitate.
Alzheimer Disease
From virtual screening hits targeting a cryptic pocket in BACE-1 to a nontoxic brain permeable multitarget anti-Alzheimer lead with disease-modifying and cognition-enhancing effects.
Alzheimer Disease
Full-length cellular ?-secretase has a trimeric subunit stoichiometry, and its sulfur-rich transmembrane interaction site modulates cytosolic copper compartmentalization.
Alzheimer Disease
Function, therapeutic potential and cell biology of BACE proteases: current status and future prospects.
Alzheimer Disease
Functional characterization of novel presenilin-2 variants identified in human breast cancers.
Alzheimer Disease
Functional gamma-secretase inhibitors reduce beta-amyloid peptide levels in brain.
Alzheimer Disease
Functional implications of the presenilin dimerization: reconstitution of gamma-secretase activity by assembly of a catalytic site at the dimer interface of two catalytically inactive presenilins.
Alzheimer Disease
Functional interactions of APP with the apoE receptor family.
Alzheimer Disease
Functional phenotype in transgenic mice expressing mutant human presenilin-1.
Alzheimer Disease
Functions of the Alzheimer's Disease Protease BACE1 at the Synapse in the Central Nervous System.
Alzheimer Disease
Fyn knock-down increases A?, decreases phospho-tau, and worsens spatial learning in 3×Tg-AD mice.
Alzheimer Disease
G Protein-Coupled Receptors (GPCRs) in Alzheimer's Disease: A Focus on BACE1 Related GPCRs.
Alzheimer Disease
G206D Mutation of Presenilin-1 Reduces Pen2 Interaction, Increases A?42/A?40 Ratio and Elevates ER Ca(2+) Accumulation.
Alzheimer Disease
Gadd153 and NF-?B Crosstalk Regulates 27-Hydroxycholesterol-Induced Increase in BACE1 and ?-Amyloid Production in Human Neuroblastoma SH-SY5Y Cells.
Alzheimer Disease
Gain of function by phosphorylation in Presenilin 1-mediated regulation of insulin signaling.
Alzheimer Disease
Gallic Acid is a Dual ?/?-Secretase Modulator that Reverses Cognitive Impairment and Remediates Pathology in Alzheimer Mice.
Alzheimer Disease
Gamma -secretase inhibitors repress thymocyte development.
Alzheimer Disease
Gamma secretase-activating protein is a substrate for caspase-3: implications for Alzheimer's disease.
Alzheimer Disease
gamma-cleavage-independent functions of presenilin, nicastrin, and Aph-1 regulate cell-junction organization and prevent tau toxicity in vivo.
Alzheimer Disease
Gamma-secretase activating protein is a therapeutic target for Alzheimer's disease.
Alzheimer Disease
Gamma-secretase activity is associated with a conformational change of nicastrin.
Alzheimer Disease
gamma-Secretase activity modulates store-operated Ca2+ entry into rat sensory neurons.
Alzheimer Disease
Gamma-secretase activity of presenilin 1 regulates acetylcholine muscarinic receptor-mediated signal transduction.
Alzheimer Disease
Gamma-secretase and the intramembrane proteolysis of Notch.
Alzheimer Disease
Gamma-secretase as a pharmacological target in Alzheimer disease research: when, why and how?
Alzheimer Disease
gamma-Secretase as a target for drug intervention in Alzheimer's disease.
Alzheimer Disease
Gamma-secretase as a therapeutic target for the treatment of Alzheimer's disease.
Alzheimer Disease
gamma-Secretase as a Therapeutic Target for Treatment of Alzheimer's Disease.
Alzheimer Disease
gamma-Secretase as a therapeutic target in Alzheimer's disease.
Alzheimer Disease
gamma-Secretase can cleave amyloid precursor protein fragments independent of alpha- and beta-secretase pre-cutting.
Alzheimer Disease
gamma-Secretase dependent production of intracellular domains is reduced in adult compared to embryonic rat brain membranes.
Alzheimer Disease
Gamma-secretase gene mutations link acne inversa (flexural, scarring acne) with Alzheimer's disease.
Alzheimer Disease
gamma-Secretase heterogeneity in the Aph1 subunit: relevance for Alzheimer's disease.
Alzheimer Disease
gamma-Secretase in biology and medicine.
Alzheimer Disease
Gamma-secretase inhibition and modulation for Alzheimer's disease.
Alzheimer Disease
Gamma-secretase inhibition.
Alzheimer Disease
Gamma-secretase inhibitors and Alzheimer's disease.
Alzheimer Disease
gamma-Secretase inhibitors as molecular probes of presenilin function.
Alzheimer Disease
gamma-Secretase Inhibitors for Alzheimer's Disease : Balancing Efficacy and Toxicity.
Alzheimer Disease
gamma-Secretase Inhibitors for the Treatment of Alzheimer's Disease: The Current State.
Alzheimer Disease
Gamma-secretase is a membrane protein complex comprised of presenilin, nicastrin, Aph-1, and Pen-2.
Alzheimer Disease
Gamma-secretase modulation and its promise for Alzheimer's disease: a medicinal chemistry perspective.
Alzheimer Disease
Gamma-secretase modulation and its promise for Alzheimer's disease: a rationale for drug discovery.
Alzheimer Disease
gamma-Secretase modulators.
Alzheimer Disease
gamma-Secretase substrate selectivity can be modulated directly via interaction with a nucleotide-binding site.
Alzheimer Disease
Gamma-secretase subunit composition and distribution in the presenilin wild-type and mutant mouse brain.
Alzheimer Disease
gamma-Secretase, evidence for multiple proteolytic activities and influence of membrane positioning of substrate on generation of amyloid beta peptides of varying length.
Alzheimer Disease
gamma-Secretase, Notch, Abeta and Alzheimer's disease: where do the presenilins fit in?
Alzheimer Disease
Gamma-secretase--intramembrane protease with a complex.
Alzheimer Disease
Gamma-secretase-dependent and -independent effects of presenilin1 on beta-catenin.Tcf-4 transcriptional activity.
Alzheimer Disease
Gamma-secretase/presenilin inhibitors for Alzheimer's disease phenocopy Notch mutations in Drosophila.
Alzheimer Disease
Gamma-secretase: a catalyst of Alzheimer disease and signal transduction.
Alzheimer Disease
Gamma-secretase: a complex target for Alzheimer's disease.
Alzheimer Disease
gamma-Secretase: characterization and implication for Alzheimer disease therapy.
Alzheimer Disease
Gamma-secretase: structure, function, and modulation for Alzheimer's disease.
Alzheimer Disease
gamma-secretases: from cell biology to therapeutic strategies.
Alzheimer Disease
Gastrodin suppresses BACE1 expression under oxidative stress condition via inhibition of the PKR/eIF2? pathway in Alzheimer's disease.
Alzheimer Disease
Gender- and age-dependent gamma-secretase activity in mouse brain and its implication in sporadic Alzheimer disease.
Alzheimer Disease
Gene expression in Alzheimer's disease.
Alzheimer Disease
Gene expression of Alzheimer-associated presenilin-2 in the frontal cortex of Alzheimer and aged control brain.
Alzheimer Disease
Gene Expression Profiles of APP and BACE1 in Tg SOD1G93A Cortical Cells.
Alzheimer Disease
Gene expression profiling in cells with enhanced gamma-secretase activity.
Alzheimer Disease
Gene mutations associated with early onset familial Alzheimer's disease in China: An overview and current status.
Alzheimer Disease
Gene polymorphism in apolipoprotein E and presenilin-1 in patients with late-onset Alzheimer's disease.
Alzheimer Disease
Generation and deposition of A?43 by the virtually inactive presenilin-1 L435F mutant contradicts the presenilin loss-of-function hypothesis of Alzheimer's disease.
Alzheimer Disease
Generation of a gene-corrected isogenic control hiPSC line derived from a familial Alzheimer's disease patient carrying a L150P mutation in presenilin 1.
Alzheimer Disease
Generation of Abeta38 and Abeta42 is independently and differentially affected by familial Alzheimer disease-associated presenilin mutations and gamma-secretase modulation.
Alzheimer Disease
Generation of aggregation prone N-terminally truncated amyloid ? peptides by meprin ? depends on the sequence specificity at the cleavage site.
Alzheimer Disease
Generation of amyloid beta protein from a presenilin-1 and betaAPP complex.
Alzheimer Disease
Generation of an integration-free iPSC line, ICCSICi006-A, derived from a male Alzheimer's disease patient carrying the PSEN1-G206D mutation.
Alzheimer Disease
Generation of induced pluripotent stem cells (iPSCs) from an Alzheimer's disease patient carrying a L150P mutation in PSEN-1.
Alzheimer Disease
Generation of induced pluripotent stem cells (iPSCs) from an Alzheimer's disease patient carrying a M146I mutation in PSEN1.
Alzheimer Disease
Generation of induced pluripotent stem cells (iPSCs) from an Alzheimer's disease patient carrying an A79V mutation in PSEN1.
Alzheimer Disease
Generation of induced pluripotent stem cells (IRMBi001-A) from an Alzheimer's disease patient carrying a G217D mutation in the PSEN1 gene.
Alzheimer Disease
Genes implicated in the pathogenesis of Alzheimer's disease.
Alzheimer Disease
Genes involved in cerebrospinal fluid production as candidate genes for late-onset Alzheimer's disease: a hypothesis.
Alzheimer Disease
Genetic and molecular aspects of Alzheimer's disease shed light on new mechanisms of transcriptional regulation.
Alzheimer Disease
Genetic aspects of Alzheimer disease.
Alzheimer Disease
Genetic association between intronic polymorphism in presenilin-1 gene and late-onset Alzheimer's disease. Alzheimer's Disease Collaborative Group.
Alzheimer Disease
Genetic association of BACE1 gene polymorphism C786G with late-onset Alzheimer's disease in Chinese.
Alzheimer Disease
Genetic association of the presenilin-1 regulatory region with early-onset Alzheimer's disease in a population-based sample.
Alzheimer Disease
Genetic association of two chromosome 14 genes (presenilin 1 and alpha 1-antichymotrypsin) with Alzheimer's disease.
Alzheimer Disease
Genetic complexity of Alzheimer's disease: successes and challenges.
Alzheimer Disease
Genetic counseling and presenilin-1 Alzheimer's disease: "Research Family" members share some thoughts.
Alzheimer Disease
Genetic deletion of BACE1 in mice affects remyelination of sciatic nerves.
Alzheimer Disease
Genetic influences on white matter and metabolism abnormal change in Alzheimer's disease: Meta-analysis for neuroimaging research on presenilin 1 mutation.
Alzheimer Disease
Genetic inhibition of phosphorylation of the translation initiation factor eIF2? does not block A?-dependent elevation of BACE1 and APP levels or reduce amyloid pathology in a mouse model of Alzheimer's disease.
Alzheimer Disease
Genetic markers in the diagnosis of Alzheimer's disease.
Alzheimer Disease
Genetic Markers of Alzheimer's Disease.
Alzheimer Disease
Genetic reductions of beta-site amyloid precursor protein-cleaving enzyme 1 and amyloid-beta ameliorate impairment of conditioned taste aversion memory in 5XFAD Alzheimer's disease model mice.
Alzheimer Disease
Genetic screening in early-onset Alzheimer's disease identified three novel presenilin mutations.
Alzheimer Disease
Genetic screening in two Iranian families with early-onset Alzheimer's disease identified a novel PSEN1 mutation.
Alzheimer Disease
Genetic studies of A2M and BACE1 genes in Chinese Han Alzheimer's disease patients.
Alzheimer Disease
Genetic variability at the amyloid-beta precursor protein locus may contribute to the risk of late-onset Alzheimer's disease.
Alzheimer Disease
Genetic variability in the regulatory region of presenilin 1 associated with risk for Alzheimer's disease and variable expression.
Alzheimer Disease
Genetics and pathology of alpha-secretase site AbetaPP mutations in the understanding of Alzheimer's disease.
Alzheimer Disease
Genetics of Alzheimer's disease.
Alzheimer Disease
Genomic structure, expression pattern, and chromosomal localization of the human calsenilin gene: no association between an exonic polymorphism and Alzheimer's disease.
Alzheimer Disease
Genotoxicity Studies of Titanium Dioxide Nanoparticles (TiO2NPs) in the Brain of Mice.
Alzheimer Disease
Genotype-phenotype analysis in early-onset Alzheimer's disease due to presenilin-1 mutations at codon 139.
Alzheimer Disease
Genotype-phenotype correlation in early-onset Alzheimer disease with presenilin 1 gene mutations.
Alzheimer Disease
Genotype-Phenotype Relationships of Presenilin-1 Mutations in Alzheimer's Disease: An Update.
Alzheimer Disease
Geriatric neurogenetics: oxymoron or reality?
Alzheimer Disease
Germline mutational analysis of presenilin 1 and APP genes in Jewish-Israeli individuals with familial or early-onset Alzheimer disease using denaturing gradient gel electrophoresis (DGGE).
Alzheimer Disease
GGA proteins mediate the recycling pathway of memapsin 2 (BACE).
Alzheimer Disease
GGA1 acts as a spatial switch altering amyloid precursor protein trafficking and processing.
Alzheimer Disease
GGA1 is expressed in the human brain and affects the generation of amyloid beta-peptide.
Alzheimer Disease
Gga3 deletion and a GGA3 rare variant associated with late onset Alzheimer's disease trigger BACE1 accumulation in axonal swellings.
Alzheimer Disease
Ginsenoside Rg1 attenuates ?-amyloid generation via suppressing PPAR?-regulated BACE1 activity in N2a-APP695 cells.
Alzheimer Disease
Glucose metabolism and PIB binding in carriers of a His163Tyr presenilin 1 mutation.
Alzheimer Disease
Glycogen synthase kinase-3beta regulates presenilin 1 C-terminal fragment levels.
Alzheimer Disease
Glycosaminoglycans from Litopenaeus vannamei Inhibit the Alzheimer's Disease ? Secretase, BACE1.
Alzheimer Disease
Got RIP? Presenilin-dependent intramembrane proteolysis in growth factor receptor signaling.
Alzheimer Disease
Grape seed polyphenols and curcumin reduce genomic instability events in a transgenic mouse model for Alzheimer's disease.
Alzheimer Disease
GSK3beta activity modifies the localization and function of presenilin 1.
Alzheimer Disease
High affinity, bioavailable 3-amino-1,4-benzodiazepine-based gamma-secretase inhibitors.
Alzheimer Disease
High beta-secretase activity elicits neurodegeneration in transgenic mice despite reductions in amyloid-beta levels: implications for the treatment of Alzheimer disease.
Alzheimer Disease
High content analysis of gamma-secretase activity reveals variable dominance of presenilin mutations linked to familial Alzheimer's disease.
Alzheimer Disease
High levels of Alzheimer beta-amyloid precursor protein (APP) in children with severely autistic behavior and aggression.
Alzheimer Disease
High resolution imaging study of interactions between the 37 kDa/67 kDa laminin receptor and APP, beta-secretase and gamma-secretase in Alzheimer's disease.
Alzheimer Disease
High-fat diet exacerbates cognitive and metabolic abnormalities in neuronal BACE1 knock-in mice - partial prevention by Fenretinide.
Alzheimer Disease
Highlights in BACE1 Inhibitors for Alzheimer's Disease Treatment.
Alzheimer Disease
Highly Pathogenic Alzheimer's Disease Presenilin 1 P117R Mutation Causes a specific Increase in p53 and p21 Protein Levels and Cell Cycle Dysregulation in Human Lymphocytes.
Alzheimer Disease
Histological and Behavioral Phenotypes of a Novel Mutated APP Knock-In Mouse.
Alzheimer Disease
Histone acetyltransferase p300 mediates histone acetylation of PS1 and BACE1 in a cellular model of Alzheimer's disease.
Alzheimer Disease
HMGA1a induces alternative splicing of estrogen receptor alpha in MCF-7 human breast cancer cells.
Alzheimer Disease
HMGA1a trapping of U1 snRNP at an authentic 5' splice site induces aberrant exon skipping in sporadic Alzheimer's disease.
Alzheimer Disease
HMGA1a: sequence-specific RNA-binding factor causing sporadic Alzheimer's disease-linked exon skipping of presenilin-2 pre-mRNA.
Alzheimer Disease
Homozygosity of the autosomal dominant Alzheimer disease presenilin 1 E280A mutation.
Alzheimer Disease
Human aspartic protease memapsin 2 cleaves the beta-secretase site of beta-amyloid precursor protein.
Alzheimer Disease
Human fibroblast and stem cell resource from the Dominantly Inherited Alzheimer Network.
Alzheimer Disease
Human neuroblastoma cells transfected with two Chinese presenilin 1 mutations are sensitized to trophic factor withdrawal and protected by insulin-like growth factor-1.
Alzheimer Disease
Human presenilin-1, but not familial Alzheimer's disease (FAD) mutants, facilitate Caenorhabditis elegans Notch signalling independently of proteolytic processing.
Alzheimer Disease
Human wild presenilin-1 mimics the effect of the mutant presenilin-1 on the processing of Alzheimer's amyloid precursor protein in PC12D cells.
Alzheimer Disease
Human-Induced Neurons from Presenilin 1 Mutant Patients Model Aspects of Alzheimer's Disease Pathology.
Alzheimer Disease
Hybrid approach to sieve out natural compounds against dual targets in Alzheimer's Disease.
Alzheimer Disease
Hybrid Structure-Based Virtual Screening Protocol for the Identification of Novel BACE1 Inhibitors.
Alzheimer Disease
Hybrid structure-based virtual screening protocol for the identification of novel BACE1 inhibitors.
Alzheimer Disease
Hydrocephalus and abnormal subcommissural organ in mice lacking presenilin-1 in Wnt1 cell lineages.
Alzheimer Disease
Hydrogen peroxide promotes Abeta production through JNK-dependent activation of gamma-secretase.
Alzheimer Disease
Hyperaccumulation of FAD-linked presenilin 1 variants in vivo.
Alzheimer Disease
Hypertension accelerates the progression of Alzheimer-like pathology in a mouse model of the disease.
Alzheimer Disease
Hypocapnia induces caspase-3 activation and increases Abeta production.
Alzheimer Disease
Hypometabolism exceeds atrophy in presymptomatic early-onset familial Alzheimer's disease.
Alzheimer Disease
Hypoxia facilitates Alzheimer's disease pathogenesis by up-regulating BACE1 gene expression.
Alzheimer Disease
Hypoxia-inducible factor 1alpha (HIF-1alpha)-mediated hypoxia increases BACE1 expression and beta-amyloid generation.
Alzheimer Disease
Hypoxic remodelling of Ca2+ mobilization in type I cortical astrocytes: involvement of ROS and pro-amyloidogenic APP processing.
Alzheimer Disease
Ibuprofen rescues abnormalities in periodontal tissues in conditional presenilin 1 and presenilin 2 double knockout mice.
Alzheimer Disease
Icariin decreases the expression of APP and BACE-1 and reduces the ?-amyloid burden in an APP transgenic mouse model of Alzheimer's disease.
Alzheimer Disease
Identification of a BACE1 Binding Peptide Candidate for the Prevention of Amyloid Beta in Alzheimer's Disease.
Alzheimer Disease
Identification of a cis-acting element involved in the regulation of BACE1 mRNA alternative splicing.
Alzheimer Disease
Identification of a new presenilin-dependent zeta-cleavage site within the transmembrane domain of amyloid precursor protein.
Alzheimer Disease
Identification of a novel 4.6-kb genomic deletion in presenilin-1 gene which results in exclusion of exon 9 in a Finnish early onset Alzheimer's disease family: an Alu core sequence-stimulated recombination?
Alzheimer Disease
Identification of a novel BACE1 inhibitor, timosaponin A-III, for treatment of Alzheimer's disease by a cell extraction and chemogenomics target knowledgebase-guided method.
Alzheimer Disease
Identification of a novel family of presenilin homologues.
Alzheimer Disease
Identification of a novel mutation (Leu282Arg) of the human presenilin 1 gene in Alzheimer's disease.
Alzheimer Disease
Identification of a novel mutation in the presenilin 1 gene in a Chinese Alzheimer's disease family.
Alzheimer Disease
Identification of a novel PSEN1 Gly111Val missense mutation in a Chinese pedigree with early-onset Alzheimer's disease.
Alzheimer Disease
Identification of a novel PSEN1 mutation (Leu232Pro) in a Korean patient with early-onset Alzheimer's disease and a family history of dementia.
Alzheimer Disease
Identification of a Pathogenic PSEN1 Ala285Val Mutation Associated with Early-Onset Alzheimer's Disease.
Alzheimer Disease
Identification of BACE1 inhibitors from Panax ginseng saponins-An Insilco approach.
Alzheimer Disease
Identification of beta-secretase (BACE1) substrates using quantitative proteomics.
Alzheimer Disease
Identification of distinct gamma-secretase complexes with different APH-1 variants.
Alzheimer Disease
Identification of gamma-secretase inhibitor potency determinants on presenilin.
Alzheimer Disease
Identification of Human Islet Amyloid Polypeptide as a BACE2 Substrate.
Alzheimer Disease
Identification of new BACE1 inhibitors for treating Alzheimer's disease.
Alzheimer Disease
Identification of new presenilin gene mutations in early-onset familial Alzheimer disease.
Alzheimer Disease
Identification of syntaxin 1A as a novel binding protein for presenilin-1.
Alzheimer Disease
Identification of tetrahydrocarbazoles as novel multifactorial drug candidates for treatment of Alzheimer's disease.
Alzheimer Disease
Identification of the presenilins in hematopoietic cells with localization of presenilin 1 to neutrophil and platelet granules.
Alzheimer Disease
Identification of the role of presenilins beyond Alzheimer's disease.
Alzheimer Disease
Identification of ubiquilin, a novel presenilin interactor that increases presenilin protein accumulation.
Alzheimer Disease
Identifying genes that interact with Drosophila presenilin and amyloid precursor protein.
Alzheimer Disease
Iminoheterocycle as a druggable motif: BACE1 inhibitors and beyond.
Alzheimer Disease
Immunocytochemical Characterization of Alzheimer Disease Hallmarks in APP/PS1 Transgenic Mice Treated with a New Anti-Amyloid- ? Vaccine.
Alzheimer Disease
Immunocytochemical Characterization of Alzheimer's Disease Hallmarks in APP/PS1 Transgenic Mice Treated with a New Anti-Amyloid-? Vaccine.
Alzheimer Disease
Immunohistochemical analysis of presenilin 2 expression in the mouse brain: distribution pattern and co-localization with presenilin 1 protein.
Alzheimer Disease
Immunohistochemical analysis of presenilin-1 expression in the mouse brain.
Alzheimer Disease
Immunohistochemical characterization of gamma-secretase activating protein expression in Alzheimer's disease brains.
Alzheimer Disease
Immunomodulation of A?PP Processing Alleviates Amyloid-?-Related Pathology in Alzheimer's Disease Transgenic Mice.
Alzheimer Disease
Immunoreactivity of presenilin-1 and tau in Alzheimer's disease brain.
Alzheimer Disease
Impaired cell proliferation in the subventricular zone in an Alzheimer's disease model.
Alzheimer Disease
Impaired proteolytic processing of presenilin-1 in chromosome 14-linked familial Alzheimer's disease patient lymphocytes.
Alzheimer Disease
Impairment in hippocampal long-term potentiation in mice under-expressing the Alzheimer's disease related gene presenilin-1.
Alzheimer Disease
Implication of APP secretases in notch signaling.
Alzheimer Disease
Implications of presenilin 1 mutations in Alzheimer's disease.
Alzheimer Disease
In silico Analysis of Gamma-Secretase-Complex Mutations in Hidradenitis Suppurativa Demonstrates Disease-Specific Substrate Recognition and Cleavage Alterations.
Alzheimer Disease
In silico design of BACE1 inhibitor for Alzheimer's disease by traditional Chinese medicine.
Alzheimer Disease
In Silico Design of Beta-Secretase Inhibitors in Alzheimer's Disease.
Alzheimer Disease
In silico prediction and screening of gamma-secretase inhibitors by molecular descriptors and machine learning methods.
Alzheimer Disease
In silico screening of drugs to find potential gamma-secretase inhibitors using pharmacophore modeling, QSAR and molecular docking studies.
Alzheimer Disease
In situ hybridization analysis of presenilin 1 mRNA in Alzheimer disease and in lesioned rat brain.
Alzheimer Disease
In vitro and in vivo metabolism of a gamma-secretase inhibitor BMS-299897 and generation of active metabolites in milligram quantities with a microbial bioreactor.
Alzheimer Disease
In vitro biological activity of Salvia fruticosa Mill. infusion against amyloid ?-peptide-induced toxicity and inhibition of GSK-3?, CK-1?, and BACE-1 enzymes relevant to Alzheimer's disease.
Alzheimer Disease
In vitro characterization of a gamma-secretase radiotracer in mammalian brain.
Alzheimer Disease
In vitro gamma-secretase cleavage of the Alzheimer's amyloid precursor protein correlates to a subset of presenilin complexes and is inhibited by zinc.
Alzheimer Disease
In vitro reconstitution of gamma-secretase activity using yeast microsomes.
Alzheimer Disease
In vivo cleavage of alpha2,6-sialyltransferase by Alzheimer beta-secretase.
Alzheimer Disease
In vivo manifestation of Notch related phenotypes in zebrafish treated with Alzheimer's amyloid reducing gamma-secretase inhibitors.
Alzheimer Disease
In vivo neuronal gene editing via CRISPR-Cas9 amphiphilic nanocomplexes alleviates deficits in mouse models of Alzheimer's disease.
Alzheimer Disease
In vivo Reconstitution of {gamma}-Secretase in Drosophila Results in Substrate Specificity.
Alzheimer Disease
Incomplete penetrance of familial Alzheimer's disease in a pedigree with a novel presenilin-1 gene mutation.
Alzheimer Disease
Increase in p53 protein levels by presenilin 1 gene mutations and its inhibition by secretase inhibitors.
Alzheimer Disease
Increase of BACE1, Brain-Renal Risk Factor, Contributes to Kidney Damage in an Alzheimer's Disease Mouse Model.
Alzheimer Disease
Increased Abeta42(43) from cell lines expressing presenilin 1 mutations.
Alzheimer Disease
Increased activity-regulating and neuroprotective efficacy of alpha-secretase-derived secreted amyloid precursor protein conferred by a C-terminal heparin-binding domain.
Alzheimer Disease
Increased amyloid-beta42(43) in brains of mice expressing mutant presenilin 1.
Alzheimer Disease
Increased apoptosis arising from increased expression of the Alzheimer's disease-associated presenilin-2 mutation (N141I).
Alzheimer Disease
Increased BACE1 maturation contributes to the pathogenesis of Alzheimer's disease in Down syndrome.
Alzheimer Disease
Increased blood BACE1 activity as a potential common pathogenic factor of vascular dementia and late onset Alzheimer's disease.
Alzheimer Disease
Increased CSF- BACE1 Activity Associated with Decreased Hippocampus Volume in Alzheimer's Disease.
Alzheimer Disease
Increased CSF-BACE 1 activity is associated with ApoE-epsilon 4 genotype in subjects with mild cognitive impairment and Alzheimer's disease.
Alzheimer Disease
Increased expression of the gamma-secretase components presenilin-1 and nicastrin in activated astrocytes and microglia following traumatic brain injury.
Alzheimer Disease
Increased Foxo3a Nuclear Translocation and Activity is an Early Neuronal Response to ??-Secretase-Mediated Processing of the Amyloid-? Protein Precursor: Utility of an A?PP-GAL4 Reporter Assay.
Alzheimer Disease
Increased Inflammatory Response Both in Brain and in Periphery in Presenilins Conditional Double Knock-Out Mice.
Alzheimer Disease
Increased NF-?B signalling up-regulates BACE1 expression and its therapeutic potential in Alzheimer's disease.
Alzheimer Disease
Increased oxidative stress and astrogliosis responses in conditional double-knockout mice of Alzheimer-like presenilin-1 and presenilin-2.
Alzheimer Disease
Increased Phosphorylation of Tau and Synaptic Protein Loss in the Aged Transgenic Mice Expressing Familiar Alzheimer's Disease-Linked Presenilin 1 Mutation.
Alzheimer Disease
Increased sensitivity to mitochondrial toxin-induced apoptosis in neural cells expressing mutant presenilin-1 is linked to perturbed calcium homeostasis and enhanced oxyradical production.
Alzheimer Disease
Increased tau phosphorylation but absence of formation of neurofibrillary tangles in mice double transgenic for human tau and Alzheimer mutant (M146L) presenilin-1.
Alzheimer Disease
Increased vulnerability of hippocampal neurons from presenilin-1 mutant knock-in mice to amyloid beta-peptide toxicity: central roles of superoxide production and caspase activation.
Alzheimer Disease
Independent generation of Abeta42 and Abeta38 peptide species by gamma-secretase.
Alzheimer Disease
Independent inhibition of Alzheimer disease beta- and gamma-secretase cleavage by lowered cholesterol levels.
Alzheimer Disease
Indirubin-3'-monoxime rescues spatial memory deficits and attenuates beta-amyloid-associated neuropathology in a mouse model of Alzheimer's disease.
Alzheimer Disease
Induced dimerization of the amyloid precursor protein leads to decreased amyloid-beta protein production.
Alzheimer Disease
Induced HMGA1a expression causes aberrant splicing of Presenilin-2 pre-mRNA in sporadic Alzheimer's disease.
Alzheimer Disease
Induction of neuronal death by ER stress in Alzheimer's disease.
Alzheimer Disease
Inflammatory responses to amyloidosis in a transgenic mouse model of Alzheimer's disease.
Alzheimer Disease
Influence of low frequency PSEN1 variants on familial Alzheimer's disease risk in Brazil.
Alzheimer Disease
Inherited Alzheimer's disease PS-1 olfactory function: a 10-year follow-up study.
Alzheimer Disease
Inhibiting amyloid precursor protein C-terminal cleavage promotes an interaction with presenilin 1.
Alzheimer Disease
Inhibiting BACE1 to reverse synaptic dysfunctions in Alzheimer's disease.
Alzheimer Disease
Inhibition and modulation of gamma-secretase for Alzheimer's disease.
Alzheimer Disease
Inhibition of ?-site amyloid precursor protein cleaving enzyme 1 and cholinesterases by pterosins via a specific structure-activity relationship with a strong BBB permeability.
Alzheimer Disease
Inhibition of Alzheimer's amyloid-?42 peptide aggregation by a bi-functional bis-tryptoline triazole: key insights from molecular dynamics simulations.
Alzheimer Disease
Inhibition of AMPA responses by mutated presenilin 1.
Alzheimer Disease
Inhibition of BACE1 Activity by a DNA Aptamer in an Alzheimer's Disease Cell Model.
Alzheimer Disease
Inhibition of BACE1 for therapeutic use in Alzheimer's disease.
Alzheimer Disease
Inhibition of BACE1, the ?-secretase implicated in Alzheimer's disease, by a chondroitin sulfate extract from Sardina pilchardus.
Alzheimer Disease
Inhibition of cyclooxygenase as potential novel therapeutic strategy in N141I presenilin-2 familial Alzheimer's disease.
Alzheimer Disease
Inhibition of gamma-Secretase Activity by Helical beta-Peptide Foldamers.
Alzheimer Disease
Inhibition of gamma-secretase activity reduces Abeta production, reduces oxidative stress, increases mitochondrial activity and leads to reduced vulnerability to apoptosis: Implications for the treatment of Alzheimer's disease.
Alzheimer Disease
Inhibition of gamma-secretase as a therapeutic intervention for Alzheimer's disease: prospects, limitations and strategies.
Alzheimer Disease
Inhibition of gamma-secretase by the CK1 inhibitor IC261 does not depend on CK1delta.
Alzheimer Disease
Inhibition of neurite outgrowth by familial Alzheimer's disease-linked presenilin-1 mutations.
Alzheimer Disease
Inhibition of presenilin 1 expression is promoted by p53 and p21WAF-1 and results in apoptosis and tumor suppression.
Alzheimer Disease
Inhibition of stress induced premature senescence in presenilin-1 mutated cells with water soluble Coenzyme Q10.
Alzheimer Disease
Inhibitors of BACE for treating Alzheimer's disease: a fragment-based drug discovery story.
Alzheimer Disease
Inhibitory effect of a presenilin 1 mutation on the Wnt signalling pathway by enhancement of beta-catenin phosphorylation.
Alzheimer Disease
Inhibitory effect of chloroquine derivatives on presenilin 1 and ubiquilin 1 expression in Alzheimer's disease [Retraction].
Alzheimer Disease
Inhibitory effect of chloroquine derivatives on presenilin 1 and ubiquilin 1 expression in Alzheimer's disease.
Alzheimer Disease
Injury induces presenilin-1 gene expression in mouse brain.
Alzheimer Disease
Insensitivity to Abeta42-lowering nonsteroidal anti-inflammatory drugs and gamma-secretase inhibitors is common among aggressive presenilin-1 mutations.
Alzheimer Disease
Insight into the genetic etiology of Alzheimer's disease: A comprehensive review of the role of rare variants.
Alzheimer Disease
Insights from modeling the tertiary structure of human BACE2.
Alzheimer Disease
Insights into Alzheimer disease pathogenesis from studies in transgenic animal models.
Alzheimer Disease
Insulin Suppresses the Expression of Amyloid Precursor Protein, Presenilins, and Glycogen Synthase Kinase-3{beta} in Peripheral Blood Mononuclear Cells.
Alzheimer Disease
Insulysin Cleaves the APP Cytoplasmic Fragment at Multiple Sites.
Alzheimer Disease
Interaction between the APOE epsilon4 allele and the APH-1b c + 651T > G SNP in Alzheimer's disease.
Alzheimer Disease
Interaction of Alzheimer's presenilin-1 and presenilin-2 with Bcl-X(L). A potential role in modulating the threshold of cell death.
Alzheimer Disease
Interaction of the Presenilins with the Amyloid Precursor Protein (APP).
Alzheimer Disease
Interleukin-1 and the immunogenetics of Alzheimer disease.
Alzheimer Disease
Internalization of exogenously added memapsin 2 (beta-secretase) ectodomain by cells is mediated by amyloid precursor protein.
Alzheimer Disease
Intra- or intercomplex binding to the gamma-secretase enzyme. A model to differentiate inhibitor classes.
Alzheimer Disease
Intracellular calcium deficits in Drosophila cholinergic neurons expressing wild type or FAD-mutant presenilin.
Alzheimer Disease
Intracellularly generated amyloid-beta peptide counteracts the antiapoptotic function of its precursor protein and primes proapoptotic pathways for activation by other insults in neuroblastoma cells.
Alzheimer Disease
Intracerebroventricular transplantation of human amniotic epithelial cells ameliorates spatial memory deficit in the doubly transgenic mice coexpressing APPswe and PS1?E9-deleted genes.
Alzheimer Disease
Intramembrane proteolysis by gamma-secretase.
Alzheimer Disease
Intramembrane proteolysis by signal peptidepeptidases - a comparative discussion of GxGD -type aspartyl proteases.
Alzheimer Disease
Intramembrane proteolysis of GXGD-type aspartyl proteases is slowed by a familial Alzheimer disease-like mutation.
Alzheimer Disease
Intraneuronal advanced glycation endproducts in presenilin-1 Alzheimer's disease.
Alzheimer Disease
Investigation of naphthofuran moiety as potential dual inhibitor against BACE-1 and GSK-3?: molecular dynamics simulations, binding energy, and network analysis to identify first-in-class dual inhibitors against Alzheimer's disease.
Alzheimer Disease
Involvement of Gadd153 in the pathogenic action of presenilin-1 mutations.
Alzheimer Disease
Involvement of Insulin Signaling Disturbances in Bisphenol A-Induced Alzheimer's Disease-like Neurotoxicity.
Alzheimer Disease
Involvement of ubiquilin-1 transcript variants in protein degradation and accumulation.
Alzheimer Disease
Ion channel regulation by ?-secretase BACE1 - enzymatic and non-enzymatic effects beyond Alzheimer's disease.
Alzheimer Disease
Is Alzheimer's Disease a Disorder of Mitochondria-Associated Membranes?
Alzheimer Disease
Is BACE1 a suitable therapeutic target for the treatment of Alzheimer's disease? Current strategies and future directions.
Alzheimer Disease
Is the presenilin-1 E318G missense mutation a risk factor for Alzheimer's disease?
Alzheimer Disease
Isolation and characterization of Drosophila presenilin homolog.
Alzheimer Disease
JLK isocoumarin inhibitors: selective gamma-secretase inhibitors that do not interfere with notch pathway in vitro or in vivo.
Alzheimer Disease
Kinetics and molecular docking studies of fucosterol and fucoxanthin, BACE1 inhibitors from brown algae Undaria pinnatifida and Ecklonia stolonifera.
Alzheimer Disease
Kinetics and molecular docking studies of loganin, morroniside and 7-O-galloyl-D-sedoheptulose derived from Corni fructus as cholinesterase and ?-secretase 1 inhibitors.
Alzheimer Disease
L655,240, acting as a competitive BACE1 inhibitor, efficiently decreases ?-amyloid peptide production in HEK293-APPswe cells.
Alzheimer Disease
Label-free quantitative analysis of the membrane proteome of Bace1 protease knock-out zebrafish brains.
Alzheimer Disease
Label-free Quantitative Proteomics of Mouse Cerebrospinal Fluid Detects ?-Site APP Cleaving Enzyme (BACE1) Protease Substrates In Vivo.
Alzheimer Disease
Lack of ?-amyloid cleaving enzyme-1 (BACE1) impairs long-term synaptic plasticity but enhances granule cell excitability and oscillatory activity in the dentate gyrus in vivo.
Alzheimer Disease
Lack of association between an intronic polymorphism in the presenilin-1 gene and sporadic late-onset Alzheimer disease in Polish patients.
Alzheimer Disease
Lack of association of presenilin-1 intron-8 polymorphism with neuropathological features of Alzheimer's disease.
Alzheimer Disease
Lack of BACE1 S-palmitoylation reduces amyloid burden and mitigates memory deficits in transgenic mouse models of Alzheimer's disease.
Alzheimer Disease
Lack of effect of Presenilin 1, betaAPP and their Alzheimer's disease-related mutated forms on Xenopus oocytes membrane currents.
Alzheimer Disease
Lack of human-like extracellular sortilin neuropathology in transgenic Alzheimer's disease model mice and macaques.
Alzheimer Disease
Lack of interactions between amyloid precursor protein and hydrophilic domains of presenilin 1 and 2 using the yeast two hybrid system.
Alzheimer Disease
Lack of specific association of presenilin 1 (PS-1) protein with plaques and tangles in Alzheimer's disease.
Alzheimer Disease
Lactic acid induces aberrant amyloid precursor protein processing by promoting its interaction with endoplasmic reticulum chaperone proteins.
Alzheimer Disease
Laminar distribution of ?-amyloid (A?) peptide deposits in the frontal lobe in familial and sporadic Alzheimer's disease.
Alzheimer Disease
Laminar specific loss of isocortical presenilin 1 immunoreactivity in Alzheimer's disease. Correlations with the amyloid load and the density of tau-positive neurofibrillary tangles.
Alzheimer Disease
Lanabecestat: Neuroimaging results in early symptomatic Alzheimer's disease.
Alzheimer Disease
Las noticias de Madrid (News from Madrid).
Alzheimer Disease
LDL receptor-related protein (LRP) in Alzheimer's disease: towards a unified theory of pathogenesis.
Alzheimer Disease
Lead neurotoxicity: exploring the potential impact of lead substitution in zinc-finger proteins on mental health.
Alzheimer Disease
Length and overall sequence of the PEN-2 C-terminal domain determines its function in the stabilization of presenilin fragments.
Alzheimer Disease
Lentivirus-expressed siRNA vectors against Alzheimer disease.
Alzheimer Disease
Ligand binding and calcium influx induce distinct ectodomain/gamma-secretase-processing pathways of EphB2 receptor.
Alzheimer Disease
Linear patterns of Alzheimer's disease mutations along alpha-helices of presenilins as a tool for PS-1 model construction.
Alzheimer Disease
Linking vascular disorders and Alzheimer's disease: Potential involvement of BACE1.
Alzheimer Disease
Lipid peroxidation up-regulates BACE1 expression in vivo: a possible early event of amyloidogenesis in Alzheimer's disease.
Alzheimer Disease
Liquid-liquid extraction of strongly protein bound BMS-299897 from human plasma and cerebrospinal fluid, followed by high-performance liquid chromatography/tandem mass spectrometry.
Alzheimer Disease
Localisation of presenilin 2 in human and rodent pancreatic islet beta-cells; Met239Val presenilin 2 variant is not associated with diabetes in man.
Alzheimer Disease
Localization and trafficking of endogenous anterior pharynx-defective 1, a component of Alzheimer's disease related gamma-secretase.
Alzheimer Disease
Localization of Alzheimer-associated presenilin 1 in transfected COS-7 cells.
Alzheimer Disease
Locomotor activity, emotionality, sensori-motor gating, learning and memory in the APPswe/PS1dE9 mouse model of Alzheimer's disease.
Alzheimer Disease
Long-term safety and tolerability of atabecestat (JNJ-54861911), an oral BACE1 inhibitor, in early Alzheimer's disease spectrum patients: a randomized, double-blind, placebo-controlled study and a two-period extension study.
Alzheimer Disease
Longitudinal observation on CSF Abeta42 levels in young to middle-aged amyloid precursor protein/presenilin-1 doubly transgenic mice.
Alzheimer Disease
Loss of A?43 Production Caused by Presenilin-1 Mutations in the Knockin Mouse Brain.
Alzheimer Disease
Loss of endophilin-B1 exacerbates Alzheimer's disease pathology.
Alzheimer Disease
Loss of gamma-secretase function impairs endocytosis of lipoprotein particles and membrane cholesterol homeostasis.
Alzheimer Disease
Loss of microRNA cluster miR-29a/b-1 in sporadic Alzheimer's disease correlates with increased BACE1/beta-secretase expression.
Alzheimer Disease
Loss of neuronal cell cycle control as a mechanism of neurodegeneration in the presenilin-1 Alzheimer's disease brain.
Alzheimer Disease
Loss of presenilin 1 is associated with enhanced beta-catenin signaling and skin tumorigenesis.
Alzheimer Disease
Loss of presenilin function causes Alzheimer's disease-like neurodegeneration in the mouse.
Alzheimer Disease
Loss of stability and hydrophobicity of presenilin 1 mutations causing Alzheimer's disease.
Alzheimer Disease
Low brain ascorbic acid increases susceptibility to seizures in mouse models of decreased brain ascorbic acid transport and Alzheimer's disease.
Alzheimer Disease
Low cholesterol stimulates the nonamyloidogenic pathway by its effect on the alpha -secretase ADAM 10.
Alzheimer Disease
Low-density lipoprotein receptor-related protein promotes amyloid precursor protein trafficking to lipid rafts in the endocytic pathway.
Alzheimer Disease
LRP1 Downregulates the Alzheimer's ?-Secretase BACE1 by Modulating Its Intraneuronal Trafficking(1,2,3).
Alzheimer Disease
LRRTM3 interacts with APP and BACE1 and has variants associating with late-onset Alzheimer's disease (LOAD).
Alzheimer Disease
LRRTM3 promotes processing of amyloid-precursor protein by BACE1 and is a positional candidate gene for late-onset Alzheimer's disease.
Alzheimer Disease
Luteolin Reduces BACE1 Expression through NF-?B and Estrogen Receptor Mediated Pathways in HEK293 and SH-SY5Y Cells.
Alzheimer Disease
Lysosomal alkalization and dysfunction in human fibroblasts with the Alzheimer's disease-linked presenilin 1 A246E mutation can be reversed with cAMP.
Alzheimer Disease
Lysosomal proteolysis and autophagy require presenilin 1 and are disrupted by Alzheimer-related PS1 mutations.
Alzheimer Disease
Lysosomal TPCN (two pore segment channel) inhibition ameliorates beta-amyloid pathology and mitigates memory impairment in Alzheimer disease.
Alzheimer Disease
Machine learning models for predicting the activity of AChE and BACE1 dual inhibitors for the treatment of Alzheimer's disease.
Alzheimer Disease
Macrocyclic BACE inhibitors: Optimization of a micromolar hit to nanomolar leads.
Alzheimer Disease
Magnesium Modulates Amyloid-beta Protein Precursor Trafficking and Processing.
Alzheimer Disease
Maladaptive exploratory behavior and neuropathology of the PS-1 P117L Alzheimer transgenic mice.
Alzheimer Disease
Male-specific association between a gamma-secretase polymorphism and premature coronary atherosclerosis.
Alzheimer Disease
Mapping the APP/presenilin (PS) binding domains: the hydrophilic N-terminus of PS2 is sufficient for interaction with APP and can displace APP/PS1 interaction.
Alzheimer Disease
Masking of transmembrane-based retention signals controls ER export of gamma-secretase.
Alzheimer Disease
Maturation and endosomal targeting of beta-site amyloid precursor protein-cleaving enzyme. The Alzheimer's disease beta-secretase.
Alzheimer Disease
Mean age of onset in familial Alzheimer's disease is determined by amyloid beta 42.
Alzheimer Disease
Measuring human beta-secretase (BACE1) activity using homogeneous time-resolved fluorescence.
Alzheimer Disease
Mechanism of gamma-secretase cleavage activation: is gamma-secretase regulated through autoinhibition involving the presenilin-1 exon 9 loop?
Alzheimer Disease
Mechanism of the cleavage specificity of Alzheimer's disease gamma-secretase identified by phenylalanine-scanning mutagenesis of the transmembrane domain of the amyloid precursor protein.
Alzheimer Disease
Mechanisms that lessen benefits of ?-secretase reduction in a mouse model of Alzheimer's disease.
Alzheimer Disease
Memapsin 2 (beta-secretase) as a therapeutic target.
Alzheimer Disease
Memapsin 2 (beta-secretase) cytosolic domain binds to the VHS domains of GGA1 and GGA2: implications on the endocytosis mechanism of memapsin 2.
Alzheimer Disease
Memapsin 2, a drug target for Alzheimer's disease.
Alzheimer Disease
Membrane topology of Alzheimer's disease-related presenilin 1. Evidence for the existence of a molecular species with a seven membrane-spanning and one membrane-embedded structure.
Alzheimer Disease
Membrane topology of gamma-secretase component PEN-2.
Alzheimer Disease
Membrane-Associated Effects of Glucocorticoid on BACE1 Upregulation and A? Generation: Involvement of Lipid Raft-Mediated CREB Activation.
Alzheimer Disease
Mental Disorders in Young Adults from Families with the Presenilin-1 Gene Mutation E280A in the Preclinical Stage of Alzheimer's Disease.
Alzheimer Disease
Meta-analysis of BACE1 gene rs638405 polymorphism and the risk of Alzheimer's disease in Caucasion and Asian population.
Alzheimer Disease
Mice expressing human mutant presenilin-1 exhibit decreased activation of NF-kappaB p50 in hippocampal neurons after injury.
Alzheimer Disease
Microglia and neuritic plaques in familial Alzheimer's disease induced by a new mutation of presenilin-1 gene. An ultrastructural study.
Alzheimer Disease
MicroRNA-149 is downregulated in Alzheimer's disease and inhibits ?-amyloid accumulation and ameliorates neuronal viability through targeting BACE1.
Alzheimer Disease
MicroRNA-195 downregulates Alzheimer's disease amyloid-? production by targeting BACE1.
Alzheimer Disease
Microsecond molecular dynamics simulation of A?42 and identification of a novel dual inhibitor of A?42 aggregation and BACE1 activity.
Alzheimer Disease
Microvesicles from cerebrospinal fluid of patients with Alzheimer's disease display reduced concentrations of tau and APP protein.
Alzheimer Disease
Mif1: a missing link between the unfolded protein response pathway and ER-associated protein degradation?
Alzheimer Disease
Mild oxidative stress induces redistribution of BACE1 in non-apoptotic conditions and promotes the amyloidogenic processing of Alzheimer's disease amyloid precursor protein.
Alzheimer Disease
MiR-124 acts as a target for Alzheimer's disease by regulating BACE1.
Alzheimer Disease
miR-124 downregulates BACE 1 and alters autophagy in APP/PS1 transgenic mice.
Alzheimer Disease
miR-15b represses BACE1 expression in sporadic Alzheimer's disease.
Alzheimer Disease
miR-16-5p and miR-19b-3p prevent amyloid ?-induced injury by targeting BACE1 in SH-SY5Y cells.
Alzheimer Disease
miR-186 in Alzheimer's disease: a big hope for a small RNA?
Alzheimer Disease
MiR-361-3p inhibits ?-amyloid accumulation and attenuates cognitive deficits through targeting BACE1 in Alzheimer's disease.
Alzheimer Disease
miRNA-31 Improves Cognition and Abolishes Amyloid-? Pathology by Targeting APP and BACE1 in an Animal Model of Alzheimer's Disease.
Alzheimer Disease
miRNA-Based Rapid Differentiation of Purified Neurons from hPSCs Advancestowards Quick Screening for Neuronal Disease Phenotypes In Vitro.
Alzheimer Disease
Missense mutation in exon 11 (Codon 378) of the presenilin-1 gene in a French family with early-onset Alzheimer's disease and transmission study by mismatch enhanced allele specific amplification. Mutations in brief no. 141. Online. besancon@rockefeller1.univ.lyon1.fr.
Alzheimer Disease
Missense mutations in the chromosome 14 familial Alzheimer's disease presenilin 1 gene.
Alzheimer Disease
Mitochondria-targeted catalase reduces abnormal APP processing, amyloid ? production and BACE1 in a mouse model of Alzheimer's disease: implications for neuroprotection and lifespan extension.
Alzheimer Disease
Mitochondrial function in fibroblasts with aging in culture and/or Alzheimer's disease.
Alzheimer Disease
MMP13 inhibition rescues cognitive decline in Alzheimer transgenic mice via BACE1 regulation.
Alzheimer Disease
Model peptides uncover the role of the ?-secretase transmembrane sequence in metal ion mediated oligomerization.
Alzheimer Disease
Modeling the tertiary structure of human cathepsin-E.
Alzheimer Disease
Moderate reduction of gamma-secretase attenuates amyloid burden and limits mechanism-based liabilities.
Alzheimer Disease
Modification of endoplasmic reticulum Ca2+ stores by select oxidants produces changes reminiscent of those in cells from patients with Alzheimer disease.
Alzheimer Disease
Modulation of BACE1 Activity by Chemically Modified Aptamers.
Alzheimer Disease
Modulation of gamma-secretase for the treatment of Alzheimer's disease.
Alzheimer Disease
Modulation of gamma-secretase reduces beta-amyloid deposition in a transgenic mouse model of Alzheimer's disease.
Alzheimer Disease
Modulation of in?vitro activity of zymogenic and mature recombinant human ?-secretase by dietary plants.
Alzheimer Disease
Modulation of the endoplasmic reticulum-mitochondria interface in Alzheimer's disease and related models.
Alzheimer Disease
Modulatory effect of acetyl-l-carnitine on amyloid precursor protein metabolism in hippocampal neurons.
Alzheimer Disease
Molecular analysis of the presenilin 1 (S182) gene in "sporadic" cases of Alzheimer's disease: identification and characterisation of unusual splice variants.
Alzheimer Disease
Molecular characterization and temporal expression profiling of presenilins in the developing porcine brain.
Alzheimer Disease
Molecular cloning and characterization of CALP/KChIP4, a novel EF-hand protein interacting with presenilin 2 and voltage-gated potassium channel subunit Kv4.
Alzheimer Disease
Molecular cloning and expression of the rat homologue of presenilin-1.
Alzheimer Disease
Molecular Docking and 3D Qsar Studies of C000000956 as a Potent Inhibitor of Bace-1.
Alzheimer Disease
Molecular Docking and Dynamic Simulation of AZD3293 and Solanezumab Effects Against BACE1 to Treat Alzheimer's Disease.
Alzheimer Disease
Molecular evidence of presenilin 1 mutation in familial early onset dementia.
Alzheimer Disease
Molecular Genetic Analysis of the APP, PSEN1, and PSEN2 Genes in Finnish Patients With Early-onset Alzheimer Disease and Frontotemporal Lobar Degeneration.
Alzheimer Disease
Molecular genetics of Alzheimer's disease.
Alzheimer Disease
Molecular genetics of Alzheimer's disease: presenilin 1 gene analysis in a cohort of patients from the PoznaÅ region.
Alzheimer Disease
Molecular Models of the Interface between Anterior Pharynx-Defective Protein 1 (APH-1) and Presenilin Involving GxxxG Motifs.
Alzheimer Disease
Monogenic determinants of familial Alzheimer's disease: presenilin-1 mutations.
Alzheimer Disease
Monogenic determinants of familial Alzheimer's disease: presenilin-2 mutations.
Alzheimer Disease
Morphological change by overexpression of D385A dominant negative presenilin 1 in human neuroblastoma SH-SY5Y cells.
Alzheimer Disease
Mouse brain proteomics establishes MDGA1 and CACHD1 as in vivo substrates of the Alzheimer protease BACE1.
Alzheimer Disease
Multifunctional iminochromene-2H-carboxamide derivatives containing different aminomethylene triazole with BACE1 inhibitory, neuroprotective and metal chelating properties targeting Alzheimer's disease.
Alzheimer Disease
Multimodal Imaging in a Patient With Alzheimer Disease and Parkinsonism Because of a Presenilin-1 Mutation.
Alzheimer Disease
Multipotent AChE and BACE-1 inhibitors for the treatment of Alzheimer's disease: Design, synthesis and bio-analysis of 7-amino-1,4-dihydro-2H-isoquilin-3-one derivates.
Alzheimer Disease
Multitarget Approach to Drug Candidates against Alzheimer's Disease Related to AChE, SERT, BACE1 and GSK3? Protein Targets.
Alzheimer Disease
Multitarget drug discovery for Alzheimer's disease: triazinones as BACE-1 and GSK-3? inhibitors.
Alzheimer Disease
Multiwell fluorometric and colorimetric microassays for the evaluation of beta-secretase (BACE-1) inhibitors.
Alzheimer Disease
Muscarinic agonists reduce tau phosphorylation in non-neuronal cells via GSK-3beta inhibition and in neurons.
Alzheimer Disease
Mutagenesis mapping of the presenilin 1 calcium leak conductance pore.
Alzheimer Disease
Mutant human presenilin 1 protects presenilin 1 null mouse against embryonic lethality and elevates Abeta1-42/43 expression.
Alzheimer Disease
Mutant presenilin (A260V) affects Rab8 in PC12D cell.
Alzheimer Disease
Mutant presenilin 1 expression in excitatory neurons impairs enrichment-mediated phenotypes of adult hippocampal progenitor cells.
Alzheimer Disease
Mutant presenilin 1 increases the expression and activity of BACE1.
Alzheimer Disease
Mutant presenilin 1 increases the levels of Alzheimer amyloid beta-peptide Abeta42 in late compartments of the constitutive secretory pathway.
Alzheimer Disease
Mutant presenilin 1 proteins induce cell death and reduce tau-dependent processes outgrowth.
Alzheimer Disease
Mutant presenilin-1 deregulated peripheral immunity exacerbates alzheimer-like pathology.
Alzheimer Disease
Mutant presenilin-1 induces apoptosis and downregulates Akt/PKB.
Alzheimer Disease
Mutant presenilins specifically elevate the levels of the 42 residue beta-amyloid peptide in vivo: evidence for augmentation of a 42-specific gamma secretase.
Alzheimer Disease
Mutation profile of APP, PSEN1, and PSEN2 in Chinese familial Alzheimer's disease.
Alzheimer Disease
Mutational analysis in early-onset familial Alzheimer's disease in Mainland China.
Alzheimer Disease
Mutational analysis in early-onset familial dementia in the Japanese population. The role of PSEN1 and MAPT R406W mutations.
Alzheimer Disease
Mutations in amyloid precursor protein and presenilin-1 genes increase the basal oxidative stress in murine neuronal cells and lead to increased sensitivity to oxidative stress mediated by amyloid beta-peptide (1-42), HO and kainic acid: implications for Alzheimer's disease.
Alzheimer Disease
Mutations in presenilin 1, presenilin 2 and amyloid precursor protein genes in patients with early-onset Alzheimer's disease in Poland.
Alzheimer Disease
Mutations in progranulin explain atypical phenotypes with variants in MAPT.
Alzheimer Disease
Mutations in the transmembrane domain of APP altering gamma-secretase specificity.
Alzheimer Disease
Myeloproliferative disease in mice with reduced presenilin gene dosage: effect of gamma-secretase blockage.
Alzheimer Disease
N-glycosylation of human nicastrin is required for interaction with the lectins from the secretory pathway calnexin and ERGIC-53.
Alzheimer Disease
N-Substituted carbazolyloxyacetic acids modulate Alzheimer associated gamma-secretase.
Alzheimer Disease
N141I mutant presenilin-2 gene enhances neuronal cell death and decreases bcl-2 expression.
Alzheimer Disease
NACP/alpha-synuclein, NAC, and beta-amyloid pathology of familial Alzheimer's disease with the E184D presenilin-1 mutation: a clinicopathological study of two autopsy cases.
Alzheimer Disease
Nanolipidic particles improve the bioavailability and alpha-secretase inducing ability of epigallocatechin-3-gallate (EGCG) for the treatment of Alzheimer's disease.
Alzheimer Disease
Natural antisense transcripts of Alzheimer's disease associated genes.
Alzheimer Disease
Natural Compounds with Anti-BACE1 Activity as Promising Therapeutic Drugs for Treating Alzheimer's Disease.
Alzheimer Disease
Natural Products based P-glycoprotein Activators for Improved ?-amyloid Clearance in Alzheimer's Disease: An in silico Approach.
Alzheimer Disease
Nav?2 knockdown improves cognition in APP/PS1 mice by partially inhibiting seizures and APP amyloid processing.
Alzheimer Disease
Neprilysin activity and expression are controlled by nicastrin.
Alzheimer Disease
Neurite-like structures induced by mevalonate pathway blockade are due to the stability of cell adhesion foci and are enhanced by the presence of APP.
Alzheimer Disease
Neuro-protective effects of aloperine in an Alzheimer's disease cellular model.
Alzheimer Disease
Neurodegeneration in Alzheimer disease: role of amyloid precursor protein and presenilin 1 intracellular signaling.
Alzheimer Disease
Neurogranin and BACE1 in CSF as Potential Biomarkers Differentiating Depression with Cognitive Deficits from Early Alzheimer's Disease: A Pilot Study.
Alzheimer Disease
Neurological dysfunctions associated with altered BACE1-dependent Neuregulin-1 signaling.
Alzheimer Disease
Neuronal and nonneuronal quantitative BACE immunocytochemical expression in the entorhinohippocampal and frontal regions in Alzheimer's disease.
Alzheimer Disease
Neuronal expression and intracellular localization of presenilins in normal and Alzheimer disease brains.
Alzheimer Disease
Neuronal human BACE1 knockin induces systemic diabetes in mice.
Alzheimer Disease
Neuronal localization of presenilin-1 and association with amyloid plaques and neurofibrillary tangles in Alzheimer's disease.
Alzheimer Disease
Neuronal Migration and Neurodegeneration: 2 Sides of the Same Coin.
Alzheimer Disease
Neuronal protein trafficking associated with Alzheimer disease: From APP and BACE1 to glutamate receptors.
Alzheimer Disease
Neuronal RNA oxidation is a prominent feature of familial Alzheimer's disease.
Alzheimer Disease
Neuropathological and clinical phenotype of an Italian Alzheimer family with M239V mutation of presenilin 2 gene.
Alzheimer Disease
Neuropathological, biochemical and genetic alterations in AD.
Alzheimer Disease
Neuropathology and biochemistry of early onset familial Alzheimer's disease caused by presenilin-1 missense mutation Thr116Asn.
Alzheimer Disease
Neuropathology of the recessive A673V APP mutation: Alzheimer disease with distinctive features.
Alzheimer Disease
Neuroprotective mechanism conferred by 17beta-estradiol on the biochemical basis of Alzheimer's disease.
Alzheimer Disease
Neuropsychological functions in variant Alzheimer's disease with spastic paraparesis.
Alzheimer Disease
Neuropsychological profile of a large kindred with familial Alzheimer's disease caused by the E280A single presenilin-1 mutation.
Alzheimer Disease
Neuropsychological profiles of familial Alzheimer's disease associated with mutations in the presenilin 1 and amyloid precursor protein genes.
Alzheimer Disease
Neuropsychological study of familial Alzheimer's disease caused by mutation E280A in the presenilin 1 gene.
Alzheimer Disease
Neurotoxic mechanisms caused by the Alzheimer's disease-linked Swedish amyloid precursor protein mutation: oxidative stress, caspases, and the JNK pathway.
Alzheimer Disease
Neurotrophic factors [activity-dependent neurotrophic factor (ADNF) and basic fibroblast growth factor (bFGF)] interrupt excitotoxic neurodegenerative cascades promoted by a PS1 mutation.
Alzheimer Disease
New 1,2,3,4-tetrahydroisoquinoline derivatives as modulators of proteolytic cleavage of amyloid precursor proteins.
Alzheimer Disease
New 3,5-dimethylorsellinic acid-based meroterpenoids with BACE1 and AchE inhibitory activities from Aspergillus terreus.
Alzheimer Disease
New aminoimidazoles as ?-secretase (BACE-1) inhibitors showing amyloid-? (A?) lowering in brain.
Alzheimer Disease
New BACE1 Chimeric Peptide Inhibitors Selectively Prevent A?PP-? Cleavage Decreasing Amyloid-? Production and Accumulation in Alzheimer's Disease Models.
Alzheimer Disease
New developments in mild cognitive impairment and Alzheimer's disease.
Alzheimer Disease
New mutation in the PSEN1 (E120G) gene associated with early onset Alzheimer's disease.
Alzheimer Disease
New N(4)-substituted piperazine naphthamide derivatives as BACE-1 inhibitors.
Alzheimer Disease
New presenilin 1 mutation with Alzheimer disease and Lewy bodies.
Alzheimer Disease
NF-E2-related factor 2 activation boosts antioxidant defenses and ameliorates inflammatory and amyloid properties in human Presenilin-1 mutated Alzheimer's disease astrocytes.
Alzheimer Disease
NF{kappa}B-dependent Control of BACE1 Promoter Transactivation by A{beta}42.
Alzheimer Disease
Nicastrin binds to membrane-tethered Notch.
Alzheimer Disease
Nicastrin Is Dispensable for {gamma}-Secretase Protease Activity in the Presence of Specific Presenilin Mutations.
Alzheimer Disease
Nicastrin is required for assembly of presenilin/gamma-secretase complexes to mediate Notch signaling and for processing and trafficking of beta-amyloid precursor protein in mammals.
Alzheimer Disease
Nicastrin, presenilin, APH-1, and PEN-2 form active gamma-secretase complexes in mitochondria.
Alzheimer Disease
Nitrosylation of Vesicular Transporters in Brain of Amyloid Precursor Protein/Presenilin 1 Double Transgenic Mice.
Alzheimer Disease
No association between a polymorphism in the presenilin 1 gene and dementia with Lewy bodies.
Alzheimer Disease
No association between a presenilin 1 polymorphism and Alzheimer disease.
Alzheimer Disease
No association between an intronic polymorphism in the presenilin-1 gene and Alzheimer disease in a German population.
Alzheimer Disease
No association between an intronic polymorphism in the presenilin-1 gene and Alzheimer disease in a Tunisian population.
Alzheimer Disease
No association between an intronic polymorphism in the presenilin-1 gene and Alzheimer's disease.
Alzheimer Disease
No association between presenilin 1 (PS1) intronic polymorphism and sporadic Alzheimer's disease in Koreans.
Alzheimer Disease
No association between the intronic presenilin 1 polymorphism and Alzheimer's disease in the Chinese population.
Alzheimer Disease
No association between the intronic presenilin-1 polymorphism and Alzheimer's disease in clinic and population-based samples.
Alzheimer Disease
No association of presenilin-1 intronic polymorphism and Alzheimer's disease in Australia.
Alzheimer Disease
No association of spastic paraparesis genes in PSEN1 Alzheimer's disease with spastic paraparesis.
Alzheimer Disease
No association of the -48CT polymorphism of the presenilin 1 gene with Alzheimer disease in a late-onset sporadic population.
Alzheimer Disease
No association or linkage between an intronic polymorphism of presenilin-1 and sporadic or late-onset familial Alzheimer disease.
Alzheimer Disease
No detected mutations in the genes for the amyloid precursor protein and presenilins 1 and 2 in a swiss early-onset Alzheimer's disease family with a dominant mode of inheritance.
Alzheimer Disease
No replication of genetic association between candidate polymorphisms and Alzheimer's disease.
Alzheimer Disease
Non-proteolytic effect of beta-site APP-cleaving enzyme 1 (BACE1) on sodium channel function.
Alzheimer Disease
Normal distribution of presenilin-1 and nicastrin in skeletal muscle and the differential responses of these proteins after denervation.
Alzheimer Disease
Normal proteolytic processing of the presenilins.
Alzheimer Disease
Nose-to-brain delivery of BACE1 siRNA loaded in solid lipid nanoparticles for Alzheimer's therapy.
Alzheimer Disease
Notch is expressed in adult brain, is coexpressed with presenilin-1, and is altered in Alzheimer disease.
Alzheimer Disease
Notch-1 activation by familial Alzheimer's disease (FAD)-linked mutant forms of presenilin-1.
Alzheimer Disease
Notch/gamma-secretase inhibition turns proliferative cells in intestinal crypts and adenomas into goblet cells.
Alzheimer Disease
Novel 'inflammatory plaque' pathology in presenilin-1 Alzheimer's disease.
Alzheimer Disease
Novel brain 14-3-3 interacting proteins involved in neurodegenerative disease.
Alzheimer Disease
Novel insertional presenilin 1 mutation causing Alzheimer disease with spastic paraparesis.
Alzheimer Disease
Novel intronic polymorphisms in the presenilin-2 gene and a case-control association study of Alzheimer's disease.
Alzheimer Disease
Novel orally active, dibenzazepinone-based gamma-secretase inhibitors.
Alzheimer Disease
Novel Plasma miRNAs as Biomarkers and Therapeutic Targets of Alzheimer's Disease at the Prodromal Stage.
Alzheimer Disease
Novel presenilin 1 mutation (Ile408Thr) in an Italian family with late-onset Alzheimer's disease.
Alzheimer Disease
Novel presenilin 1 mutation (p.F386I) in a Chinese family with early-onset Alzheimer's disease.
Alzheimer Disease
Novel presenilin 1 mutation (p.I83T) in Tunisian family with early-onset Alzheimer's disease.
Alzheimer Disease
Novel presenilin 1 mutation (p.Thr-Pro116-117Ser-Thr) in a Spanish family with early-onset Alzheimer's disease.
Alzheimer Disease
Novel presenilin 1 mutation (S170F) causing Alzheimer disease with Lewy bodies in the third decade of life.
Alzheimer Disease
Novel presenilin 1 mutation with profound neurofibrillary pathology in an indigenous Southern African family with early-onset Alzheimer's disease.
Alzheimer Disease
Novel presenilin 1 mutations associated with early onset of dementia in a family with both early-onset and late-onset Alzheimer disease.
Alzheimer Disease
Novel presenilin 1 variant (P117A) causing Alzheimer's disease in the fourth decade of life.
Alzheimer Disease
Novel presenilin-1 Y159F sequence variant associated with early-onset Alzheimer's disease.
Alzheimer Disease
Novel Presenilins mutations within Moroccan patients with Early Onset Alzheimer's Disease.
Alzheimer Disease
Novel PSEN1 mutations (H214N and R220P) associated with familial Alzheimer's disease identified by targeted exome sequencing.
Alzheimer Disease
Novel PSEN1 p.Gly417Ala mutation in a Korean patient with early-onset Alzheimer's disease with parkinsonism.
Alzheimer Disease
Novel small molecule therapeutic agents for Alzheimer disease: Focusing on BACE1 and multi-target directed ligands.
Alzheimer Disease
Novel {gamma}-secretase inhibitors uncover a common nucleotide-binding site in JAK3, SIRT2, and PS1.
Alzheimer Disease
NRF2/ARE pathway negatively regulates BACE1 expression and ameliorates cognitive deficits in mouse Alzheimer's models.
Alzheimer Disease
NSAID-derived gamma-secretase modulators. Part III: Membrane anchoring.
Alzheimer Disease
Octapeptide repeat insertions in the prion protein gene and early onset dementia.
Alzheimer Disease
Oleic acid and linoleic acid from Tenebrio molitor larvae inhibit BACE1 activity in vitro: molecular docking studies.
Alzheimer Disease
One novel presenilin-1 gene mutation in a Chinese pedigree of familial Alzheimer's disease.
Alzheimer Disease
Optimisation of BACE1 inhibition of tripartite structures by modification of membrane anchors, spacers and pharmacophores - development of potential agents for the treatment of Alzheimer's disease.
Alzheimer Disease
Optimization and biological evaluation of imidazopyridine derivatives as a novel scaffold for ?-secretase modulators with oral efficacy against cognitive deficits in Alzheimer's disease model mice.
Alzheimer Disease
Oral administration of a potent and selective non-peptidic BACE-1 inhibitor decreases beta-cleavage of amyloid precursor protein and amyloid-beta production in vivo.
Alzheimer Disease
Oral treatment with a gamma-secretase inhibitor improves long-term potentiation in a mouse model of Alzheimer's disease.
Alzheimer Disease
Origin of the PSEN1 E280A mutation causing early-onset Alzheimer's disease.
Alzheimer Disease
Overactive BRCA1 Affects Presenilin 1 in Induced Pluripotent Stem Cell-Derived Neurons in Alzheimer's Disease.
Alzheimer Disease
Overexpression in neurons of human presenilin-1 or a presenilin-1 familial Alzheimer disease mutant does not enhance apoptosis.
Alzheimer Disease
Overexpression of presenilin-2 enhances apoptotic death of cultured cortical neurons.
Alzheimer Disease
Overexpression of wild type but not an FAD mutant presenilin-1 promotes neurogenesis in the hippocampus of adult mice.
Alzheimer Disease
Oxidative stress activates a positive feedback between the gamma- and beta-secretase cleavages of the beta-amyloid precursor protein.
Alzheimer Disease
Oxidative stress in synaptosomal proteins from mutant presenilin-1 knock-in mice: implications for familial Alzheimer's disease.
Alzheimer Disease
Oxidative stress increases BACE1 protein levels through activation of the PKR-eIF2? pathway.
Alzheimer Disease
Oxidative stress potentiates BACE1 gene expression and Abeta generation.
Alzheimer Disease
p300 activation by Presenilin 1 but not by its M146L mutant.
Alzheimer Disease
p35/cdk5 binds and phosphorylates beta-catenin and regulates beta-catenin/presenilin-1 interaction.
Alzheimer Disease
p53-dependent control of transactivation of the Pen2 promoter by presenilins.
Alzheimer Disease
p53-independent NOXA induction overcomes apoptotic resistance of malignant melanomas.
Alzheimer Disease
Palmitoylation of the C-terminal fragment of p75(NTR) regulates death signaling and is required for subsequent cleavage by gamma-secretase.
Alzheimer Disease
PAMP and PARL, two novel putative metalloproteases interacting with the COOH-terminus of Presenilin-1 and -2.
Alzheimer Disease
Partial BACE1 reduction in a Down syndrome mouse model blocks Alzheimer-related endosomal anomalies and cholinergic neurodegeneration: role of APP-CTF.
Alzheimer Disease
Partial loss of presenilins causes seborrheic keratosis and autoimmune disease in mice.
Alzheimer Disease
Partial purification and characterization of gamma-secretase from post-mortem human brain.
Alzheimer Disease
Partial reduction of BACE1 has dramatic effects on Alzheimer plaque and synaptic pathology in APP Transgenic Mice.
Alzheimer Disease
Partial reduction of BACE1 improves synaptic plasticity, recent and remote memories in Alzheimer's disease transgenic mice.
Alzheimer Disease
Partial, Rather than Full, BACE1 Inhibition May Be a Better Therapeutic Strategy for Alzheimer's Disease Due to Effects of Complete Loss of BACE1 Activity on Adult Hippocampal Neurogenesis.
Alzheimer Disease
Participation of Amyloid and Tau Protein in Post-Ischemic Neurodegeneration of the Hippocampus of a Nature Identical to Alzheimer's Disease.
Alzheimer Disease
Pathogenic presenilin 1 mutations (P436S & I143F) in early-onset Alzheimer's disease in the UK. Mutations in brief no. 223. Online.
Alzheimer Disease
Pathogenic PSEN1 Thr119Ile Mutation in Two Korean Patients with Early-Onset Alzheimer's Disease.
Alzheimer Disease
Pathological activity of familial Alzheimer's disease-associated mutant presenilin can be executed by six different gamma-secretase complexes.
Alzheimer Disease
Pathological and physiological functions of presenilins.
Alzheimer Disease
Pathological manifestation of the induced pluripotent stem cell-derived cortical neurons from an early-onset Alzheimer's disease patient carrying a presenilin-1 mutation (S170F).
Alzheimer Disease
Pathology of early-onset Alzheimer's disease cases bearing the Thr113-114ins presenilin-1 mutation.
Alzheimer Disease
Pathophysiological subtypes of Alzheimer's disease based on cerebrospinal fluid proteomics.
Alzheimer Disease
PCSK9 is Present in Human Cerebrospinal Fluid and is Maintained at Remarkably Constant Concentrations Throughout the Course of the Day.
Alzheimer Disease
PCSK9 is required for the disposal of non-acetylated intermediates of the nascent membrane protein BACE1.
Alzheimer Disease
PEDF Maintains RPE Function by Inhibiting VEGF-R2 Signaling Through {gamma}-Secretase.
Alzheimer Disease
Pen2 and presenilin-1 modulate the dynamic equilibrium of presenilin-1 and presenilin-2 gamma-secretase complexes.
Alzheimer Disease
PEN2 is not a genetic risk factor for Alzheimer's disease in a large family sample.
Alzheimer Disease
Peptide EphB2/CTF2 Generated by the gamma-secretase processing of EphB2 receptor promotes tyrosine phosphorylation and cell surface localization of N-methyl-D-aspartate receptors.
Alzheimer Disease
Peptides of presenilin-1 bind the amyloid precursor protein ectodomain and offer a novel and specific therapeutic approach to reduce ß-amyloid in Alzheimer's disease.
Alzheimer Disease
Peripheral Activity and Central Substrates of BACE1: Therapeutic Implications for Alzheimer's Disease.
Alzheimer Disease
PERK mediates eIF2? phosphorylation responsible for BACE1 elevation, CREB dysfunction and neurodegeneration in a mouse model of Alzheimer's disease.
Alzheimer Disease
PET amyloid ligand [11C]PIB uptake shows predominantly striatal increase in variant Alzheimer's disease.
Alzheimer Disease
pH-Dependent Population Shift Regulates BACE1 Activity and Inhibition.
Alzheimer Disease
Pharmacodynamics of atabecestat (JNJ-54861911), an oral BACE1 inhibitor in patients with early Alzheimer's disease: randomized, double-blind, placebo-controlled study.
Alzheimer Disease
Pharmacological Inhibition of BACE1 Impairs Synaptic Plasticity and Cognitive Functions.
Alzheimer Disease
Pharmacological knock-down of the presenilin 1 heterodimer by a novel gamma -secretase inhibitor: implications for presenilin biology.
Alzheimer Disease
Phase 2 safety trial targeting amyloid beta production with a gamma-secretase inhibitor in Alzheimer disease.
Alzheimer Disease
Phenotypic analysis of images of zebrafish treated with Alzheimer's gamma-secretase inhibitors.
Alzheimer Disease
Phenotypic Profile of Early-Onset Familial Alzheimer's Disease Caused by Presenilin-1 E280A Mutation.
Alzheimer Disease
Phenotypic Variability in Autosomal Dominant Familial Alzheimer Disease due to the S170F Mutation of Presenilin-1.
Alzheimer Disease
Phosphorylation of presenilin-2 regulates its cleavage by caspases and retards progression of apoptosis.
Alzheimer Disease
Phosphorylation of the translation initiation factor eIF2alpha increases BACE1 levels and promotes amyloidogenesis.
Alzheimer Disease
Phosphorylation, subcellular localization, and membrane orientation of the Alzheimer's disease-associated presenilins.
Alzheimer Disease
Photoactivated gamma-secretase inhibitors directed to the active site covalently label presenilin 1.
Alzheimer Disease
Physical evidence supporting a ribosomal shunting mechanism of translation initiation for BACE1 mRNA.
Alzheimer Disease
Physiological Control of Nitric Oxide on neuronal BACE1 Translation by Heme-Regulated Eif2-alpha Kinase HRI Induces Synaptogenesis.
Alzheimer Disease
Physiological Functions of the ?-Site Amyloid Precursor Protein Cleaving Enzyme 1 and 2.
Alzheimer Disease
Physiological functions of the amyloid precursor protein secretases ADAM10, BACE1, and Presenilin.
Alzheimer Disease
Physiologically generated presenilin 1 lacking exon 8 fails to rescue brain PS1-/- phenotype and forms complexes with wildtype PS1 and nicastrin.
Alzheimer Disease
Pick bodies in a family with presenilin-1 Alzheimer's disease.
Alzheimer Disease
Piperazinyl pyrimidine derivatives as potent gamma-secretase modulators.
Alzheimer Disease
Plasma ?-secretase1 concentrations correlate with basal forebrain atrophy and neurodegeneration in cognitively healthy individuals at risk for AD.
Alzheimer Disease
Plasma Lipids as Biomarkers for Alzheimer's Disease: A Systematic Review.
Alzheimer Disease
Plasma long non-coding RNA BACE1 as a novel biomarker for diagnosis of Alzheimer disease.
Alzheimer Disease
Plasma neurofilament light chain in the presenilin 1 E280A autosomal dominant Alzheimer's disease kindred: a cross-sectional and longitudinal cohort study.
Alzheimer Disease
Platelet amyloid precursor protein processing: a bio-marker for Alzheimer's disease.
Alzheimer Disease
Polymorphism of the regulatory region of the presenilin-2 gene in sporadic Alzheimer's disease: a case-control study.
Alzheimer Disease
Polymorphisms in the presenilin 1 and presenilin 2 genes and risk for sporadic Alzheimer's disease.
Alzheimer Disease
Polypharmacology of Berberine Based on Multi-Target Binding Motifs.
Alzheimer Disease
Population density analysis for determining the protonation state of the catalytic dyad in BACE1-tertiary carbinamine-based inhibitor complex.
Alzheimer Disease
Positional effects of presenilin-1 mutations on tau phosphorylation in cortical plaques.
Alzheimer Disease
Post-Translational Modifications of BACE1 in Alzheimer's Disease.
Alzheimer Disease
Post-translational regulation of the ?-secretase BACE1.
Alzheimer Disease
Posterior Accumulation of Tau and Concordant Hypometabolism in an Early-Onset Alzheimer's Disease Patient with Presenilin-1 Mutation.
Alzheimer Disease
Postsynaptic Target Specific Synaptic Dysfunctions in the CA3 Area of BACE1 Knockout Mice.
Alzheimer Disease
Posttranslational modification and plasma membrane localization of the Drosophila melanogaster presenilin.
Alzheimer Disease
Potential of Pueraria tuberosa (Willd.) DC. to rescue cognitive decline associated with BACE1 protein of Alzheimer's disease on Drosophila model: An integrated molecular modeling and in vivo approach.
Alzheimer Disease
Pre-dementia clinical stages in presenilin 1 E280A familial early-onset Alzheimer's disease: a retrospective cohort study.
Alzheimer Disease
Precuneus Failures in Subjects of the PSEN1 E280A Family at Risk of Developing Alzheimer's Disease Detected Using Quantitative Electroencephalography.
Alzheimer Disease
Predicting memapsin 2 (?-secretase) hydrolytic activity.
Alzheimer Disease
Preparation and biological evaluation of BACE1 inhibitors: Leveraging trans-cyclopropyl moieties as ligand efficient conformational constraints.
Alzheimer Disease
Preparation and biological evaluation of conformationally constrained BACE1 inhibitors.
Alzheimer Disease
Presenilin 1 and APP Gene Mutations in Early-Onset AD Families from a Southeast Region of China.
Alzheimer Disease
Presenilin 1 and cadherins: stabilization of cell-cell adhesion and proteolysis-dependent regulation of transcription.
Alzheimer Disease
Presenilin 1 associates with glycogen synthase kinase-3beta and its substrate tau.
Alzheimer Disease
Presenilin 1 controls gamma-secretase processing of amyloid precursor protein in pre-golgi compartments of hippocampal neurons.
Alzheimer Disease
Presenilin 1 deficiency suppresses autophagy in human neural stem cells through reducing ?-secretase-independent ERK/CREB signaling.
Alzheimer Disease
Presenilin 1 facilitates the constitutive turnover of beta-catenin: differential activity of Alzheimer's disease-linked PS1 mutants in the beta-catenin-signaling pathway.
Alzheimer Disease
Presenilin 1 familial Alzheimer's disease mutation leads to defective associative learning and impaired adult neurogenesis.
Alzheimer Disease
Presenilin 1 gene mutation (M139I) in a patient with an early-onset Alzheimer's disease: clinical characteristics and genetic identification.
Alzheimer Disease
Presenilin 1 Gene Mutation (M139V) in a German Family with Early-Onset Alzheimer's Disease: A Case Report.
Alzheimer Disease
Presenilin 1 gene silencing by S-adenosylmethionine: a treatment for Alzheimer disease?
Alzheimer Disease
Presenilin 1 immunostaining using well-characterized antibodies in human tissues.
Alzheimer Disease
Presenilin 1 interacts with acetylcholinesterase and alters its enzymatic activity and glycosylation.
Alzheimer Disease
Presenilin 1 intronic polymorphism in sporadic Alzheimer's disease in a Northern Chinese population.
Alzheimer Disease
Presenilin 1 intronic polymorphism is not associated with Alzheimer type neuropathological changes or sporadic Alzheimer's disease.
Alzheimer Disease
Presenilin 1 is essential for cardiac morphogenesis.
Alzheimer Disease
Presenilin 1 is involved in maturation and trafficking of N-cadherin to the plasma membrane.
Alzheimer Disease
Presenilin 1 is required for Notch1 and DII1 expression in the paraxial mesoderm.
Alzheimer Disease
Presenilin 1 Maintains Lysosomal Ca(2+) Homeostasis via TRPML1 by Regulating vATPase-Mediated Lysosome Acidification.
Alzheimer Disease
Presenilin 1 mediates retinoic acid-induced differentiation of SH-SY5Y cells through facilitation of Wnt signaling.
Alzheimer Disease
Presenilin 1 Met146Leu variant due to an A --> T transversion in an early-onset familial Alzheimer's disease pedigree from Argentina.
Alzheimer Disease
Presenilin 1 mRNA expression in hippocampi of sporadic Alzheimer's disease patients.
Alzheimer Disease
Presenilin 1 mutation decreases both calcium and contractile responses in cerebral arteries.
Alzheimer Disease
Presenilin 1 mutation in an african american family presenting with atypical Alzheimer dementia.
Alzheimer Disease
PRESENILIN 1 Mutations Causing Early-Onset Familial Alzheimer's Disease or Familial Acne Inversa Differ in Their Effects on Genes Facilitating Energy Metabolism and Signal Transduction.
Alzheimer Disease
Presenilin 1 mutations in Polish families with early-onset Alzheimer's disease.
Alzheimer Disease
Presenilin 1 mutations increase amyloid precursor protein production and proteolysis in Xenopus laevis oocytes.
Alzheimer Disease
Presenilin 1 mutations linked to familial Alzheimer's disease increase the intracellular levels of amyloid beta-protein 1-42 and its N-terminally truncated variant(s) which are generated at distinct sites.
Alzheimer Disease
Presenilin 1 overexpressions in Chinese hamster ovary (CHO) cells decreases the phosphorylation of retinoblastoma protein: relevance for neurodegeneration.
Alzheimer Disease
Presenilin 1 polymorphism associated with Alzheimer's disease in apolipoprotein E4 carriers.
Alzheimer Disease
Presenilin 1 promotes trypsin-induced neuroprotection via the PAR2/ERK signaling pathway. Effects of presenilin 1 FAD mutations.
Alzheimer Disease
Presenilin 1 regulates beta-catenin-mediated transcription in a glycogen synthase kinase-3-independent fashion.
Alzheimer Disease
Presenilin 1 regulates epidermal growth factor receptor turnover and signaling in the endosomal-lysosomal pathway.
Alzheimer Disease
Presenilin 1 Regulates Membrane Homeostatic Pathways that are Dysregulated in Alzheimer's Disease.
Alzheimer Disease
Presenilin 1 Regulates NF-?B Activation via Association with Breakpoint Cluster Region and Casein Kinase II.
Alzheimer Disease
Presenilin 1 regulates pharmacologically distinct gamma -secretase activities. Implications for the role of presenilin in gamma -secretase cleavage.
Alzheimer Disease
Presenilin 1 Regulates [Ca2+]i and Mitochondria/ER Interaction in Cultured Rat Hippocampal Neurons.
Alzheimer Disease
Presenilin 1 stabilizes the C-terminal fragment of the amyloid precursor protein independently of gamma-secretase activity.
Alzheimer Disease
Presenilin 1 suppresses the function of c-Jun homodimers via interaction with QM/Jif-1.
Alzheimer Disease
Presenilin 1 transgene addition to amyloid precursor protein overexpressing transgenic rats increases amyloid beta 42 levels and results in loss of memory retention.
Alzheimer Disease
Presenilin 2 deficiency causes a mild pulmonary phenotype and no changes in amyloid precursor protein processing but enhances the embryonic lethal phenotype of presenilin 1 deficiency.
Alzheimer Disease
Presenilin 2 expression in neuronal cells: induction during differentiation of embryonic carcinoma cells.
Alzheimer Disease
Presenilin 2 is secreted in mouse primary neurons: a release enhanced by apoptosis.
Alzheimer Disease
Presenilin 2 mutation accelerates the onset of impairment in trace eyeblink conditioning in a mouse model of Alzheimer's disease overexpressing human mutant amyloid precursor protein.
Alzheimer Disease
Presenilin 2 mutation R71W in an Italian early-onset sporadic Alzheimer's disease case.
Alzheimer Disease
Presenilin affects arm/beta-catenin localization and function in Drosophila.
Alzheimer Disease
Presenilin dependence of phospholipase C and protein kinase C signaling.
Alzheimer Disease
Presenilin E318G variant and Alzheimer's disease risk: the Cache County study.
Alzheimer Disease
Presenilin endoproteolysis mediated by an aspartyl protease activity pharmacologically distinct from gamma-secretase.
Alzheimer Disease
Presenilin function in APP processing.
Alzheimer Disease
Presenilin function: connections to Alzheimer's disease and signal transduction.
Alzheimer Disease
Presenilin I expression in yeast lowers secretion of the amyloid precursor protein.
Alzheimer Disease
Presenilin mediates neuroprotective functions of ephrinB and brain-derived neurotrophic factor and regulates ligand-induced internalization and metabolism of EphB2 and TrkB receptors.
Alzheimer Disease
Presenilin mutations line up along transmembrane alpha-helices.
Alzheimer Disease
Presenilin mutations linked to familial Alzheimer's disease reduce endoplasmic reticulum and Golgi apparatus calcium levels.
Alzheimer Disease
Presenilin transgenic mice as models of Alzheimer's disease.
Alzheimer Disease
Presenilin-1 280Glu-->Ala Mutation Alters C-Terminal APP Processing Yielding Longer Abeta Peptides: Implications for Alzheimer's Disease.
Alzheimer Disease
Presenilin-1 adopts pathogenic conformation in normal aging and in sporadic Alzheimer's disease.
Alzheimer Disease
Presenilin-1 and -2 are molecular targets for gamma-secretase inhibitors.
Alzheimer Disease
Presenilin-1 and the amyloid precursor protein are transported bidirectionally in the sciatic nerve of adult rat.
Alzheimer Disease
Presenilin-1 binds cytoplasmic epithelial cadherin, inhibits cadherin/p120 association, and regulates stability and function of the cadherin/catenin adhesion complex.
Alzheimer Disease
Presenilin-1 but not amyloid precursor protein mutations present in mouse models of Alzheimer's disease attenuate the response of cultured cells to ?-secretase modulators regardless of their potency and structure.
Alzheimer Disease
Presenilin-1 C410Y Alzheimer disease plaques contain synaptic proteins.
Alzheimer Disease
Presenilin-1 controls the growth and differentiation of endothelial progenitor cells through its beta-catenin-binding region.
Alzheimer Disease
Presenilin-1 deficiency impairs glutamate-evoked intracellular calcium responses in neurons.
Alzheimer Disease
Presenilin-1 deficiency leads to loss of Cajal-Retzius neurons and cortical dysplasia similar to human type 2 lissencephaly.
Alzheimer Disease
Presenilin-1 Delta E9 Mutant Induces STIM1-Driven Store-Operated Calcium Channel Hyperactivation in Hippocampal Neurons.
Alzheimer Disease
Presenilin-1 differentially facilitates endoproteolysis of the beta-amyloid precursor protein and Notch.
Alzheimer Disease
Presenilin-1 exists in the axoplasm fraction in the brains of aged Down's syndrome subjects and non-demented individuals.
Alzheimer Disease
Presenilin-1 expression in Pick's disease.
Alzheimer Disease
Presenilin-1 familial Alzheimer's disease mutation alters hippocampal neurogenesis and memory function in CCL2 null mice.
Alzheimer Disease
Presenilin-1 gene intronic polymorphism and late-onset Alzheimer's disease.
Alzheimer Disease
Presenilin-1 gene intronic polymorphism in sporadic and familial Alzheimer's disease.
Alzheimer Disease
Presenilin-1 immunoreactivity is localized intracellularly in Alzheimer's disease brain, but not detected in amyloid plaques.
Alzheimer Disease
Presenilin-1 in late-onset depressive disorder.
Alzheimer Disease
Presenilin-1 intron 8 polymorphism is not associated with autopsy-confirmed late-onset Alzheimer's disease.
Alzheimer Disease
Presenilin-1 is associated with Alzheimer's disease amyloid.
Alzheimer Disease
Presenilin-1 is processed into two major cleavage products in neuronal cell lines.
Alzheimer Disease
Presenilin-1 Knockin Mice Reveal Loss-of-Function Mechanism for Familial Alzheimer's Disease.
Alzheimer Disease
Presenilin-1 mutation activates the signaling pathway of caspase-4 in endoplasmic reticulum stress-induced apoptosis.
Alzheimer Disease
Presenilin-1 mutation alters NGF-induced neurite outgrowth, calcium homeostasis, and transcription factor (AP-1) activation in PC12 cells.
Alzheimer Disease
Presenilin-1 mutation Alzheimer's disease: a genetic epilepsy syndrome?
Alzheimer Disease
Presenilin-1 mutation E318G and familial Alzheimer's disease in the Italian population.
Alzheimer Disease
Presenilin-1 mutation impairs cholinergic modulation of synaptic plasticity and suppresses NMDA currents in hippocampus slices.
Alzheimer Disease
Presenilin-1 mutation increases neuronal vulnerability to focal ischemia in vivo and to hypoxia and glucose deprivation in cell culture: involvement of perturbed calcium homeostasis.
Alzheimer Disease
Presenilin-1 mutation is associated with a hippocampus defect in alzheimer's disease: Meta-Analysis for neuroimaging research.
Alzheimer Disease
Presenilin-1 mutation L271V results in altered exon 8 splicing and Alzheimer's disease with non-cored plaques and no neuritic dystrophy.
Alzheimer Disease
Presenilin-1 mutations alter K+ currents in the human neuroblastoma cell line, SH-SY5Y.
Alzheimer Disease
Presenilin-1 mutations and Alzheimer's disease.
Alzheimer Disease
Presenilin-1 mutations associated with familial Alzheimer's disease do not disrupt protein transport from the endoplasmic reticulum to the Golgi apparatus.
Alzheimer Disease
Presenilin-1 mutations downregulate the signalling pathway of the unfolded-protein response.
Alzheimer Disease
Presenilin-1 mutations in Alzheimer's disease.
Alzheimer Disease
Presenilin-1 Mutations in Alzheimer's Disease: An Update on Genotype-Phenotype Relationships.
Alzheimer Disease
Presenilin-1 mutations increase levels of ryanodine receptors and calcium release in PC12 cells and cortical neurons.
Alzheimer Disease
Presenilin-1 mutations of leucine 166 equally affect the generation of the Notch and APP intracellular domains independent of their effect on Abeta 42 production.
Alzheimer Disease
Presenilin-1 mutations sensitize neurons to DNA damage-induced death by a mechanism involving perturbed calcium homeostasis and activation of calpains and caspase-12.
Alzheimer Disease
Presenilin-1 P264L knock-in mutation: differential effects on abeta production, amyloid deposition, and neuronal vulnerability.
Alzheimer Disease
Presenilin-1 polymorphism and Alzheimer's disease.
Alzheimer Disease
Presenilin-1 polymorphism and Alzheimer's disease. The Alzheimer's Study Group.
Alzheimer Disease
Presenilin-1 polymorphism and Alzheimer's disease. The UK Alzheimer's Disease Collaborative Group.
Alzheimer Disease
Presenilin-1 polymorphism in Alzheimer's disease and vascular dementia.
Alzheimer Disease
Presenilin-1 polymorphism in patients with Alzheimer's disease, vascular dementia and alcohol-associated dementia in Japanese population.
Alzheimer Disease
Presenilin-1 protects against neuronal apoptosis caused by its interacting protein PAG.
Alzheimer Disease
Presenilin-1 protein expression in familial and sporadic Alzheimer's disease.
Alzheimer Disease
Presenilin-1 protein specifically expressed in Leydig cells with its expression level increased during rat testis development.
Alzheimer Disease
Presenilin-1 regulates induction of hypoxia inducible factor-1?: altered activation by a mutation associated with familial Alzheimer's disease.
Alzheimer Disease
Presenilin-1 regulates neuronal differentiation during neurogenesis.
Alzheimer Disease
Presenilin-1 regulates the constitutive turnover of the fibronectin matrix in endothelial cells.
Alzheimer Disease
Presenilin-1 Regulates the Expression of p62 to Govern p62-dependent Tau Degradation.
Alzheimer Disease
Presenilin-1 regulates the neuronal threshold to excitotoxicity both physiologically and pathologically.
Alzheimer Disease
Presenilin-1 Targeted Morpholino Induces Cognitive Deficits, Increased Brain A?1-42 and Decreased Synaptic Marker PSD-95 in Zebrafish Larvae.
Alzheimer Disease
Presenilin-1, amyloid precursor protein and amyloid precursor-like protein 2 mRNA levels in human superior frontal cortex during aging.
Alzheimer Disease
Presenilin-1-deficient neurons are nitric oxide-dependently killed by hydrogen peroxide in vitro.
Alzheimer Disease
Presenilin-1-dependent transcriptome changes.
Alzheimer Disease
Presenilin-1-immunoreactive neurons are preserved in late-onset Alzheimer's disease.
Alzheimer Disease
Presenilin-2 and Calcium Handling: Molecules, Organelles, Cells and Brain Networks.
Alzheimer Disease
Presenilin-2 dampens intracellular Ca(2+) stores by increasing Ca(2+) leakage and reducing Ca(2+) uptake.
Alzheimer Disease
Presenilin-2 in the cynomolgus monkey brain: investigation of age-related changes.
Alzheimer Disease
Presenilin-2 mutation and polymorphism in Japanese Alzheimer disease patients.
Alzheimer Disease
Presenilin-2 mutation causes early amyloid accumulation and memory impairment in a transgenic mouse model of Alzheimer's disease.
Alzheimer Disease
Presenilin-2 polymorphisms and risk of sporadic AD: evidence from a meta-analysis.
Alzheimer Disease
Presenilin-Deficient Neurons and Astrocytes Display Normal Mitochondrial Phenotypes.
Alzheimer Disease
Presenilin-dependent expression of STIM proteins and dysregulation of capacitative Ca(2+) entry in familial Alzheimer's disease.
Alzheimer Disease
Presenilin-dependent gamma-secretase activity modulates neurite outgrowth.
Alzheimer Disease
Presenilin-dependent intramembrane cleavage of ephrin-B1.
Alzheimer Disease
Presenilin-dependent intramembrane proteolysis of CD44 leads to the liberation of its intracellular domain and the secretion of an Abeta-like peptide.
Alzheimer Disease
Presenilin-dependent regulated intramembrane proteolysis and gamma-secretase activity.
Alzheimer Disease
Presenilin-dependent transcriptional control of the Abeta-degrading enzyme neprilysin by intracellular domains of betaAPP and APLP.
Alzheimer Disease
Presenilin-interacting proteins.
Alzheimer Disease
Presenilin1 familial Alzheimer disease mutants inactivate EFNB1- and BDNF-dependent neuroprotection against excitotoxicity by affecting neuroprotective complexes of N-methyl-d-aspartate receptor.
Alzheimer Disease
Presenilins and Alzheimer's disease: biological functions and pathogenic mechanisms.
Alzheimer Disease
Presenilins and Alzheimer's disease: the role of A beta 42.
Alzheimer Disease
Presenilins Are Enriched in Endoplasmic Reticulum Membranes Associated with Mitochondria.
Alzheimer Disease
Presenilins as Drug Targets for Alzheimer's Disease-Recent Insights from Cell Biology and Electrophysiology as Novel Opportunities in Drug Development.
Alzheimer Disease
Presenilins as therapeutic targets for the treatment of Alzheimer's disease.
Alzheimer Disease
Presenilins in memory, Alzheimer's disease, and therapy.
Alzheimer Disease
Presenilins in the heart: presenilin-2 expression is increased by low glucose and by hypoxia in cardiac cells.
Alzheimer Disease
Presenilins interact with armadillo proteins including neural-specific plakophilin-related protein and beta-catenin.
Alzheimer Disease
Presenilins interact with Rab11, a small GTPase involved in the regulation of vesicular transport.
Alzheimer Disease
Presenilins upregulate functional K+ channel currents in mammalian cells.
Alzheimer Disease
Presenilins, the endoplasmic reticulum, and neuronal apoptosis in Alzheimer's disease.
Alzheimer Disease
Presenilins: molecular switches between proteolysis and signal transduction.
Alzheimer Disease
Preservation of cell-survival mechanisms by the presenilin-1 K239N mutation may cause its milder clinical phenotype.
Alzheimer Disease
Presynaptic dystrophic neurites surrounding amyloid plaques are sites of microtubule disruption, BACE1 elevation, and increased A? generation in Alzheimer's disease.
Alzheimer Disease
Prevalence of pathogenic mutations in an Italian clinical series of patients with familial dementia.
Alzheimer Disease
Previously not recognized deletion in presenilin-1 (p.Leu174del.) in a patient with early-onset familial Alzheimer's disease.
Alzheimer Disease
Prion protein and Alzheimer disease.
Alzheimer Disease
Prion protein expression alters APP cleavage without interaction with BACE-1.
Alzheimer Disease
Proamyloidogenic effects of membrane type 1 matrix metalloproteinase involve MMP-2 and BACE-1 activities, and the modulation of APP trafficking.
Alzheimer Disease
Probable novel PSEN1 Gln222Leu mutation in a Chinese family with early-onset Alzheimer's disease.
Alzheimer Disease
Probing the Mint2 protein-protein interaction network with relevance for the pathophysiology of Alzheimer's disease.
Alzheimer Disease
Processing of amyloid precursor protein as a biochemical link between atherosclerosis and Alzheimer's disease.
Alzheimer Disease
Processing of Notch and amyloid precursor protein by gamma-secretase is spatially distinct.
Alzheimer Disease
Processing of presenilin 1 in brains of patients with Alzheimer's disease and controls.
Alzheimer Disease
Processing of the Alzheimer's disease amyloid precursor protein in Pichia pastoris: immunodetection of alpha-, beta-, and gamma-secretase products.
Alzheimer Disease
Progress in the Development of Nonpeptidomimetic BACE 1 Inhibitors for Alzheimer's Disease.
Alzheimer Disease
Progress toward a practical BACE-1 inhibitor.
Alzheimer Disease
Progressive Age-Related Impairment of the Late Long-Term Potentiation in Alzheimer's Disease Presenilin-1 Mutant Knock-in Mice.
Alzheimer Disease
Progressive age-related impairment of the late long-term potentiation in Alzheimer's disease presenilin-1 mutant knock-in mice.
Alzheimer Disease
Prominent behavioural and psychiatric symptoms in early-onset Alzheimer's disease in a sib pair with the presenilin-1 gene R269G mutation.
Alzheimer Disease
Prominent expression of presenilin-1 in senile plaques and reactive astrocytes in Alzheimer's disease brain.
Alzheimer Disease
Prominent neuroleptic sensitivity in a case of early-onset Alzheimer disease due to presenilin-1 G206A mutation.
Alzheimer Disease
Promising anti-Alzheimer's dimer bis(7)-tacrine reduces beta-amyloid generation by directly inhibiting BACE-1 activity.
Alzheimer Disease
Promising multifunctional anti-Alzheimer's dimer bis(7)-Cognitin acting as an activator of protein kinase C regulates activities of alpha-secretase and BACE-1 concurrently.
Alzheimer Disease
Promoter polymorphisms which modulate BACE1 expression are associated with sporadic Alzheimer's disease.
Alzheimer Disease
Proprotein convertase activity contributes to the processing of the Alzheimer's beta-amyloid precursor protein in human cells: evidence for a role of the prohormone convertase PC7 in the constitutive alpha-secretase pathway.
Alzheimer Disease
Proteasome inhibitors prevent the degradation of familial Alzheimer's disease-linked presenilin 1 and potentiate A beta 42 recovery from human cells.
Alzheimer Disease
Protective effects of BACE1 inhibitory ligand molecules against amyloid beta-induced synaptic and mitochondrial toxicities in Alzheimer's disease.
Alzheimer Disease
Protective effects of ferulic acid in amyloid precursor protein plus presenilin-1 transgenic mouse model of Alzheimer disease.
Alzheimer Disease
Protein Expression of BACE1 is Downregulated by Donepezil in Alzheimer's Disease Platelets.
Alzheimer Disease
Protein levels of ADAM10, BACE1, and PSEN1 in platelets and leukocytes of Alzheimer's disease patients.
Alzheimer Disease
Protein markers for Alzheimer disease in the frontal cortex and cerebellum.
Alzheimer Disease
Protein Predictive Modeling and Simulation of Mutations of Presenilin-1 Familial Alzheimer's Disease on the Orthosteric Site.
Alzheimer Disease
Proteolytic fragments of Alzheimer's disease-associated presenilin 1 are present in synaptic organelles and growth cone membranes of rat brain.
Alzheimer Disease
Proteolytic processing and degradation of human presenilin-1 expressed in yeast.
Alzheimer Disease
Proteolytic processing of Neuregulin-1.
Alzheimer Disease
Proteolytic Processing of Neurexins by Presenilins Sustains Synaptic Vesicle Release.
Alzheimer Disease
Proteolytic processing of presenilin-1 (PS-1) is not associated with Alzheimer's disease with or without PS-1 mutations.
Alzheimer Disease
Proteolytic processing of the amyloid-beta protein precursor of Alzheimer's disease.
Alzheimer Disease
Proteomic identification of sorting nexin 6 as a negative regulator of BACE1-mediated APP processing.
Alzheimer Disease
Proteomic profiling of gamma-secretase substrates and mapping of substrate requirements.
Alzheimer Disease
PSEN2 (presenilin 2) mutants linked to familial Alzheimer disease impair autophagy by altering Ca2+ homeostasis.
Alzheimer Disease
Psychiatric Disorders in Alzheimer Disease With the Presenilin-1 L226F Mutation.
Alzheimer Disease
Psychosis in a Middle-aged Woman: A Case of Presenilin-1 p.Gly206Ala Alzheimer Disease.
Alzheimer Disease
Pulse Pressure: An Emerging Therapeutic Target for Dementia.
Alzheimer Disease
Purine derivatives as potent gamma-secretase modulators.
Alzheimer Disease
Putative function of ADAM9, ADAM10, and ADAM17 as APP alpha-secretase.
Alzheimer Disease
Quantification of presenilin-1 mRNA in Alzheimer's disease brains.
Alzheimer Disease
Quantitative interaction proteomics of neurodegenerative disease proteins.
Alzheimer Disease
Quantum mechanics study of the hydroxyethylamines-BACE-1 active site interaction energies.
Alzheimer Disease
Rab6 membrane association is dependent of Presenilin 1 and cellular phosphorylation events.
Alzheimer Disease
RAGE regulates BACE1 and A{beta} generation via NFAT1 activation in Alzheimer's disease animal model.
Alzheimer Disease
Randomized Trial of Verubecestat for Mild-to-Moderate Alzheimer's Disease.
Alzheimer Disease
Rapid and Direct Transport of Cell Surface APP to the Lysosome defines a novel selective pathway.
Alzheimer Disease
Rapid cell death is preceded by amyloid plaque-mediated oxidative stress.
Alzheimer Disease
Rapid Notch1 nuclear translocation after ligand binding depends on presenilin-associated gamma-secretase activity.
Alzheimer Disease
Rapid purification of active gamma-secretase, an intramembrane protease implicated in Alzheimer's disease.
Alzheimer Disease
Rapid stimulation of amyloid precursor protein release by epidermal growth factor: role of protein kinase C.
Alzheimer Disease
Rare autosomal copy number variations in early-onset familial Alzheimer's disease.
Alzheimer Disease
Rat brain gamma-secretase activity is highly influenced by detergents.
Alzheimer Disease
Rational Design of Novel 1,3-Oxazine Based ?-Secretase (BACE1) Inhibitors: Incorporation of a Double Bond To Reduce P-gp Efflux Leading to Robust A? Reduction in the Brain.
Alzheimer Disease
Rational design, synthesis and in vitro evaluation of allylidene hydrazinecarboximidamide derivatives as BACE-1 inhibitors.
Alzheimer Disease
RCAN1 Inhibits BACE2 Turnover by Attenuating Proteasome-Mediated BACE2 Degradation.
Alzheimer Disease
Recent Advances in the Identification of gamma-Secretase Inhibitors To Clinically Test the Abeta Oligomer Hypothesis of Alzheimer's Disease.
Alzheimer Disease
Recent Studies on Design and Development of Drugs Against Alzheimer's Disease (AD) Based on Inhibition of BACE-1 and Other AD-causative Agents.
Alzheimer Disease
Reconstitution of gamma-secretase activity.
Alzheimer Disease
Reduced expression of amyloid precursor protein, presenilin-1 and rab3a in cortical brain regions in Alzheimer's disease.
Alzheimer Disease
Reduced Sodium Channel Nav1.1 Levels in BACE1-null Mice.
Alzheimer Disease
Reduction BACE1 expression via suppressing NF-?B mediated signaling by Tamibarotene in a mouse model of Alzheimer's disease.
Alzheimer Disease
Reduction of Ca2+ stores and capacitative Ca2+ entry is associated with the familial Alzheimer's disease presenilin-2 T122R mutation and anticipates the onset of dementia.
Alzheimer Disease
Reduction of SorLA/LR11, a sorting protein limiting beta-amyloid production, in Alzheimer disease cerebrospinal fluid.
Alzheimer Disease
Reductions in beta-amyloid concentrations in vivo by the gamma-secretase inhibitors BMS-289948 and BMS-299897.
Alzheimer Disease
Refractory epilepsy in PSEN 1 mutation (I83T).
Alzheimer Disease
Regional and cellular presenilin 1 gene expression in human and rat tissues.
Alzheimer Disease
Regional brain evaluation of acetylcholinesterase activity in PS1/A246E transgenic mice.
Alzheimer Disease
Regional cerebral glucose utilization is modulated by the dosage of apolipoprotein E type 4 allele and alpha1-antichymotrypsin type A allele in Alzheimer's disease.
Alzheimer Disease
Regional distribution of presenilin-1 messenger RNA in the embryonic rat brain: comparison with beta-amyloid precursor protein messenger RNA localization.
Alzheimer Disease
Regional distribution of synaptic markers and APP correlate with distinct clinicopathological features in sporadic and familial Alzheimer's disease.
Alzheimer Disease
Regulated intramembrane proteolysis of the interleukin-1 receptor II by alpha-, beta-, and gamma-secretase.
Alzheimer Disease
Regulation of Alzheimer's disease amyloid-beta formation by casein kinase I.
Alzheimer Disease
Regulation of amyloid beta-protein precursor by phosphorylation and protein interactions.
Alzheimer Disease
Regulation of apoptosis by presenilin 1.
Alzheimer Disease
Regulation of brain G-protein go by Alzheimer's disease gene presenilin-1.
Alzheimer Disease
Regulation of gamma-secretase activity in Alzheimer's disease.
Alzheimer Disease
Regulation of secretases by all-trans-retinoic acid.
Alzheimer Disease
Regulation of Synaptic Amyloid-? Generation through BACE1 Retrograde Transport in a Mouse Model of Alzheimer's Disease.
Alzheimer Disease
Relationship between beta amyloid peptide generating molecules and neprilysin in Alzheimer disease and normal brain.
Alzheimer Disease
Relationship between neuronal loss and 'inflammatory plaques' in early onset Alzheimer's disease.
Alzheimer Disease
Relationship between the polymorphism in exon 5 of BACE1 gene and Alzheimer's disease.
Alzheimer Disease
Relationship between ubiquilin-1 and BACE1 in human Alzheimer's disease and APdE9 transgenic mouse brain and cell-based models.
Alzheimer Disease
Relative ratio and level of amyloid-? 42 surrogate in cerebrospinal fluid of familial Alzheimer disease patients with presenilin 1 mutations.
Alzheimer Disease
Release of a membrane-bound death domain by gamma-secretase processing of the p75NTR homolog NRADD.
Alzheimer Disease
Remodelling of Ca2+ homeostasis in type I cortical astrocytes by hypoxia: evidence for association with Alzheimer's disease.
Alzheimer Disease
Repurposing bromocriptine for A? metabolism in Alzheimer's disease (REBRAnD) study: randomised placebo-controlled double-blind comparative trial and open-label extension trial to investigate the safety and efficacy of bromocriptine in Alzheimer's disease with presenilin 1 (PSEN1) mutations.
Alzheimer Disease
Requirement for small side chain residues within the GxGD-motif of presenilin for gamma-secretase substrate cleavage.
Alzheimer Disease
Residues at P2-P1 positions of varepsilon- and zeta-cleavage sites are important in formation of beta-amyloid peptide.
Alzheimer Disease
Restricted growth and insulin-like growth factor-1 deficiency in mice lacking presenilin-1 in the neural crest cell lineage.
Alzheimer Disease
Retention of the Alzheimer's amyloid precursor fragment C99 in the endoplasmic reticulum prevents formation of amyloid beta-peptide.
Alzheimer Disease
Reticulons RTN3 and RTN4-B/C interact with BACE1 and inhibit its ability to produce amyloid beta-protein.
Alzheimer Disease
RNA aptamers selectively modulate protein recruitment to the cytoplasmic domain of beta-secretase BACE1 in vitro.
Alzheimer Disease
RNA interference in silencing of genes of Alzheimer's disease in cellular and rat brain models.
Alzheimer Disease
Role of presenilin-1 in cortical lamination and survival of Cajal-Retzius neurons.
Alzheimer Disease
Role of the APP non-amyloidogenic signaling pathway and targeting alpha-secretase as an alternative drug target for treatment of Alzheimer's disease.
Alzheimer Disease
Role of tyrosine phosphorylation in the antioxidant effects of the p75 neurotrophin receptor.
Alzheimer Disease
RVG-Peptide-Linked Trimethylated Chitosan for Delivery of siRNA to the Brain.
Alzheimer Disease
S100A7, a novel Alzheimer's disease biomarker with non-amyloidogenic alpha-secretase activity acts via selective promotion of ADAM-10.
Alzheimer Disease
sA?PP? is a Potent Endogenous Inhibitor of BACE1.
Alzheimer Disease
Safety, tolerability, and effects on plasma and cerebrospinal fluid amyloid-beta after inhibition of gamma-secretase.
Alzheimer Disease
Safety, Tolerability, Pharmacokinetics, and Pharmacodynamic Effects of PF-06751979, a Potent and Selective Oral BACE1 Inhibitor: Results from Phase I Studies in Healthy Adults and Healthy Older Subjects.
Alzheimer Disease
Scaffold of the cyclooxygenase-2 (COX-2) inhibitor carprofen provides Alzheimer gamma-secretase modulators.
Alzheimer Disease
SCF(Fbx2) -E3-ligase-mediated degradation of BACE1 attenuates Alzheimer's disease amyloidosis and improves synaptic function.
Alzheimer Disease
Scope of ?-Secretase (BACE1)-Targeted Therapy in Alzheimer's Disease: Emphasizing the Flavonoid Based Natural Scaffold for BACE1 Inhibition.
Alzheimer Disease
Screening for presenilin-1 gene mutations by PCR-SSCP analysis in patients with early-onset Alzheimer's disease.
Alzheimer Disease
Searching for the Multi-Target-Directed Ligands against Alzheimer's disease: discovery of quinoxaline-based hybrid compounds with AChE, H?R and BACE 1 inhibitory activities.
Alzheimer Disease
Second generation of BACE-1 inhibitors part 2: Optimisation of the non-prime side substituent.
Alzheimer Disease
Second generation of BACE-1 inhibitors. Part 1: The need for improved pharmacokinetics.
Alzheimer Disease
Second generation of hydroxyethylamine BACE-1 inhibitors: optimizing potency and oral bioavailability.
Alzheimer Disease
Secretase inhibitors for Alzheimer's disease: challenges of a promiscuous protease.
Alzheimer Disease
Secreted amyloid beta-protein similar to that in the senile plaques of Alzheimer's disease is increased in vivo by the presenilin 1 and 2 and APP mutations linked to familial Alzheimer's disease.
Alzheimer Disease
Secreted beta-amyloid precursor protein counteracts the proapoptotic action of mutant presenilin-1 by activation of NF-kappaB and stabilization of calcium homeostasis.
Alzheimer Disease
Secretion of long Abeta-related peptides processed at epsilon-cleavage site is dependent on the alpha-secretase pre-cutting.
Alzheimer Disease
Seizure protein 6 and its homolog seizure 6-like protein are physiological substrates of BACE1 in neurons.
Alzheimer Disease
Seizure protein 6 controls glycosylation and trafficking of kainate receptor subunits GluK2 and GluK3.
Alzheimer Disease
Seladin-1 transcription is linked to neuronal degeneration in Alzheimer's disease.
Alzheimer Disease
Selected non-steroidal anti-inflammatory drugs and their derivatives target gamma-secretase at a novel site. Evidence for an allosteric mechanism.
Alzheimer Disease
Selecting cells with different Alzheimer's disease gamma-secretase activity using FACS. Differential effect on presenilin exon 9 gamma- and epsilon-cleavage.
Alzheimer Disease
Self-refinement of Notch activity through the transmembrane protein Crumbs: modulation of gamma-secretase activity.
Alzheimer Disease
Semagacestat, a gamma-secretase inhibitor for the potential treatment of Alzheimer's disease.
Alzheimer Disease
Semi-synthetic isoflavones as BACE-1 inhibitors against Alzheimer's disease.
Alzheimer Disease
Sequence analysis of presenilin-1 gene mutation in Japanese Alzheimer's disease patients.
Alzheimer Disease
Serpents on the road to dementia and death. Accumulating evidence from several studies points to the normal function of presenilin 1 and suggests how the mutant protein contributes to deposition of amyloid plaques in Alzheimer's disease.
Alzheimer Disease
Serum Beta Secretase 1 (BACE1) activity increases in patients with mild cognitive impairment.
Alzheimer Disease
Sex Differences in Cognitive Abilities Among Children With the Autosomal Dominant Alzheimer Disease Presenilin 1 E280A Variant From a Colombian Cohort.
Alzheimer Disease
Signal peptide peptidase and gamma-secretase share equivalent inhibitor binding pharmacology.
Alzheimer Disease
Signal peptide peptidase dependent cleavage of type II transmembrane substrates releases intracellular and extracellular signals.
Alzheimer Disease
Signal peptide peptidase: biochemical properties and modulation by nonsteroidal antiinflammatory drugs.
Alzheimer Disease
Signaling effect of amyloid-beta(42) on the processing of AbetaPP.
Alzheimer Disease
Significance of intracellular Abeta42 accumulation in Alzheimer's disease.
Alzheimer Disease
Significance of transcytosis in Alzheimer's disease: BACE1 takes the scenic route to axons.
Alzheimer Disease
Similar mechanisms regulated by gamma-secretase are involved in both directions of the bi-directional Notch-Delta signaling pathway as well as play a potential role in signaling events involving type 1 transmembrane proteins.
Alzheimer Disease
Simple structure-based approach for predicting the activity of inhibitors of beta-secretase (BACE1) associated with Alzheimer's disease.
Alzheimer Disease
Simultaneous quantitation of the BACE1 inhibitor AZD3293 and its metabolite AZ13569724 in human matrices by LC-MS/MS.
Alzheimer Disease
Single chain variable fragment against nicastrin inhibits the gamma-secretase activity.
Alzheimer Disease
Single-entity heparan sulfate glycomimetic clusters for therapeutic applications.
Alzheimer Disease
Skeletal and CNS defects in Presenilin-1-deficient mice.
Alzheimer Disease
Small-molecule BACE1 inhibitors: a patent literature review (2006 - 2011).
Alzheimer Disease
Sodium channel cleavage is associated with aberrant neuronal activity and cognitive deficits in a mouse model of Alzheimer's disease.
Alzheimer Disease
Soluble amyloid precursor protein alpha inhibits tau phosphorylation through modulation of GSK3? signaling pathway.
Alzheimer Disease
Soluble BACE-1 Activity and sA?PP? Concentrations in Alzheimer's Disease and Age-Matched Healthy Control Cerebrospinal Fluid from the Alzheimer's Disease Neuroimaging Initiative-1 Baseline Cohort.
Alzheimer Disease
Solution-phase parallel synthesis of carbamates as gamma-secretase inhibitors.
Alzheimer Disease
Somatic mutation analysis of the APP and Presenilin 1 and 2 genes in Alzheimer's disease brains.
Alzheimer Disease
Sorting out the cell biology of Alzheimer's disease: focus on BACE1 and APP.
Alzheimer Disease
Spastic paraplegia preceding PSEN1-related familial Alzheimer's disease.
Alzheimer Disease
Spatial learning in transgenic mice expressing human presenilin 1 (PS1) transgenes.
Alzheimer Disease
Spatial patterns of ?-amyloid (A?) deposits in familial and sporadic Alzheimer's disease.
Alzheimer Disease
Specific BACE1 genotypes provide additional risk for late-onset Alzheimer disease in APOE epsilon 4 carriers.
Alzheimer Disease
Specific deficit of colour-colour short-term memory binding in sporadic and familial Alzheimer's disease.
Alzheimer Disease
Specific mutations in presenilin 1 cause conformational changes in ?-secretase to modulate amyloid ? trimming.
Alzheimer Disease
Specificity of memapsin 1 and its implications on the design of memapsin 2 (beta-secretase) inhibitor selectivity.
Alzheimer Disease
Specificity of presenilin-1- and presenilin-2-dependent ?-secretases towards substrate processing.
Alzheimer Disease
Spectral Analysis of EEG in Familial Alzheimer's Disease with E280A Presenilin-1 Mutation Gene.
Alzheimer Disease
Sphingosylphosphorylcholine Attenuated ?-Amyloid Production by Reducing BACE1 Expression and Catalysis in PC12 Cells.
Alzheimer Disease
Spirocyclic Sulfamides as BACE-1 Inhibitors for the Treatment of Alzheimer's Disease: Utilization of Structure Based Drug Design, WaterMap, and CNS Penetration Studies to Identify Centrally Efficacious Inhibitors.
Alzheimer Disease
Spirocyclic ß-Site Amyloid Precursor Protein Cleaving Enzyme 1 (BACE1) Inhibitors: From Hit to Lowering of Cerebrospinal Fluid (CSF) Amyloid Beta in a Higher Species.
Alzheimer Disease
Splice variants of the Alzheimer's disease beta-secretase, BACE1.
Alzheimer Disease
Splicing mutation of presenilin-1 gene for early-onset familial Alzheimer's disease.
Alzheimer Disease
Sporadic inclusion-body myositis and its similarities to Alzheimer disease brain. Recent approaches to diagnosis and pathogenesis, and relation to aging.
Alzheimer Disease
Stable association of presenilin derivatives and absence of presenilin interactions with APP.
Alzheimer Disease
Statins and the Squalene Synthase Inhibitor Zaragozic Acid Stimulate the Non-Amyloidogenic Pathway of Amyloid-beta Protein Precursor Processing by Suppression of Cholesterol Synthesis.
Alzheimer Disease
Staurosporine-induced activation of caspase-3 is potentiated by presenilin 1 familial Alzheimer's disease mutations in human neuroglioma cells.
Alzheimer Disease
Stepping closer to treating Alzheimer's disease patients with BACE1 inhibitor drugs.
Alzheimer Disease
Stereoselective synthesis of constrained azacyclic hydroxyethylene isosteres as aspartic protease inhibitors: dipolar cycloaddition and related methodologies toward branched pyrrolidine and pyrrolidinone carboxylic acids.
Alzheimer Disease
Stereoselective synthesis of constrained oxacyclic hydroxyethylene isosteres of aspartic protease inhibitors: aldol and Mukaiyama aldol methodologies for branched tetrahydrofuran 2-carboxylic acids.
Alzheimer Disease
Structural and Functional Determinants of gamma-Secretase, an Intramembrane Protease Implicated in Alzheimer's Disease.
Alzheimer Disease
Structural features of human memapsin 2 (beta-secretase) and their biological and pathological implications.
Alzheimer Disease
Structural investigation of the C-terminal catalytic fragment of presenilin 1.
Alzheimer Disease
Structural locations and functional roles of new subsites S5, S6, and S7 in memapsin 2 (beta-secretase).
Alzheimer Disease
Structure and alternative splicing of the presenilin-2 gene.
Alzheimer Disease
Structure and function of gamma-secretase.
Alzheimer Disease
Structure of the catalytic pore of gamma-secretase probed by the accessibility of substituted cysteines.
Alzheimer Disease
Structure of the protease domain of memapsin 2 (beta-secretase) complexed with inhibitor.
Alzheimer Disease
Structure, mechanism and inhibition of gamma-secretase and presenilin-like proteases.
Alzheimer Disease
Structure-activity relationship of memapsin 2: implications on physiological functions and Alzheimer's disease.
Alzheimer Disease
Structure-Based Approaches to Improving Selectivity through Utilizing Explicit Water Molecules: Discovery of Selective ?-Secretase (BACE1) Inhibitors over BACE2.
Alzheimer Disease
Structure-Based Design of Selective ?-Site Amyloid Precursor Protein Cleaving Enzyme 1 (BACE1) Inhibitors: Targeting the Flap to Gain Selectivity over BACE2.
Alzheimer Disease
Structure-based design: potent inhibitors of human brain memapsin 2 (beta-secretase).
Alzheimer Disease
Structure-Based Survey of the Binding Modes of BACE1 Inhibitors.
Alzheimer Disease
Studies to investigate the in vivo therapeutic window of the gamma-secretase inhibitor N2-[(2S)-2-(3,5-difluorophenyl)-2-hydroxyethanoyl]-N1-[(7S)-5-methyl-6-oxo-6,7-dihydro-5H-dibenzo[b,d]azepin-7-yl]-L-alaninamide (LY411,575) in the CRND8 mouse.
Alzheimer Disease
Study of memapsin 2 (beta-secretase) and strategy of inhibitor design.
Alzheimer Disease
Subcellular distribution and turnover of presenilins in transfected cells.
Alzheimer Disease
Subcellular localization of presenilin 2 endoproteolytic C-terminal fragments.
Alzheimer Disease
Subcellular localization of presenilins during mouse preimplantation development.
Alzheimer Disease
Subcellular mechanisms of presenilin-mediated enhancement of calcium signaling.
Alzheimer Disease
Subsite specificity of memapsin 2 (beta-secretase): implications for inhibitor design.
Alzheimer Disease
Substituted 2-oxo-azepane derivatives are potent, orally active gamma-secretase inhibitors.
Alzheimer Disease
Substituted thiazolamide coupled to a redox delivery system: a new gamma-secretase inhibitor with enhanced pharmacokinetic profile.
Alzheimer Disease
Substitution of a glycogen synthase kinase-3beta phosphorylation site in presenilin 1 separates presenilin function from beta-catenin signaling.
Alzheimer Disease
Substrate specificity of gamma-secretase and other intramembrane proteases.
Alzheimer Disease
Substrate-targeting gamma-secretase modulators.
Alzheimer Disease
Sulfonamido-derivatives of unsubstituted carbazoles as BACE1 inhibitors.
Alzheimer Disease
Sulfuretin exerts diversified functions in the processing of amyloid precursor protein.
Alzheimer Disease
SUMO1 modulates A? generation via BACE1 accumulation.
Alzheimer Disease
Superimposing the 27 crystal protein/inhibitor complexes of ?-secretase to calculate the binding affinities by the linear interaction energy method.
Alzheimer Disease
Superoxide free radical and intracellular calcium mediate A beta(1-42) induced endothelial toxicity.
Alzheimer Disease
Superoxide mediates the cell-death-enhancing action of presenilin-1 mutations.
Alzheimer Disease
Supplementation with apple juice attenuates presenilin-1 overexpression during dietary and genetically-induced oxidative stress.
Alzheimer Disease
Suppressor Mutations for Presenilin 1 Familial Alzheimer Disease Mutants Modulate ?-Secretase Activities.
Alzheimer Disease
Susceptibility to cellular stress in PS1 mutant N2a cells is associated with mitochondrial defects and altered calcium homeostasis.
Alzheimer Disease
Susceptibility to diet-induced obesity and glucose intolerance in the APP (SWE)/PSEN1 (A246E) mouse model of Alzheimer's disease is associated with increased brain levels of protein tyrosine phosphatase 1B (PTP1B) and retinol-binding protein 4 (RBP4), and basal phosphorylation of S6 ribosomal protein.
Alzheimer Disease
Swedish mutant APP-based BACE1 binding site peptide reduces APP ?-cleavage and cerebral A? levels in Alzheimer's mice.
Alzheimer Disease
Synaptic activity prompts gamma-secretase-mediated cleavage of EphA4 and dendritic spine formation.
Alzheimer Disease
Synaptic and endosomal localization of active gamma-secretase in rat brain.
Alzheimer Disease
Synaptic transmission and hippocampal long-term potentiation in transgenic mice expressing FAD-linked presenilin 1.
Alzheimer Disease
Synergistic Deleterious Effect of Chronic Stress and Sodium Azide in the Mouse Hippocampus.
Alzheimer Disease
Synthesis and evaluation of arylquinones as BACE1 inhibitors, ?-amyloid peptide aggregation inhibitors, and destabilizers of preformed ?-amyloid fibrils.
Alzheimer Disease
Synthesis and evaluation of multi-target-directed ligands with BACE-1 inhibitory and Nrf2 agonist activities as potential agents against Alzheimer's disease.
Alzheimer Disease
Synthesis and evaluation of succinoyl-caprolactam gamma-secretase inhibitors.
Alzheimer Disease
Synthesis and structure-activity relationship of a novel series of heterocyclic sulfonamide gamma-secretase inhibitors.
Alzheimer Disease
Synthesis of Verubecestat, a BACE1 Inhibitor for the Treatment of Alzheimer's Disease.
Alzheimer Disease
Systematic genetic study of Alzheimer disease in Latin America: mutation frequencies of the amyloid beta precursor protein and presenilin genes in Colombia.
Alzheimer Disease
Systematic substrate identification indicates a central role for the metalloprotease ADAM10 in axon targeting and synapse function.
Alzheimer Disease
Systemic delivery of BACE1 siRNA through neuron-targeted nanocomplexes for treatment of Alzheimer's disease.
Alzheimer Disease
T/G polymorphism at intron 9 of presenilin 1 gene is associated with, but not responsible for sporadic late-onset Alzheimer's disease in Japanese population.
Alzheimer Disease
Target specific proteochemometric model development for BACE1 - protein flexibility and structural water are critical in virtual screening.
Alzheimer Disease
Targeting ADAM10 to lipid rafts in neuroblastoma SH-SY5Y cells impairs amyloidogenic processing of the amyloid precursor protein.
Alzheimer Disease
Targeting antigen-specific receptors on B lymphocytes to generate high yields of specific monoclonal antibodies directed against biologically active lower antigenic peptides within presenilin 1.
Alzheimer Disease
Targeting BACE1 with siRNAs ameliorates Alzheimer disease neuropathology in a transgenic model.
Alzheimer Disease
Targeting Cannabinoid Receptor Activation and BACE-1 Activity Counteracts TgAPP Mice Memory Impairment and Alzheimer's Disease Lymphoblast Alterations.
Alzheimer Disease
Targeting the ? secretase BACE1 for Alzheimer's disease therapy.
Alzheimer Disease
TASTPM Mice Expressing Amyloid Precursor Protein and Presenilin-1 Mutant Transgenes Are Sensitive to gamma-Secretase Modulation and Amyloid-beta(42) Lowering by GSM-10h.
Alzheimer Disease
Tau deletion reduces plaque-associated BACE1 accumulation and decelerates plaque formation in a mouse model of Alzheimer's disease.
Alzheimer Disease
Tau load is associated with apolipoprotein E genotype and the amount of amyloid beta protein, Abeta40, in sporadic and familial Alzheimer's disease.
Alzheimer Disease
Tau negative frontal lobe dementia at 17q21: significant finemapping of the candidate region to a 4.8 cM interval.
Alzheimer Disease
Tau phosphorylation in cells transfected with wild-type or an Alzheimer's disease mutant Presenilin 1.
Alzheimer Disease
Tauroursodeoxycholic acid modulates p53-mediated apoptosis in Alzheimer's disease mutant neuroblastoma cells.
Alzheimer Disease
Temporal Effects of Neuron-specific beta-secretase 1 (BACE1) Knock-in on the Mouse Brain Metabolome: Implications for Alzheimer's Disease.
Alzheimer Disease
Temporal-spatial expression of presenilin 1 and the production of amyloid-beta after acute spinal cord injury in adult rat.
Alzheimer Disease
Tetrahydroquinoline sulfonamides as gamma-secretase inhibitors.
Alzheimer Disease
Tetrapeptides, as small-sized peptidic inhibitors; synthesis and their inhibitory activity against BACE1.
Alzheimer Disease
The β-Secretase Enzyme BACE1: A Biochemical Enigma for Alzheimer's Disease.
Alzheimer Disease
The -22c/t polymorphism in presenilin 1 gene is not connected with late-onset and early-onset familial Alzheimer's disease in Poland.
Alzheimer Disease
The -48 C/T polymorphism in the presenilin 1 promoter is associated with an increased risk of developing Alzheimer's disease and an increased Abeta load in brain.
Alzheimer Disease
The 1239G/C polymorphism in exon 5 of BACE1 gene may be associated with sporadic Alzheimer's disease in Chinese Hans.
Alzheimer Disease
The 4,752 C/T polymorphism in the presenilin 1 gene increases the risk of Alzheimer's disease in apolipoprotein E4 carriers.
Alzheimer Disease
The ?-Secretase BACE1 in Alzheimer's Disease.
Alzheimer Disease
The ?-secretase enzyme BACE1 as a therapeutic target for Alzheimer's disease.
Alzheimer Disease
The Alzheimer disease-related calcium-binding protein Calmyrin is present in human forebrain with an altered distribution in Alzheimer's as compared to normal ageing brains.
Alzheimer Disease
The Alzheimer's disease beta-secretase enzyme, BACE1.
Alzheimer Disease
The Alzheimer's prevention initiative composite cognitive test score: sample size estimates for the evaluation of preclinical Alzheimer's disease treatments in presenilin 1 E280A mutation carriers.
Alzheimer Disease
The Alzheimer-related gene presenilin 1 facilitates notch 1 in primary mammalian neurons.
Alzheimer Disease
The amyloid beta-protein precursor of Alzheimer's disease is degraded extracellularly by a Kunitz protease inhibitor domain-sensitive trypsin-like serine protease in cultures of chick sympathetic neurons.
Alzheimer Disease
The amyloid-beta rise and gamma-secretase inhibitor potency depend on the level of substrate expression.
Alzheimer Disease
The association of the regulatory region of the presenilin-2 gene with Alzheimer's disease in the Northern Han Chinese population.
Alzheimer Disease
The association of three BACE1 gene polymorphisms (exon5 C/G, intron 5 T/G and 3'UTR T/A) with sporadic Alzheimer's disease susceptibility: a meta-analysis.
Alzheimer Disease
The BACE inhibitor NB-360 in preclinical models: From ?-amyloid reduction to downstream disease-relevant effects.
Alzheimer Disease
The BACE-1 inhibitor CNP520 for prevention trials in Alzheimer's disease.
Alzheimer Disease
The BACE1 inhibitor verubecestat (MK-8931) reduces CNS ?-amyloid in animal models and in Alzheimer's disease patients.
Alzheimer Disease
The Basic Biology of BACE1: A Key Therapeutic Target for Alzheimer's Disease.
Alzheimer Disease
The biochemistry of Alzheimer disease.
Alzheimer Disease
The biochemistry of Alzheimer's disease.
Alzheimer Disease
The biological and pathological function of the presenilin-1 Deltaexon 9 mutation is independent of its defect to undergo proteolytic processing.
Alzheimer Disease
The C-terminal fragment of the Alzheimer's disease amyloid protein precursor is degraded by a proteasome-dependent mechanism distinct from gamma-secretase.
Alzheimer Disease
The C-terminal region of CHD3/ZFH interacts with the CIDD region of the Ets transcription factor ERM and represses transcription of the human presenilin 1 gene.
Alzheimer Disease
The cell adhesion protein P-selectin glycoprotein ligand-1 is a substrate for the aspartyl protease BACE1.
Alzheimer Disease
The clinical phenotype of two missense mutations in the presenilin I gene in Japanese patients.
Alzheimer Disease
The coat protein complex II, COPII, protein Sec13 directly interacts with presenilin-1.
Alzheimer Disease
The Cysteine Protease Inhibitor, E64d, Reduces Brain Amyloid-? and Improves Memory Deficits in Alzheimer's Disease Animal Models by Inhibiting Cathepsin B, but not BACE1, ?-Secretase Activity.
Alzheimer Disease
The cytosolic inclusion bodies that consist of splice variants that lack exon 5 of the presenilin-2 gene differ obviously from Hirano bodies observed in the brain from sporadic cases of Alzheimer's disease patients.
Alzheimer Disease
The cytosolic loop of the gamma-secretase component presenilin enhancer 2 protects zebrafish embryos from apoptosis.
Alzheimer Disease
The cytosolic N-terminus of presenilin-1 potentiates mouse ryanodine receptor single channel activity.
Alzheimer Disease
The discovery and role of CD147 as a subunit of gamma-secretase complex.
Alzheimer Disease
The dynamic mechanism of presenilin-1 function: Sensitive gate dynamics and loop unplugging control protein access.
Alzheimer Disease
The E280A presenilin 1 Alzheimer mutation produces increased A beta 42 deposition and severe cerebellar pathology.
Alzheimer Disease
The E318G substitution in PSEN1 gene is not connected with Alzheimer's disease in a large Polish cohort.
Alzheimer Disease
The effects of dietary restriction and aging on amyloid precursor protein and presenilin-1 mRNA and protein expression in rat brain.
Alzheimer Disease
The Endosome-associated Deubiquitinating Enzyme USP8 Regulates BACE1 Enzyme Ubiquitination and Degradation.
Alzheimer Disease
The expression of HMGA1a is increased in lymphoblastoid cell lines from schizophrenia patients.
Alzheimer Disease
The expression of microRNA miR-107 decreases early in Alzheimer's disease and may accelerate disease progression through regulation of beta-site amyloid precursor protein-cleaving enzyme 1.
Alzheimer Disease
The expression of presenilin 1 mRNA in skin fibroblasts and brains from sporadic Alzheimer's disease.
Alzheimer Disease
The expression of presenilin-1 mRNA in skin fibroblasts from Alzheimer's disease.
Alzheimer Disease
The expression of the nicotinic acetylcholine receptor ?3 subunit in the brains of patients with Alzheimer's disease and its effects on ?- and ?-secretases and Notch signal transduction in SH-SY5Y cells.
Alzheimer Disease
The gamma-secretase complex: machinery for intramembrane proteolysis.
Alzheimer Disease
The gamma-secretase-generated intracellular domain of beta-amyloid precursor protein binds Numb and inhibits Notch signaling.
Alzheimer Disease
The gamma/epsilon-Secretase-Derived APP Intracellular Domain Fragments Regulate p53.
Alzheimer Disease
The gene encoding nicastrin, a major gamma-secretase component, modifies risk for familial early-onset Alzheimer disease in a Dutch population-based sample.
Alzheimer Disease
The genetics of Alzheimer disease: current status and future prospects.
Alzheimer Disease
The genetics of Alzheimer's disease.
Alzheimer Disease
The genotype 2/2 of the presenilin-1 polymorphism is decreased in Spanish early-onset Alzheimer's disease.
Alzheimer Disease
The Glu318Gly mutation of the presenilin-1 gene does not necessarily cause Alzheimer's disease.
Alzheimer Disease
The Glu318Gly substitution in presenilin 1 is not causally related to Alzheimer disease.
Alzheimer Disease
The Golgi-Localized ?-Ear-Containing ARF-Binding (GGA) Proteins Alter Amyloid-? Precursor Protein (APP) Processing through Interaction of Their GAE Domain with the Beta-Site APP Cleaving Enzyme 1 (BACE1).
Alzheimer Disease
The GxGD motif of presenilin contributes to catalytic function and substrate identification of gamma-secretase.
Alzheimer Disease
The Identification of Biochanin A as a Potent and Selective ?-Site App-Cleaving Enzyme 1 (Bace1) Inhibitor.
Alzheimer Disease
The impact of different presenilin 1 andpresenilin 2 mutations on amyloid deposition, neurofibrillary changes and neuronal loss in the familial Alzheimer's disease brain: evidence for other phenotype-modifying factors.
Alzheimer Disease
The increased activity of BACE1 correlates with oxidative stress in Alzheimer's disease.
Alzheimer Disease
The inhibition of gamma-secretase as a therapeutic approach to Alzheimer's disease.
Alzheimer Disease
The initial substrate-binding site of gamma-secretase is located on presenilin near the active site.
Alzheimer Disease
The L392V mutation of presenilin 1 associated with autosomal dominant early-onset Alzheimer's disease alters the secondary structure of the hydrophilic loop.
Alzheimer Disease
The large hydrophilic loop of presenilin 1 is important for regulating gamma-secretase complex assembly and dictating the amyloid beta peptide (Abeta) Profile without affecting Notch processing.
Alzheimer Disease
The Latin American Spanish version of the Face-Name Associative Memory Exam is sensitive to cognitive and pathological changes in preclinical autosomal dominant Alzheimer's disease.
Alzheimer Disease
The law of mass action applied to neurodegenerative disease: a hypothesis concerning the etiology and pathogenesis of complex diseases.
Alzheimer Disease
The low density lipoprotein receptor-related protein (LRP) is a novel beta-secretase (BACE1) substrate.
Alzheimer Disease
The mechanism of gamma-secretase activities through high molecular weight complex formation of presenilins is conserved in Drosophila melanogaster and mammals.
Alzheimer Disease
The Membrane-Bound Aspartyl Protease BACE1: Molecular and Functional Properties in Alzheimer's Disease and Beyond.
Alzheimer Disease
The Metalloprotease Meprin ? Is an Alternative ?-Secretase of APP.
Alzheimer Disease
The modeling of Alzheimer's disease by the overexpression of mutant Presenilin 1 in human embryonic stem cells.
Alzheimer Disease
The molecular tweezer CLR01 improves behavioral deficits and reduces tau pathology in P301S-tau transgenic mice.
Alzheimer Disease
The N-terminus of presenilin-2 increases single channel activity of brain ryanodine receptors through direct protein-protein interaction.
Alzheimer Disease
The Neural Cell Adhesion Molecules L1 and CHL1 Are Cleaved by BACE1 Protease in Vivo.
Alzheimer Disease
The nonconserved hydrophilic loop domain of presenilin (PS) is not required for PS endoproteolysis or enhanced abeta 42 production mediated by familial early onset Alzheimer's disease-linked PS variants.
Alzheimer Disease
The novel multi-target iron chelating-radical scavenging compound M30 possesses beneficial effects on major hallmarks of Alzheimer's disease.
Alzheimer Disease
The pathogenic L392V mutation of presenilin 1 decreases the affinity to glycogen synthase kinase-3 beta.
Alzheimer Disease
The physical approximation of APP and BACE-1: A key event in alzheimer's disease pathogenesis.
Alzheimer Disease
The possible effect of microRNA-155 (miR-155) and BACE1 inhibitors in the memory of patients with down syndrome and Alzheimer's disease: Design, synthesis, virtual screening, molecular modeling and biological evaluations.
Alzheimer Disease
The potent BACE1 inhibitor LY2886721 elicits robust central A? pharmacodynamic responses in mice, dogs, and humans.
Alzheimer Disease
The potential for BACE1 inhibitors in the treatment of Alzheimer's disease.
Alzheimer Disease
The presenilin 1 C92S mutation increases abeta 42 production.
Alzheimer Disease
The presenilin 1 deltaE9 mutation gives enhanced basal phospholipase C activity and a resultant increase in intracellular calcium concentrations.
Alzheimer Disease
The presenilin 1 mutation (M146V) linked to familial Alzheimer's disease attenuates the neuronal differentiation of NTera 2 cells.
Alzheimer Disease
The presenilin 1 p.Gly206Ala mutation is a frequent cause of early-onset Alzheimer's disease in Hispanics in Florida.
Alzheimer Disease
The presenilin-1 familial Alzheimer disease mutant P117L impairs neurogenesis in the hippocampus of adult mice.
Alzheimer Disease
The presenilin-1 familial Alzheimer's disease mutation P117L decreases neuronal differentiation of embryonic murine neural progenitor cells.
Alzheimer Disease
The presenilins and Alzheimer's disease.
Alzheimer Disease
The processing and biological function of the human amyloid precursor protein (APP): lessons from different cellular models.
Alzheimer Disease
The proteins BACE1 and BACE2 and beta-secretase activity in normal and Alzheimer's disease brain.
Alzheimer Disease
The proteolytic processing of the amyloid precursor protein gene family members APLP-1 and APLP-2 involves alpha-, beta-, gamma-, and epsilon-like cleavages: modulation of APLP-1 processing by n-glycosylation.
Alzheimer Disease
The R269H mutation in presenilin-1 presenting as late-onset autosomal dominant Alzheimer's disease.
Alzheimer Disease
The regulation of presenilin-1 by nerve growth factor.
Alzheimer Disease
The role of Alzheimer's disease-related presenilin 1 in intercellular adhesion.
Alzheimer Disease
The role of amyloid precursor protein processing by BACE1, the beta-secretase, in Alzheimer disease pathophysiology.
Alzheimer Disease
The role of beta-catenin stability in mutant PS1-associated apoptosis.
Alzheimer Disease
The Role of Cathepsin B in the Degradation of A? and in the Production of A? Peptides Starting With Ala2 in Cultured Astrocytes.
Alzheimer Disease
The role of cerebral amyloid beta accumulation in common forms of Alzheimer disease.
Alzheimer Disease
The role of heparan sulfate in the generation of Abeta.
Alzheimer Disease
The role of low-density receptor-related protein 1 (LRP1) as a competitive substrate of the amyloid precursor protein (APP) for BACE1.
Alzheimer Disease
The role of membrane trafficking in the processing of amyloid precursor protein and production of amyloid peptides in Alzheimer's disease.
Alzheimer Disease
The role of presenilin 1 in the genetics of Alzheimer's disease.
Alzheimer Disease
The role of presenilin-1 in the gamma-secretase cleavage of the amyloid precursor protein of Alzheimer's disease.
Alzheimer Disease
The role of the presenilin-1 homologue gene sel-12 of Caenorhabditis elegans in apoptotic activities.
Alzheimer Disease
The Selective BACE1 Inhibitor VIa Reduces Amyloid-? Production in Cell and Mouse Models of Alzheimer's Disease.
Alzheimer Disease
The sterol carrier protein SCP-x/pro-SCP-2 gene has transcriptional activity and regulates the Alzheimer disease gamma-secretase.
Alzheimer Disease
The Structure and Function of ?, ? and ?-Secretase as Therapeutic Target Enzymes in the Development of Alzheimer's Disease: A Review.
Alzheimer Disease
The structure of the presenilin 1 (S182) gene and identification of six novel mutations in early onset AD families. Alzheimer's Disease Collaborative Group.
Alzheimer Disease
The Swedish APP mutation alters the effect of genetically reduced BACE1 expression on the APP processing.
Alzheimer Disease
The synergy factor: a statistic to measure interactions in complex diseases.
Alzheimer Disease
The transcription factor Yin Yang 1 is an activator of BACE1 expression.
Alzheimer Disease
The two-hydrophobic domain tertiary structure of reticulon proteins is critical for modulation of beta-secretase BACE1.
Alzheimer Disease
The Ups and Downs of BACE1: Walking a Fine Line between Neurocognitive and Other Psychiatric Symptoms of Alzheimer's Disease.
Alzheimer Disease
The Variations of Presenilin 1 Promoter are Associated with Sporadic Alzheimer's Disease.
Alzheimer Disease
Therapeutic impact of rHuEPO on abnormal platelet APP, BACE 1, presenilin 1, ADAM 10 and A? expressions in chronic kidney disease patients with cognitive dysfunction like Alzheimer's disease: A pilot study.
Alzheimer Disease
Therapeutic potential of cyanobacterial pigment protein phycoerythrin: in silico and in vitro study of BACE1 interaction and in vivo A? reduction.
Alzheimer Disease
Therapeutic potential of gamma-secretase inhibitors and modulators.
Alzheimer Disease
Therapeutic targeting of the alpha-secretase pathway to treat Alzheimer's disease.
Alzheimer Disease
Thiamine deficiency alters APP but not presenilin-1 immunoreactivity in vulnerable brain regions.
Alzheimer Disease
Thioredoxin-80 is a product of alpha-secretase cleavage that inhibits amyloid-beta aggregation and is decreased in Alzheimer's disease brain.
Alzheimer Disease
Three different mutations of presenilin 1 gene in early-onset Alzheimer's disease families.
Alzheimer Disease
Three novel presenilin 1 mutations marking the wide spectrum of age at onset and clinical patterns in familial Alzheimer's disease.
Alzheimer Disease
Three-amino acid spacing of presenilin endoproteolysis suggests a general stepwise cleavage of gamma-secretase-mediated intramembrane proteolysis.
Alzheimer Disease
Three-year follow-up of a patient with early-onset Alzheimer's disease with presenilin-2 N141I mutation - case report and review of the literature.
Alzheimer Disease
Time-domain fluorescent plate reader for cell based protein-protein interaction and protein conformation assays.
Alzheimer Disease
Tolfenamic acid downregulates BACE1 and protects against lead-induced upregulation of Alzheimer's disease related biomarkers.
Alzheimer Disease
Topology of the C-terminal fragment of human presenilin 1.
Alzheimer Disease
Toward ?-Secretase-1 Inhibitors with Improved Isoform Selectivity.
Alzheimer Disease
Trans-dominant negative effects of pathogenic PSEN1 mutations on ?-secretase activity and A? production.
Alzheimer Disease
Transcriptional and post-transcriptional profile of human chromosome 21.
Alzheimer Disease
Transcriptional and translational regulation of BACE1 expression--implications for Alzheimer's disease.
Alzheimer Disease
Transcriptional regulation of BACE1, the beta-amyloid precursor protein beta-secretase, by Sp1.
Alzheimer Disease
Transcriptional regulation of the murine Presenilin-2 gene reveals similarities and differences to its human orthologue.
Alzheimer Disease
Transcriptional regulation of the presenilin-1 gene: implication in Alzheimer's disease.
Alzheimer Disease
Transferrin is responsible for mediating the effects of iron ions on the regulation of anterior pharynx-defective-1?/? and Presenilin 1 expression via PGE2 and PGD2 at the early stage of Alzheimer's Disease.
Alzheimer Disease
Transgenic expression of the amyloid-beta precursor protein-intracellular domain does not induce Alzheimer's Disease-like traits in vivo.
Alzheimer Disease
Transgenic mice with Alzheimer presenilin 1 mutations show accelerated neurodegeneration without amyloid plaque formation.
Alzheimer Disease
Transition-state analogue gamma-secretase inhibitors stabilize a 900 kDa presenilin/nicastrin complex.
Alzheimer Disease
Transition-state analogue inhibitors of gamma-secretase bind directly to presenilin-1.
Alzheimer Disease
Translational control of BACE1 may go awry in Alzheimer's disease.
Alzheimer Disease
Translational regulation of BACE-1 expression in neuronal and non-neuronal cells.
Alzheimer Disease
Transmembrane domain 9 of presenilin determines the dynamic conformation of the catalytic site of gamma-secretase.
Alzheimer Disease
Transmembrane structures of amyloid precursor protein dimer predicted by replica-exchange molecular dynamics simulations.
Alzheimer Disease
Trientine Reduces BACE1 Activity and Mitigates Amyloidosis via the AGE/RAGE/NF-kappa B Pathway in a Transgenic Mouse Model of Alzheimer's Disease.
Alzheimer Disease
Tripchlorolide Attenuates ?-amyloid Generation via Suppressing PPAR?-Regulated BACE1 Activity in N2a/APP695 Cells.
Alzheimer Disease
Triptolide treatment reduces Alzheimer's disease (AD)-like pathology through inhibition of BACE1 in a transgenic mouse model of AD.
Alzheimer Disease
Turmeric and curcumin suppress presenilin 1 protein expression in Jurkat cells.
Alzheimer Disease
Twenty-nine missense mutations linked with familial Alzheimer's disease alter the processing of presenilin 1.
Alzheimer Disease
Two domains within the first putative transmembrane domain of presenilin 1 differentially influence presenilinase and gamma-secretase activity.
Alzheimer Disease
Two endoplasmic reticulum (ER)/ER Golgi intermediate compartment-based lysine acetyltransferases post-translationally regulate BACE1 levels.
Alzheimer Disease
Two novel (M233T and R278T) presenilin-1 mutations in early-onset Alzheimer's disease pedigrees and preliminary evidence for association of presenilin-1 mutations with a novel phenotype.
Alzheimer Disease
Two Novel Mutations and a de novo Mutation in PSEN1 in Early-onset Alzheimer's Disease.
Alzheimer Disease
Two Novel Mutations in the First Transmembrane Domain of Presenilin1 Cause Young-Onset Alzheimer's Disease.
Alzheimer Disease
Two novel presenilin 1 gene mutations connected with frontotemporal dementia-like clinical phenotype: genetic and bioinformatic assessment.
Alzheimer Disease
Two novel presenilin-1 mutations (I249L and P433S) in early onset Chinese Alzheimer's pedigrees and their functional characterization.
Alzheimer Disease
Two novel presenilin-1 mutations (Ser169Leu and Pro436Gln) associated with very early onset Alzheimer's disease.
Alzheimer Disease
Two novel presenilin-1 mutations (Y256S and Q222H) are associated with early-onset Alzheimer's disease.
Alzheimer Disease
Two polymorphisms of presenilin-2 gene (PSEN2) 5' regulatory region are not associated with Alzheimer's disease (AD) in the Polish population.
Alzheimer Disease
Two transmembrane aspartates in presenilin-1 required for presenilin endoproteolysis and gamma-secretase activity.
Alzheimer Disease
Tyramine fragment binding to BACE-1.
Alzheimer Disease
Ubiquitin regulates GGA3-mediated degradation of BACE1.
Alzheimer Disease
Ubiquitin-proteasome pathway mediates degradation of APH-1.
Alzheimer Disease
Ultrastructure evidence of necrotic neural cell death in familial Alzheimer's disease brains bearing presenilin-1 E280A mutation.
Alzheimer Disease
Understanding BACE1: essential protease for amyloid-beta production in Alzheimer's disease.
Alzheimer Disease
Unfolded protein response signaling by transcription factor XBP-1 regulates ADAM10 and is affected in Alzheimer's disease.
Alzheimer Disease
Unnatural amino acid-substituted (hydroxyethyl)urea peptidomimetics inhibit gamma-secretase and promote the neuronal differentiation of neuroblastoma cells.
Alzheimer Disease
Unravelling the molecular basis of AM-6494 high potency at BACE1 in Alzheimer's disease: an integrated dynamic interaction investigation.
Alzheimer Disease
Unveiling a novel transient druggable pocket in BACE-1 through molecular simulations: Conformational analysis and binding mode of multisite inhibitors.
Alzheimer Disease
Upregulation of BACE1 and beta-Amyloid Protein Mediated by Chronic Cerebral Hypoperfusion Contributes to Cognitive Impairment and Pathogenesis of Alzheimer's Disease.
Alzheimer Disease
Upregulation of Presenilin 1 in Brains of Sporadic, Late-Onset Alzheimer's Disease.
Alzheimer Disease
Using a genetically targeted sensor to investigate the role of presenilin-1 in ER Ca(2+) levels and dynamics.
Alzheimer Disease
Val(8)GLP-1 rescues synaptic plasticity and reduces dense core plaques in APP/PS1 mice.
Alzheimer Disease
Val97Leu mutant presenilin-1 induces tau hyperphosphorylation and spatial memory deficit in mice and the underlying mechanisms.
Alzheimer Disease
Variable expression of presenilin 1 is not a major determinant of risk for late-onset Alzheimer's disease.
Alzheimer Disease
Variable phenotype of Alzheimer's disease with spastic paraparesis.
Alzheimer Disease
Variant Alzheimer disease with spastic paraparesis: a rare presenilin-1 mutation.
Alzheimer Disease
Variant Alzheimer disease with spastic paraparesis: neuropathological phenotype.
Alzheimer Disease
Variant Alzheimer's disease with spastic paraparesis: clinical characterization.
Alzheimer Disease
Variation in RTN3 and PPIL2 Genes Does not Influence Platelet Membrane beta-Secretase Activity or Susceptibility to Alzheimer's Disease in the Northern Irish Population.
Alzheimer Disease
Variations in the neuropathology of familial Alzheimer's disease.
Alzheimer Disease
Vasopressin and bradykinin regulate secretory processing of the amyloid protein precursor of Alzheimer's disease.
Alzheimer Disease
Very early onset AD with a de novo mutation in the presenilin 1 gene (Met 233 Leu).
Alzheimer Disease
Very early onset Alzheimer's disease with spastic paraparesis associated with a novel presenilin 1 mutation (Phe237Ile).
Alzheimer Disease
Very early-onset familial Alzheimer's disease: a novel presenilin 1 mutation.
Alzheimer Disease
Very early-onset sporadic Alzheimer's disease with a de novo mutation in the PSEN1 gene.
Alzheimer Disease
Visual short-term memory binding deficit in familial Alzheimer's disease.
Alzheimer Disease
Visual short-term memory binding deficits in familial Alzheimer's disease.
Alzheimer Disease
Visualizing APP and BACE-1 approximation in neurons yields insight into the amyloidogenic pathway.
Alzheimer Disease
Visuo-spatial learning and memory deficits on the Barnes maze in the 16-month-old APPswe/PS1dE9 mouse model of Alzheimer's disease.
Alzheimer Disease
Voltage-dependent Na+ channels as targets of BACE1 - implications for neuronal firing and beyond.
Alzheimer Disease
What is 'early onset dementia'?
Alzheimer Disease
When loss is gain: reduced presenilin proteolytic function leads to increased Abeta42/Abeta40. Talking Point on the role of presenilin mutations in Alzheimer disease.
Alzheimer Disease
When sporadic disease is not sporadic: the potential for genetic etiology.
Alzheimer Disease
Whole-genome sequencing suggests a chemokine gene cluster that modifies age at onset in familial Alzheimer's disease.
Alzheimer Disease
Why Did Tarenflurbil Fail in Alzheimer's Disease?
Alzheimer Disease
Wide range of disease onset in a family with Alzheimer disease and a His163Tyr mutation in the presenilin-1 gene.
Alzheimer Disease
Widespread distribution of reticulon-3 in various neurodegenerative diseases.
Alzheimer Disease
Widespread gamma-secretase activity in the cell, but do we need it at the mitochondria?
Alzheimer Disease
Widespread neuronal expression of the presenilin-1 early-onset Alzheimer's disease gene in the murine brain.
Alzheimer Disease
Wild-type presenilin 1 protects against Alzheimer disease mutation-induced amyloid pathology.
Alzheimer Disease
WITHDRAWN: Mental Disorders in Young Adults from Families with the Presenilin-1 Gene Mutation E280A in the Preclinical Stage of Alzheimer's Disease.
Alzheimer Disease
Workflow and methods of high-content time-lapse analysis for quantifying intracellular calcium signals.
Alzheimer Disease
Worldwide distribution of PSEN1 Met146Leu mutation: a large variability for a founder mutation.
Alzheimer Disease
YAC fragmentation with repetitive and single-copy sequences: detailed physical mapping of the presenilin 1 gene on chromosome 14.
Alzheimer Disease
Yeast growth selection system for the identification of cell-active inhibitors of beta-secretase.
Alzheimer Disease
Young investigator award recipient.
Alzheimer Disease
Zebrafish lacking Alzheimer presenilin enhancer 2 (Pen-2) demonstrate excessive p53-dependent apoptosis and neuronal loss.
Alzheimer Disease
Zinc enhances synthesis of presenilin 1 in mouse primary cortical culture.
Alzheimer Disease
[A Japanese family with familial Alzheimer's disease associated with presenilin 1 mutation: relationship between younger age of onset and ApoE gene polymorphism]
Alzheimer Disease
[A study on mutation of exon 5 of presenilin-1 in Alzheimer's disease]
Alzheimer Disease
[alpha]-Secretase ADAM10 as well as [alpha]APPs is reduced in platelets and CSF of Alzheimer disease patients.
Alzheimer Disease
[Alzheimer's disease treatment by inhibition/modulation of the gamma-secretase activity]
Alzheimer Disease
[Alzheimer's disease: focus on beta-amyloid and gamma-secretase]
Alzheimer Disease
[Analysis of intrusive errors in a memory test as possible pre-clinical marker of familial Alzheimer disease, in E280A presenilin-1 mutation carrier]
Alzheimer Disease
[Biochemistry of presenilin 1]
Alzheimer Disease
[Clinical characteristics of a family with early-onset Alzheimer's disease associated with a presenilin 1 mutation (M139T)]
Alzheimer Disease
[Detection of antibodies to beta-amyloid in carriers of E280A mutation in the presenilin-1 gene]
Alzheimer Disease
[Effect of an inhibitor of alpha-secretase metabolizing amyloid precursor protein on memory in rats]
Alzheimer Disease
[Effect of hyperforin on learning and memory abilities and A?????, ?APP and BACE1 protein expressions in hippocampus of Alzheimer's disease model mice].
Alzheimer Disease
[Effects of huannao yicong recipe extract on the learning and memory and related factors of Abeta generation in the brain of APP transgenic mice].
Alzheimer Disease
[Effects of vitamin E on expression of PS-1 and production of Abeta in the hippocampus of female senile rats].
Alzheimer Disease
[Expression of presenilin 1 on the cell surface in motile polarized cells]
Alzheimer Disease
[Familial Alzheimer's disease mutations in the presenilin 1 gene reduce cell-cell adhesion in transfected fibroblasts].
Alzheimer Disease
[Genetics of dementia].
Alzheimer Disease
[Gly(14)]-Humanin improved the learning and memory impairment induced by scopolamine in vivo.
Alzheimer Disease
[Identification and clone of human Alzheimer's disease related gene nicastrin promoter]
Alzheimer Disease
[Molecular genetics of Alzheimer's disease--presenilin and other genes]
Alzheimer Disease
[Mutation site of presenilin-1 gene in familial Alzheimer's disease]
Alzheimer Disease
[Pathogenesis of Alzheimer's disease: implications from amyloid research front]
Alzheimer Disease
[Pathology of familial Parkinson's disease]
Alzheimer Disease
[Potential role of presenilin 1 in regulation of synaptic function].
Alzheimer Disease
[Presenilin-1 (S182) causative gene of early-onset familial Alzheimer's disease]
Alzheimer Disease
[Recent progress in 'HMGA1a' which causes aberrant splicing of Presenilin-2 pre-mRNA in sporadic Alzheimer's disease]
Alzheimer Disease
[Study on expression of PS1 in APP-PS1 double gene stably transfected cell lines and its relation to gamma-secretase]
Alzheimer Disease
[Study on mutation of presenilin-1 gene in familial Alzheimer's disease]
Alzheimer Disease
[Study on the etiology of Alzheimer's disease caused by missense mutations in presenilin 1]
Alzheimer Disease
[Targeting the structure and function relationships of the gamma-secretase for the development of Alzheimer's disease]
Alzheimer Disease
[The effect of PNS on the content and activity of alpha-secretase in the brains of SAMP8 mice with alzheimer's disease].
Alzheimer Disease
[The effect of two newly Chinese presenilin-1 mutations on the sensitivity to trophic factor withdrawal in human neuroblastoma cells]
Alzheimer Disease
{gamma}-Secretase Substrate Concentration Modulates the Abeta42/Abeta40 Ratio: IMPLICATIONS FOR ALZHEIMER DISEASE.
Alzheimer Disease
{gamma}-Secretase-dependent cleavage of amyloid precursor protein regulates osteoblast behavior.
Alzheimer Disease
{gamma}-Secretase: Successive Tripeptide and Tetrapeptide Release from the Transmembrane Domain of {beta}-Carboxyl Terminal Fragment.
Amnesia
Anti-amnesic activity of neferine with antioxidant and anti-inflammatory capacities, as well as inhibition of ChEs and BACE1.
Amnesia
Presenilin-1 mutation associated with amnesia, ataxia, and medial temporal lobe T2 signal changes.
Amyloidosis
5-Lipoxygenase gene disruption reduces amyloid-beta pathology in a mouse model of Alzheimer's disease.
Amyloidosis
A bell-shaped dependence between amyloidosis and GABA accumulation in astrocytes in a mouse model of Alzheimer's disease.
Amyloidosis
A study of long-term potentiation in transgenic mice over-expressing mutant forms of both amyloid precursor protein and presenilin-1.
Amyloidosis
Astrocytes & Astrocyte derived Extracellular Vesicles in Morphine Induced Amyloidopathy: Implications for Cognitive Deficits in Opiate Abusers.
Amyloidosis
AZ-4217: a high potency BACE inhibitor displaying acute central efficacy in different in vivo models and reduced amyloid deposition in Tg2576 mice.
Amyloidosis
BACE1 and mutated presenilin-1 differently modulate Abeta40 and Abeta42 levels and cerebral amyloidosis in APPDutch transgenic mice.
Amyloidosis
BACE1, a major determinant of selective vulnerability of the brain to amyloid-beta amyloidogenesis, is essential for cognitive, emotional, and synaptic functions.
Amyloidosis
Brain Abeta amyloidosis in APPsw mice induces accumulation of presenilin-1 and tau.
Amyloidosis
Changes in the brain and plasma A? peptide levels with age and its relationship with cognitive impairment in the APPswe/PS1dE9 mouse model of Alzheimer's disease.
Amyloidosis
Combined treatment with the phenolics (-)-epigallocatechin-3-gallate and ferulic acid improves cognition and reduces Alzheimer-like pathology in mice.
Amyloidosis
Cytosolic proteins lose solubility as amyloid deposits in a transgenic mouse model of Alzheimer-type amyloidosis.
Amyloidosis
Diversity in A? deposit morphology and secondary proteome insolubility across models of Alzheimer-type amyloidosis.
Amyloidosis
Early functional connectivity deficits and progressive microstructural alterations in the TgF344-AD rat model of Alzheimer's Disease: A longitudinal MRI study.
Amyloidosis
Efficacy of chronic BACE1 inhibition in PS2APP mice depends on the regional A? deposition rate and plaque burden at treatment initiation.
Amyloidosis
Episodic-like memory deficits in the APPswe/PS1dE9 mouse model of Alzheimer's disease: relationships to beta-amyloid deposition and neurotransmitter abnormalities.
Amyloidosis
Ferulic acid is a nutraceutical ?-secretase modulator that improves behavioral impairment and alzheimer-like pathology in transgenic mice.
Amyloidosis
Gallic Acid is a Dual ?/?-Secretase Modulator that Reverses Cognitive Impairment and Remediates Pathology in Alzheimer Mice.
Amyloidosis
Genetically altered transgenic models of Alzheimer's disease.
Amyloidosis
Lack of BACE1 S-palmitoylation reduces amyloid burden and mitigates memory deficits in transgenic mouse models of Alzheimer's disease.
Amyloidosis
Modeling an anti-amyloid combination therapy for Alzheimer's disease.
Amyloidosis
Moderate reduction of gamma-secretase attenuates amyloid burden and limits mechanism-based liabilities.
Amyloidosis
Multiple Low-Dose Infusions of Human Umbilical Cord Blood Cells Improve Cognitive Impairments and Reduce Amyloid-?-Associated Neuropathology in Alzheimer Mice.
Amyloidosis
Non-neuronal and neuronal BACE1 elevation in association with angiopathic and leptomeningeal ?-amyloid deposition in the human brain.
Amyloidosis
Presence of soluble and cell-surface B-cell maturation antigen in systemic light-chain amyloidosis and its modulation by gamma-secretase inhibition.
Amyloidosis
Presenilin-1 polymorphism and hereditary cerebral hemorrhage with amyloidosis, Dutch type.
Amyloidosis
Regulation of forkhead transcription factor FoxO3a contributes to calorie restriction-induced prevention of Alzheimer's disease-type amyloid neuropathology and spatial memory deterioration.
Amyloidosis
SCF(Fbx2) -E3-ligase-mediated degradation of BACE1 attenuates Alzheimer's disease amyloidosis and improves synaptic function.
Amyloidosis
Swedish mutant APP-based BACE1 binding site peptide reduces APP ?-cleavage and cerebral A? levels in Alzheimer's mice.
Amyloidosis
Tannic Acid Is a Natural ?-Secretase Inhibitor That Prevents Cognitive Impairment and Mitigates Alzheimer-like Pathology in Transgenic Mice.
Amyloidosis
Trientine Reduces BACE1 Activity and Mitigates Amyloidosis via the AGE/RAGE/NF-kappa B Pathway in a Transgenic Mouse Model of Alzheimer's Disease.
Amyloidosis
YXQN Reduces Alzheimer's Disease-Like Pathology and Cognitive Decline in APPswePS1dE9 Transgenic Mice.
Amyotrophic Lateral Sclerosis
Genotyping of presenilin-1 polymorphism in amyotrophic lateral sclerosis.
Aphasia
Presenilin-1 Mutations in Alzheimer's Disease: An Update on Genotype-Phenotype Relationships.
Aphasia, Primary Progressive
The presenilin 1 P264L mutation presenting as non-fluent/agrammatic primary progressive aphasia.
Astrocytoma
A?-induced Ca(2+) influx regulates astrocytic BACE1 expression via calcineurin/NFAT4 signals.
Astrocytoma
Constitutive and cytokine-regulated expression of presenilin-1 and presenilin-2 genes in human neural cell lines.
Astrocytoma
Differential effects of transforming growth factor-beta(s) and glial cell line-derived neurotrophic factor on gene expression of presenilin-1 in human post-mitotic neurons and astrocytes.
Astrocytoma
Glial expression of presenilin epitopes in human brain with cerebral infarction and in astrocytoma.
Astrocytoma
Localization of presenilin-1 mRNA in rat brain.
Astrocytoma
The effects of alpha-secretase ADAM10 on the proteolysis of neuregulin-1.
Ataxia
Familial Alzheimer's disease-associated presenilin-1 alters cerebellar activity and calcium homeostasis.
Ataxia
Presenilin-1 mutation associated with amnesia, ataxia, and medial temporal lobe T2 signal changes.
Atherosclerosis
Corrigendum to title "Expression of Bace1 is positive with the progress of atherosclerosis and formation of foam cell" [Biochem. Biophys. Res. Commun. 528 (3) (2020) 440-446].
Atherosclerosis
Elevated A?42 in Aged, Non-demented Individuals with Cerebral Atherosclerosis.
Atherosclerosis
Expression of Bace1 is positive with the progress of atherosclerosis and formation of foam cell.
Atherosclerosis
gamma-Secretase inhibitor reduces diet-induced atherosclerosis in apolipoprotein E-deficient mice.
Atherosclerosis
Male-specific association between a gamma-secretase polymorphism and premature coronary atherosclerosis.
Atherosclerosis
TNF-? regulates the proteolytic degradation of ST6Gal-1 and endothelial cell-cell junctions through upregulating expression of BACE1.
Autoimmune Diseases
Tau and mTOR: The Hotspots for Multifarious Diseases in Alzheimer's Development.
Avitaminosis
Changes in Presenilin 1 gene methylation pattern in diet-induced B vitamin deficiency.
Avitaminosis
S-adenosylmethionine reduces the progress of the Alzheimer-like features induced by B-vitamin deficiency in mice.
beta-1,4-mannosyl-glycoprotein 4-beta-n-acetylglucosaminyltransferase deficiency
Bisecting GlcNAc modification stabilizes BACE1 protein under oxidative stress conditions.
Brain Diseases
Early onset autosomal dominant dementia with ataxia, extrapyramidal features, and epilepsy.
Brain Diseases
Increased expression of the gamma-secretase components presenilin-1 and nicastrin in activated astrocytes and microglia following traumatic brain injury.
Brain Injuries
Exacerbation of poststroke dementia by type 2 diabetes is associated with synergistic increases of beta-site amyloid precursor protein-cleaving enzyme activation and beta-amyloid generation in rat brains.
Brain Injuries
Penetrating Ballistic-Like Brain Injury Leads to MicroRNA Dysregulation, BACE1 Upregulation, and Amyloid Precursor Protein Loss in Lesioned Rat Brain Tissues.
Brain Injuries
Regulation of BACE1 expression after injury is linked to the p75 neurotrophin receptor.
Brain Injuries
Shared Genomic and Proteomic Contribution of Amyloid and Tau Protein Characteristic of Alzheimer's Disease to Brain Ischemia.
Brain Injuries, Traumatic
Increased expression of the gamma-secretase components presenilin-1 and nicastrin in activated astrocytes and microglia following traumatic brain injury.
Brain Injuries, Traumatic
Lithium Reduces BACE1 Overexpression, Beta Amyloid Accumulation, and Spatial Learning Deficits in Mice with Traumatic Brain Injury.
Brain Injuries, Traumatic
Long-term accumulation of amyloid-beta, beta-secretase, presenilin-1, and caspase-3 in damaged axons following brain trauma.
Brain Ischemia
Alzheimer-associated presenilin 2 gene is dysregulated in rat medial temporal lobe cortex after complete brain ischemia due to cardiac arrest.
Brain Ischemia
Dysregulation of Amyloid-? Protein Precursor, ?-Secretase, Presenilin 1 and 2 Genes in the Rat Selectively Vulnerable CA1 Subfield of Hippocampus Following Transient Global Brain Ischemia.
Brain Ischemia
Electric Stimulation of Neurogenesis Improves Behavioral Recovery After Focal Ischemia in Aged Rats.
Brain Ischemia
Hypoxia-inducible factor 1alpha (HIF-1alpha)-mediated hypoxia increases BACE1 expression and beta-amyloid generation.
Brain Ischemia
Mild cognitive impairment: animal models.
Brain Ischemia
Oxygen-glucose deprivation regulates BACE1 expression through induction of autophagy in Neuro-2a/APP695 cells.
Brain Ischemia
The up-regulation of BACE1 mediated by hypoxia and ischemic injury: role of oxidative stress and HIF1alpha.
Brain Ischemia
Toward prevention of Alzheimers disease--potential nutraceutical strategies for suppressing the production of amyloid beta peptides.
Brain Ischemia
Upregulation of BACE1 and beta-Amyloid Protein Mediated by Chronic Cerebral Hypoperfusion Contributes to Cognitive Impairment and Pathogenesis of Alzheimer's Disease.
Brain Ischemia
[mRNA expression and activity of ADAM17 in hippocampus after chronic cerebral hypoperfusion: experiment with aged rats]
Brain Neoplasms
A computational guided, functional validation of a novel therapeutic antibody proposes Notch signaling as a clinical relevant and druggable target in glioma.
Breast Neoplasms
?-secretase components as predictors of breast cancer outcome.
Breast Neoplasms
A study on Notch signaling in human breast cancer.
Breast Neoplasms
Beta-Secretase 1 (BACE1) Is Down-Regulated in Invasive Ductal Carcinoma of Breast.
Breast Neoplasms
Cancer stem cells in breast cancer.
Breast Neoplasms
De novo discovery of a gamma-secretase inhibitor response signature using a novel in vivo breast tumor model.
Breast Neoplasms
Down regulation of CSL activity inhibits cell proliferation in prostate and breast cancer cells.
Breast Neoplasms
Downregulation of Notch pathway by a gamma-secretase inhibitor attenuates AKT/mammalian target of rapamycin signaling and glucose uptake in an ERBB2 transgenic breast cancer model.
Breast Neoplasms
DR5 antibody conjugated lipid-based nanocarriers of gamma-secretase inhibitor for the treatment of triple negative breast cancer.
Breast Neoplasms
ErbB-2 inhibition activates Notch-1 and sensitizes breast cancer cells to a gamma-secretase inhibitor.
Breast Neoplasms
Functional characterization of novel presenilin-2 variants identified in human breast cancers.
Breast Neoplasms
Gamma-secretase inhibitors target tumor-initiating cells in a mouse model of ERBB2 breast cancer.
Breast Neoplasms
High-level JAG1 mRNA and protein predict poor outcome in breast cancer.
Breast Neoplasms
Inhibition of gamma-secretase induces G2/M arrest and triggers apoptosis in breast cancer cells.
Breast Neoplasms
Mammary stem cells and breast cancer--role of Notch signalling.
Breast Neoplasms
Modeling the tertiary structure of human cathepsin-E.
Breast Neoplasms
Notch signaling in breast cancer and tumor angiogenesis: cross-talk and therapeutic potentials.
Breast Neoplasms
Presenilin 1/gamma-secretase is associated with cadmium-induced E-cadherin cleavage and COX-2 gene expression in T47D breast cancer cells.
Breast Neoplasms
Secretase-dependent tyrosine phosphorylation of Mdm2 by the ErbB-4 intracellular domain fragment.
Breast Neoplasms
Synthetic lethality through combined Notch-epidermal growth factor receptor pathway inhibition in basal-like breast cancer.
Breast Neoplasms
The cytotoxicity of gamma-secretase inhibitor I to breast cancer cells is mediated by proteasome inhibition, not by gamma-secretase inhibition.
Breast Neoplasms
The ERalpha coactivator, HER4/4ICD, regulates progesterone receptor expression in normal and malignant breast epithelium.
Breast Neoplasms
The HER4 cytoplasmic domain, but not its C terminus, inhibits mammary cell proliferation.
Carcinogenesis
gamma-Secretase inhibitors abrogate oxaliplatin-induced activation of the Notch-1 signaling pathway in colon cancer cells resulting in enhanced chemosensitivity.
Carcinogenesis
Loss of presenilin 1 is associated with enhanced beta-catenin signaling and skin tumorigenesis.
Carcinogenesis
Moderate reduction of gamma-secretase attenuates amyloid burden and limits mechanism-based liabilities.
Carcinogenesis
Phenotypic analysis of images of zebrafish treated with Alzheimer's gamma-secretase inhibitors.
Carcinogenesis
Suppression of colon carcinogenesis by targeting Notch signaling.
Carcinogenesis
The expression of presenilin 1 enhances carcinogenesis and metastasis in gastric cancer.
Carcinoma
Differential roles of Hath1, MUC2 and P27Kip1 in relation with gamma-secretase inhibition in human colonic carcinomas: a translational study.
Carcinoma
Epidermal Growth Factor Receptor and Notch Pathways Participate in the Tumor Suppressor Function of {gamma}-Secretase.
Carcinoma
Essential role of Notch signaling in apoptosis of human pancreatic tumoral cells mediated by exosomal nanoparticles.
Carcinoma
gamma-secretase inhibitors exerts antitumor activity via down-regulation of Notch and Nuclear factor kappa B in human tongue carcinoma cells.
Carcinoma
Inhibition of gamma-secretase activity impedes uterine serous carcinoma growth in a human xenograft model.
Carcinoma
Moderate reduction of gamma-secretase attenuates amyloid burden and limits mechanism-based liabilities.
Carcinoma
Morphologic and Immunohistochemical Appraisal of Primary Gastric Carcinomas.
Carcinoma
Presenilin 1 is frequently overexpressed and positively associates with epidermal growth factor receptor expression in head and neck squamous cell carcinoma.
Carcinoma
The cytotoxicity of gamma-secretase inhibitor I to breast cancer cells is mediated by proteasome inhibition, not by gamma-secretase inhibition.
Carcinoma
[Expression of Notch1, Jagged1 and NICD in epithelial ovarian carcinomas and a preliminary study on the activity of gamma-secretase in epithelial ovarian carcinoma cell lines].
Carcinoma
[Notch signaling pathway blocked by gamma-secretase inhibitor and its effect on the growth and apoptosis of SKOV3 cells].
Carcinoma, Hepatocellular
A small molecule inhibitor of signal Peptide peptidase inhibits Plasmodium development in the liver and decreases malaria severity.
Carcinoma, Hepatocellular
An upstream element containing an ETS binding site is crucial for transcription of the human presenilin-1 gene.
Carcinoma, Hepatocellular
Gamma-secretase complex-dependent intramembrane proteolysis of CD147 regulates the Notch1 signaling pathway in hepatocellular carcinoma.
Carcinoma, Hepatocellular
Inhibition of gamma-secretase affects proliferation of leukemia and hepatoma cell lines through Notch signaling.
Carcinoma, Hepatocellular
Modulation of the gamma-secretase activity as a therapy against human hepatocellular carcinoma.
Carcinoma, Hepatocellular
Notch Inhibitor PF-03084014 Inhibits Hepatocellular Carcinoma Growth and Metastasis via Suppression of Cancer Stemness due to Reduced Activation of Notch1-Stat3.
Carcinoma, Hepatocellular
Regulation of transcription of the human presenilin-1 gene by ets transcription factors and the p53 protooncogene.
Carcinoma, Intraductal, Noninfiltrating
Mammary stem cells and breast cancer--role of Notch signalling.
Carcinoma, Lobular
Aberrations of Chromosomes 1 and 16 in Breast Cancer: A Framework for Cooperation of Transcriptionally Dysregulated Genes.
Carcinoma, Non-Small-Cell Lung
MiR-574-3p accelerates cell migration and invasion through regulating BACE1 in Non-Small Cell Lung Cancer.
Carcinoma, Ovarian Epithelial
A phase II study of single-agent RO4929097, a gamma-secretase inhibitor of Notch signaling, in patients with recurrent platinum-resistant epithelial ovarian cancer: A study of the Princess Margaret Cancer Centre, Chicago and California phase II consortia.
Carcinoma, Ovarian Epithelial
[Expression of Notch1, Jagged1 and NICD in epithelial ovarian carcinomas and a preliminary study on the activity of gamma-secretase in epithelial ovarian carcinoma cell lines].
Carcinoma, Squamous Cell
Epidermal Growth Factor Receptor and Notch Pathways Participate in the Tumor Suppressor Function of {gamma}-Secretase.
Carcinoma, Squamous Cell
Moderate reduction of gamma-secretase attenuates amyloid burden and limits mechanism-based liabilities.
Carcinoma, Squamous Cell
Presenilin 1 is frequently overexpressed and positively associates with epidermal growth factor receptor expression in head and neck squamous cell carcinoma.
Cardiomyopathy, Dilated
Polymorphisms of presenilin-1 gene associate with dilated cardiomyopathy susceptibility.
Cardiovascular Diseases
Examining Sex Differences in Markers of Cognition and Neurodegeneration in Autosomal Dominant Alzheimer's Disease: Preliminary Findings from the Colombian Alzheimer's Prevention Initiative Biomarker Study.
Cataract
The link between apolipoprotein E, presenilin 1, and kinesin light chain 1 gene polymorphisms and age-related cortical cataracts in the Chinese population.
Cerebellar Ataxia
Presenilin-1 Mutations in Alzheimer's Disease: An Update on Genotype-Phenotype Relationships.
Cerebral Amyloid Angiopathy
A family with Alzheimer disease and strokes associated with A713T mutation of the APP gene.
Cerebral Amyloid Angiopathy
A mutant PSEN1 causes dementia with Lewy bodies and variant Alzheimer's disease.
Cerebral Amyloid Angiopathy
Association of presenilin-1 polymorphism with cerebral amyloid angiopathy in the elderly.
Cerebral Amyloid Angiopathy
BACE-1 is expressed in the blood-brain barrier endothelium and is upregulated in a murine model of Alzheimer's disease.
Cerebral Amyloid Angiopathy
Centrally Delivered BACE1 Inhibitor Activates Microglia, and Reverses Amyloid Pathology and Cognitive Deficit in Aged Tg2576 Mice.
Cerebral Amyloid Angiopathy
Cerebral amyloid angiopathy is a pathogenic lesion in Alzheimer's disease due to a novel presenilin 1 mutation.
Cerebral Amyloid Angiopathy
Novel presenilin-1 mutation with widespread cortical amyloid deposition but limited cerebral amyloid angiopathy.
Cerebral Amyloid Angiopathy
Occludin deficiency with BACE1 elevation in cerebral amyloid angiopathy.
Cerebral Amyloid Angiopathy, Familial
Presenilin-1 polymorphism and hereditary cerebral hemorrhage with amyloidosis, Dutch type.
Cerebral Hemorrhage
Amyloid angiopathy in a Volga German family with Alzheimer's disease and a presenilin-2 mutation (N141I).
Cerebral Hemorrhage
Presenilin-1 polymorphism and hereditary cerebral hemorrhage with amyloidosis, Dutch type.
Cerebral Hemorrhage
Selective expression of presenilin 1 in neural progenitor cells rescues the cerebral hemorrhages and cortical lamination defects in presenilin 1-null mutant mice.
Cerebral Infarction
Glial expression of presenilin epitopes in human brain with cerebral infarction and in astrocytoma.
Cerebral Infarction
Presenilin 1 immunostaining using well-characterized antibodies in human tissues.
Cerebrovascular Disorders
Increased blood BACE1 activity as a potential common pathogenic factor of vascular dementia and late onset Alzheimer's disease.
Chlamydophila Infections
Astrocytes infected with Chlamydia pneumoniae demonstrate altered expression and activity of secretases involved in the generation of ?-amyloid found in Alzheimer disease.
Cholangiocarcinoma
Inducible nitric oxide synthase up-regulates Notch-1 in mouse cholangiocytes: implications for carcinogenesis.
Choroidal Neovascularization
?-Secretase (BACE1) inhibition causes retinal pathology by vascular dysregulation and accumulation of age pigment.
Choroidal Neovascularization
Gamma-secretase regulates VEGFR-1 signalling in vascular endothelium and RPE.
Coinfection
Characterization of the reconstituted gamma-secretase complex from Sf9 cells co-expressing presenilin 1, nicastrin [correction of nacastrin], aph-1a, and pen-2.
Colitis
Distinct effects of p38alpha deletion in myeloid lineage and gut epithelia in mouse models of inflammatory bowel disease.
Colitis
Requirement of Notch activation during regeneration of the intestinal epithelia.
Colonic Neoplasms
Cleavage of ST6Gal I by radiation-induced BACE1 inhibits golgi-anchored ST6Gal I-mediated sialylation of integrin ?1 and migration in colon cancer cells.
Colonic Neoplasms
Gamma-secretase inhibition attenuates oxaliplatin-induced apoptosis through increased Mcl-1 and/or Bcl-xL in human colon cancer cells.
Colonic Neoplasms
Gamma-secretase inhibitor does not modulate angiogenesis in colon adenocarcinoma in obese mice.
Colonic Neoplasms
gamma-Secretase inhibitors abrogate oxaliplatin-induced activation of the Notch-1 signaling pathway in colon cancer cells resulting in enhanced chemosensitivity.
Colonic Neoplasms
Gamma-secretase inhibitors enhance taxane-induced mitotic arrest and apoptosis in colon cancer cells.
Colonic Neoplasms
Honokiol in combination with radiation targets Notch signaling to inhibit colon cancer stem cells.
Colonic Neoplasms
Notch and Wnt inhibitors as potential new drugs for intestinal neoplastic disease.
Colonic Neoplasms
Notch inhibits expression of the Krüppel-like factor 4 tumor suppressor in the intestinal epithelium.
Colonic Neoplasms
The COX-2 selective inhibitor-independent COX-2 effect on colon carcinoma cells is associated with the Delta1/Notch1 pathway.
Colorectal Neoplasms
Blockade of gamma-secretase activity within the hippocampus enhances long-term memory.
Colorectal Neoplasms
Gamma-secretase inhibition combined with platinum compounds enhances cell death in a large subset of colorectal cancer cells.
Colorectal Neoplasms
Gamma-secretase inhibitor, a potential target therapy for MUC2-positive colorectal carcinoma.
Colorectal Neoplasms
Gamma-secretase inhibitors enhance taxane-induced mitotic arrest and apoptosis in colon cancer cells.
Colorectal Neoplasms
miRDRN-miRNA disease regulatory network: a tool for exploring disease and tissue-specific microRNA regulatory networks.
Colorectal Neoplasms
Notch signaling in gastrointestinal tract (review).
Colorectal Neoplasms
Presenilin attenuates receptor-mediated signaling and synaptic function.
Colorectal Neoplasms
Presenilin-dependent "gamma-secretase" processing of deleted in colorectal cancer (DCC).
Communication Disorders
Development of molecular tools for diagnosis of Alzheimer's disease that are based on detection of amyloidogenic proteins.
Confusion
Epilepsy and cognitive impairments in Alzheimer disease.
Congenital Abnormalities
Normal brain development in PS1 hypomorphic mice with markedly reduced gamma-secretase cleavage of betaAPP.
Coronary Artery Disease
Male-specific association between a gamma-secretase polymorphism and premature coronary atherosclerosis.
Corticobasal Degeneration
Corticobasal Syndrome in a Family with Early-Onset Alzheimer's Disease Linked to a Presenilin-1 Gene Mutation.
Craniocerebral Trauma
Depletion of GGA1 and GGA3 Mediates Postinjury Elevation of BACE1.
Craniocerebral Trauma
Presenilin-1 polymorphism and amyloid beta-protein deposition in fatal head injury.
Creutzfeldt-Jakob Syndrome
A Common BACE1 Polymorphism Is a Risk Factor for Sporadic Creutzfeldt-Jakob Disease.
Creutzfeldt-Jakob Syndrome
CSF BACE1 activity is increased in CJD and Alzheimer disease other dementias.
Creutzfeldt-Jakob Syndrome
Development of molecular tools for diagnosis of Alzheimer's disease that are based on detection of amyloidogenic proteins.
Creutzfeldt-Jakob Syndrome
Familial Creutzfeldt-Jakob disease in a patient carrying both a presenilin 1 missense substitution and a prion protein gene insertion.
Cri-du-Chat Syndrome
GSK-3 phosphorylates delta-catenin and negatively regulates its stability via ubiquitination/proteosome-mediated proteolysis.
Deglutition Disorders
Dementia, pyramidal system involvement, and leukoencephalopathy with a presenilin 1 mutation.
Dementia
A case of probable non-familial early onset Alzheimer dementia in a Hispanic male.
Dementia
A novel p.Leu(381)Phe mutation in presenilin 1 is associated with very early onset and unusually fast progressing dementia as well as lysosomal inclusions typically seen in Kufs disease.
Dementia
A novel presenilin 1 L166H mutation in a pseudo-sporadic case of early-onset Alzheimer's disease.
Dementia
A presenilin 1 mutation associated with familial frontotemporal dementia inhibits gamma-secretase cleavage of APP and notch.
Dementia
Accelerated amyloid deposition in the brains of transgenic mice coexpressing mutant presenilin 1 and amyloid precursor proteins.
Dementia
Added value of cerebrospinal fluid multimarker analysis in diagnosis and progression of dementia.
Dementia
Alterations of chaperone protein expression in presenilin mutant neurons in response to glutamate excitotoxicity.
Dementia
AMY plaques in familial AD: comparison with sporadic Alzheimer's disease.
Dementia
Amyloid angiopathy in a Volga German family with Alzheimer's disease and a presenilin-2 mutation (N141I).
Dementia
An Overview of ?-Amyloid Cleaving Enzyme 1 (Bace1) in Alzheimer's Disease Therapy Elucidating its Exosite-Binding Antibody and Allosteric Inhibitor.
Dementia
Analysis of alpha-1 antichymotrypsin, presenilin-1, angiotensin-converting enzyme, and methylenetetrahydrofolate reductase loci as candidates for dementia.
Dementia
Analysis of apolipoprotein E, alpha1-antichymotrypsin and presenilin-1 genes polymorphisms in dementia caused by normal pressure hydrocephalus in man.
Dementia
Association of variants within APOE, SORL1, RUNX1, BACE1 and ALDH18A1 with dementia in Alzheimer's disease in subjects with Down syndrome.
Dementia
Asymptomatic Carriers of Presenilin-1 E318G Variant Show no Cerebrospinal Fluid Biochemical Signs Suggestive of Alzheimer's disease in a Family with Late-onset Dementia.
Dementia
Atypical dementia associated with a novel presenilin-2 mutation.
Dementia
Autosomal Dominant Alzheimer Disease: A Unique Resource to Study CSF Biomarker Changes in Preclinical AD.
Dementia
BACE1 role in Alzheimer's disease and other dementias: from the theory to the practice.
Dementia
Beta-Secretase 1 Underlies Reactive Astrocytes and Endothelial Disruption in Neurodegeneration.
Dementia
Biochemical markers in persons with preclinical familial Alzheimer disease.
Dementia
Biomarkers of Alzheimer disease, insulin resistance, and obesity in childhood.
Dementia
Cerebrospinal Fluid BACE1 Activity and sA?PP? as Biomarker Candidates of Alzheimer's Disease.
Dementia
Cognitive decline in patients with familial Alzheimer's disease associated with E280a presenilin-1 mutation: a longitudinal study.
Dementia
Convergence of pathology in dementia with Lewy bodies and Alzheimer's disease: a role for the novel interaction of alpha-synuclein and presenilin 1 in disease.
Dementia
CSF BACE1 activity is increased in CJD and Alzheimer disease other dementias.
Dementia
Decreased Deposition of Beta-Amyloid 1-38 and Increased Deposition of Beta-Amyloid 1-42 in Brain Tissue of Presenilin-1 E280A Familial Alzheimer's Disease Patients.
Dementia
Dementia with prominent frontotemporal features associated with L113P presenilin 1 mutation.
Dementia
Dementia, pyramidal system involvement, and leukoencephalopathy with a presenilin 1 mutation.
Dementia
Diagnostic accuracy of CERAD total score in a Colombian cohort with mild cognitive impairment and Alzheimer's disease affected by E280A mutation on presenilin-1 gene.
Dementia
Disease duration in autosomal dominant familial Alzheimer disease: A survival analysis.
Dementia
Dopa Responsive Parkinsonism in an Early Onset Alzheimer's Disease Patient with a Presenilin 1 Mutation (A434T).
Dementia
Early onset autosomal dominant dementia with ataxia, extrapyramidal features, and epilepsy.
Dementia
Electroacupuncture Mitigates Hippocampal Cognitive Impairments by Reducing BACE1 Deposition and Activating PKA in APP/PS1 Double Transgenic Mice.
Dementia
Elevated cerebrospinal fluid BACE1 activity in incipient Alzheimer disease.
Dementia
Epilepsy and cognitive impairments in Alzheimer disease.
Dementia
Exacerbation of poststroke dementia by type 2 diabetes is associated with synergistic increases of beta-site amyloid precursor protein-cleaving enzyme activation and beta-amyloid generation in rat brains.
Dementia
Examining Sex Differences in Markers of Cognition and Neurodegeneration in Autosomal Dominant Alzheimer's Disease: Preliminary Findings from the Colombian Alzheimer's Prevention Initiative Biomarker Study.
Dementia
Facilitation of glutamate, but not GABA, release in Familial Alzheimer's APP mutant Knock-in rats with increased ?-cleavage of APP.
Dementia
Familial Alzheimer disease-linked mutations specifically disrupt Ca2+ leak function of presenilin 1.
Dementia
Familial dementia with frontotemporal features associated with M146V presenilin-1 mutation.
Dementia
Frequency and clinicopathological characteristics of presenilin 1 Gly206Ala mutation in Puerto Rican Hispanics with dementia.
Dementia
Identification of Somatic Mutations in Dementia-related Genes in Cancer Patients.
Dementia
Increased blood BACE1 activity as a potential common pathogenic factor of vascular dementia and late onset Alzheimer's disease.
Dementia
Increased Plasma Beta-Secretase 1 May Predict Conversion to Alzheimer's Disease Dementia in Individuals With Mild Cognitive Impairment.
Dementia
Magnesium Modulates Amyloid-beta Protein Precursor Trafficking and Processing.
Dementia
MicroRNA-195 Protects Against Dementia Induced by Chronic Brain Hypoperfusion via Its Anti-Amyloidogenic Effect in Rats.
Dementia
MiR-9 Regulates the Expression of BACE1 in Dementia Induced by Chronic Brain Hypoperfusion in Rats.
Dementia
Molecular evidence of presenilin 1 mutation in familial early onset dementia.
Dementia
Nanolipidic particles improve the bioavailability and alpha-secretase inducing ability of epigallocatechin-3-gallate (EGCG) for the treatment of Alzheimer's disease.
Dementia
Neuropsychological profile of a large kindred with familial Alzheimer's disease caused by the E280A single presenilin-1 mutation.
Dementia
New V272A presenilin 1 mutation with very early onset subcortical dementia and parkinsonism.
Dementia
No association between a polymorphism in the presenilin 1 gene and dementia with Lewy bodies.
Dementia
Nodular bilateral amygdala degeneration in demented individuals.
Dementia
Novel presenilin 1 mutations associated with early onset of dementia in a family with both early-onset and late-onset Alzheimer disease.
Dementia
Novel Presenilin-1 Mutation (Ala275Ser) Associated With Clinical Features of Dementia With Lewy Bodies.
Dementia
Octapeptide repeat insertions in the prion protein gene and early onset dementia.
Dementia
Performance on MMSE sub-items and education level in presenilin-1 mutation carriers without dementia.
Dementia
Phenotypic Variability in Autosomal Dominant Familial Alzheimer Disease due to the S170F Mutation of Presenilin-1.
Dementia
Platelets: Peripheral Biomarkers of Dementia?
Dementia
Pre-dementia clinical stages in presenilin 1 E280A familial early-onset Alzheimer's disease: a retrospective cohort study.
Dementia
Presenilin 1 and alpha-1-antichymotrypsin polymorphisms in Down syndrome: no effect on the presence of dementia.
Dementia
Presenilin 2 mutation accelerates the onset of impairment in trace eyeblink conditioning in a mouse model of Alzheimer's disease overexpressing human mutant amyloid precursor protein.
Dementia
Presenilin gene predisposes to late-onset degenerative but not vascular dementia: a comparative study of PS1 and ApoE genes in a North Indian Cohort.
Dementia
Presenilin-1 gene intronic polymorphism and late-onset Alzheimer's disease.
Dementia
Presenilin-1 polymorphism and hereditary cerebral hemorrhage with amyloidosis, Dutch type.
Dementia
Presenilin-1 polymorphism in patients with Alzheimer's disease, vascular dementia and alcohol-associated dementia in Japanese population.
Dementia
Presenilin/gamma-Secretase and Inflammation.
Dementia
Pulse Pressure: An Emerging Therapeutic Target for Dementia.
Dementia
Reduction of Ca2+ stores and capacitative Ca2+ entry is associated with the familial Alzheimer's disease presenilin-2 T122R mutation and anticipates the onset of dementia.
Dementia
Refractory epilepsy in PSEN 1 mutation (I83T).
Dementia
Rescue of Early bace-1 and Global DNA Demethylation by S-Adenosylmethionine Reduces Amyloid Pathology and Improves Cognition in an Alzheimer's Model.
Dementia
S100A7, a novel Alzheimer's disease biomarker with non-amyloidogenic alpha-secretase activity acts via selective promotion of ADAM-10.
Dementia
Serpents on the road to dementia and death. Accumulating evidence from several studies points to the normal function of presenilin 1 and suggests how the mutant protein contributes to deposition of amyloid plaques in Alzheimer's disease.
Dementia
Serum Beta Secretase 1 (BACE1) activity increases in patients with mild cognitive impairment.
Dementia
Single and multiple transgenic mice as models for Alzheimer's disease.
Dementia
Spastic paraplegia preceding PSEN1-related familial Alzheimer's disease.
Dementia
The BACE-1 inhibitor CNP520 for prevention trials in Alzheimer's disease.
Dementia
The Latin American Spanish version of the Face-Name Associative Memory Exam is sensitive to cognitive and pathological changes in preclinical autosomal dominant Alzheimer's disease.
Dementia
Treatment of Alzheimer's Disease: The Legacy of the Cholinergic Hypothesis, Neuroplasticity, and Future Directions.
Dementia
Two novel (M233T and R278T) presenilin-1 mutations in early-onset Alzheimer's disease pedigrees and preliminary evidence for association of presenilin-1 mutations with a novel phenotype.
Dementia
Upregulation of SET Expression by BACE1 and its Implications in Down Syndrome.
Dementia
Variable phenotype of Alzheimer's disease with spastic paraparesis.
Dementia
When sporadic disease is not sporadic: the potential for genetic etiology.
Dementia, Vascular
Apolipoprotein E and intronic polymorphism of presenilin 1 and alpha-1-antichymotrypsin in Alzheimer's disease and vascular dementia.
Dementia, Vascular
Hypoxia-inducible factor 1alpha (HIF-1alpha)-mediated hypoxia increases BACE1 expression and beta-amyloid generation.
Dementia, Vascular
Increased blood BACE1 activity as a potential common pathogenic factor of vascular dementia and late onset Alzheimer's disease.
Dementia, Vascular
Presenilin-1 polymorphism in Alzheimer's disease and vascular dementia.
Dementia, Vascular
Presenilin-1 polymorphism in patients with Alzheimer's disease, vascular dementia and alcohol-associated dementia in Japanese population.
Demyelinating Diseases
Focal demyelination in Alzheimer's disease and transgenic mouse models.
Demyelinating Diseases
Overcoming failure to repair demyelination in EAE: gamma-secretase inhibition of Notch signaling.
Diabetes Mellitus
The BACE1 inhibitor LY2886721 improves diabetic phenotypes of BACE1 knock-in mice.
Diabetes Mellitus, Type 2
American Chemical Society - 240th national meeting - chemistry for preventing and combating disease: part 1.
Diabetes Mellitus, Type 2
Associations of Plasma BACE1 Level and BACE1 C786G Gene Polymorphism with Cognitive Functions in Patients with Type 2 Diabetes: A Cross- Sectional Study.
Diabetes Mellitus, Type 2
BACE2 plays a role in the insulin receptor trafficking in pancreatic beta-cells.
Diabetes Mellitus, Type 2
Exacerbation of poststroke dementia by type 2 diabetes is associated with synergistic increases of beta-site amyloid precursor protein-cleaving enzyme activation and beta-amyloid generation in rat brains.
Diabetes Mellitus, Type 2
Polymorphisms of presenilin-1 gene associate with dilated cardiomyopathy susceptibility.
Diabetes Mellitus, Type 2
Presenilin-1 Established ER-Ca2+ Leak: a Follow Up on Its Importance for the Initial Insulin Secretion in Pancreatic Islets and ?-Cells upon Elevated Glucose.
Diabetes Mellitus, Type 2
The BACE1 inhibitor LY2886721 improves diabetic phenotypes of BACE1 knock-in mice.
Diabetes Mellitus, Type 2
[Glucagon-like peptide 1 improves learning and memory abilities of rats with type 2 diabetes].
Disorders of Sex Development
Sex differences in autophagy-mediated diseases: toward precision medicine.
Down Syndrome
Abeta 17-42 in Alzheimer's disease activates JNK and caspase-8 leading to neuronal apoptosis.
Down Syndrome
Accumulation of Insoluble Amyloid-? in Down's Syndrome is Associated with Increased BACE-1 and Neprilysin Activities.
Down Syndrome
Activation of the Notch pathway in Down syndrome: cross-talk of Notch and APP.
Down Syndrome
Alzheimer's disease skin fibroblasts selectively express a bradykinin signaling pathway mediating tau protein Ser phosphorylation.
Down Syndrome
Alzheimer's-related endosome dysfunction in Down syndrome is Abeta-independent but requires APP and is reversed by BACE-1 inhibition.
Down Syndrome
Association between presenilin-1 -48C/T polymorphism and Down's syndrome.
Down Syndrome
Association between presenilin-1 polymorphism and maternal meiosis II errors in Down syndrome.
Down Syndrome
Association of variants within APOE, SORL1, RUNX1, BACE1 and ALDH18A1 with dementia in Alzheimer's disease in subjects with Down syndrome.
Down Syndrome
Characterization of a mouse model overexpressing beta-site APP-cleaving enzyme 2 reveals a new role for BACE2.
Down Syndrome
Chromosome missegregation and trisomy 21 mosaicism in Alzheimer's disease.
Down Syndrome
Combined association of Presenilin-1 and Apolipoprotein E polymorphisms with maternal meiosis II error in Down syndrome births.
Down Syndrome
Down syndrome and beta-amyloid deposition.
Down Syndrome
Dyrk1A-mediated phosphorylation of Presenilin 1: a functional link between Down syndrome and Alzheimer's disease.
Down Syndrome
Elevated expression of beta-site amyloid precursor protein cleaving enzyme 2 in brains of patients with Down syndrome.
Down Syndrome
Exploring the Pathogenesis of Alzheimer Disease in Basal Forebrain Cholinergic Neurons: Converging Insights From Alternative Hypotheses.
Down Syndrome
Expression Profiling of Notch Signalling Pathway and Gamma-Secretase Activity in the Brain of Ts1Cje Mouse Model of Down Syndrome.
Down Syndrome
Hypoxia facilitates Alzheimer's disease pathogenesis by up-regulating BACE1 gene expression.
Down Syndrome
In vivo effects of APP are not exacerbated by BACE2 co-overexpression: behavioural characterization of a double transgenic mouse model.
Down Syndrome
Increased BACE1 maturation contributes to the pathogenesis of Alzheimer's disease in Down syndrome.
Down Syndrome
Inhibition of APP gamma-secretase restores Sonic Hedgehog signaling and neurogenesis in the Ts65Dn mouse model of Down syndrome.
Down Syndrome
Insights from modeling the tertiary structure of human BACE2.
Down Syndrome
Long-term effect of neonatal inhibition of APP gamma-secretase on hippocampal development in the Ts65Dn mouse model of Down syndrome.
Down Syndrome
Partial BACE1 reduction in a Down syndrome mouse model blocks Alzheimer-related endosomal anomalies and cholinergic neurodegeneration: role of APP-CTF.
Down Syndrome
Presenilin 1 and alpha-1-antichymotrypsin polymorphisms in Down syndrome: no effect on the presence of dementia.
Down Syndrome
Presenilin-1 exists in the axoplasm fraction in the brains of aged Down's syndrome subjects and non-demented individuals.
Down Syndrome
Protein expression of BACE1, BACE2 and APP in Down syndrome brains.
Down Syndrome
The possible effect of microRNA-155 (miR-155) and BACE1 inhibitors in the memory of patients with down syndrome and Alzheimer's disease: Design, synthesis, virtual screening, molecular modeling and biological evaluations.
Down Syndrome
Upregulation of SET Expression by BACE1 and its Implications in Down Syndrome.
Dysarthria
Dementia, pyramidal system involvement, and leukoencephalopathy with a presenilin 1 mutation.
Dysarthria
Novel insertional presenilin 1 mutation causing Alzheimer disease with spastic paraparesis.
Dystonia
Novel insertional presenilin 1 mutation causing Alzheimer disease with spastic paraparesis.
Emergence Delirium
Correlation of Serum BACE1 With Emergence Delirium in Postoperative Patients: A Preliminary Study.
Encephalitis
Gallic Acid is a Dual ?/?-Secretase Modulator that Reverses Cognitive Impairment and Remediates Pathology in Alzheimer Mice.
Encephalomyelitis
Inhibition of Notch signaling enhances tissue repair in an animal model of multiple sclerosis.
Encephalomyelitis
Inhibitors of gamma-secretase block in vivo and in vitro T helper type 1 polarization by preventing Notch upregulation of Tbx21.
Encephalomyelitis
Notch3 inhibition in myelin-reactive T cells down-regulates protein kinase Ctheta and attenuates experimental autoimmune encephalomyelitis.
Encephalomyelitis
Overcoming failure to repair demyelination in EAE: gamma-secretase inhibition of Notch signaling.
Encephalomyelitis
Presenilin1 regulates Th1 and Th17 effector responses but is not required for experimental autoimmune encephalomyelitis.
Encephalomyelitis, Autoimmune, Experimental
Inhibition of Notch signaling enhances tissue repair in an animal model of multiple sclerosis.
Encephalomyelitis, Autoimmune, Experimental
Inhibitors of gamma-secretase block in vivo and in vitro T helper type 1 polarization by preventing Notch upregulation of Tbx21.
Encephalomyelitis, Autoimmune, Experimental
Notch3 inhibition in myelin-reactive T cells down-regulates protein kinase Ctheta and attenuates experimental autoimmune encephalomyelitis.
Encephalomyelitis, Autoimmune, Experimental
Overcoming failure to repair demyelination in EAE: gamma-secretase inhibition of Notch signaling.
Encephalomyelitis, Autoimmune, Experimental
Presenilin1 regulates Th1 and Th17 effector responses but is not required for experimental autoimmune encephalomyelitis.
Ependymoma
Candidate genes on chromosome 9q33-34 involved in the progression of childhood ependymomas.
Epilepsy
Alzheimer-like amyloid and tau alterations associated with cognitive deficit in temporal lobe epilepsy.
Epilepsy
Atypical presentation of a novel Presenilin 1 R377W mutation: sporadic, late-onset Alzheimer disease with epilepsy and frontotemporal atrophy.
Epilepsy
BACE1 deficiency causes altered neuronal activity and neurodegeneration.
Epilepsy
BACE1 elevation is associated with aberrant limbic axonal sprouting in epileptic CD1 mice.
Epilepsy
CA1 hippocampal neuronal loss in familial Alzheimer's disease presenilin-1 E280A mutation is related to epilepsy.
Epilepsy
Expression analysis of beta-secretase 1 (BACE1) and its naturally occurring antisense (BACE1-AS) in blood of epileptic patients.
Epilepsy
Presenilin-1 mutation Alzheimer's disease: a genetic epilepsy syndrome?
Epilepsy, Temporal Lobe
Alzheimer-like amyloid and tau alterations associated with cognitive deficit in temporal lobe epilepsy.
Epilepsy, Temporal Lobe
BACE1 elevation is associated with aberrant limbic axonal sprouting in epileptic CD1 mice.
Fatty Liver
Neuronal human BACE1 knockin induces systemic diabetes in mice.
Fibromatosis, Aggressive
Nirogacestat suppresses RANKL-Induced osteoclast formation in vitro and attenuates LPS-Induced bone resorption in vivo.
Fibromatosis, Aggressive
Safety and efficacy of gamma-secretase inhibitor nirogacestat (PF-03084014) in desmoid tumor: Report of four pediatric/young adult cases.
Frontotemporal Dementia
A presenilin 1 mutation associated with familial frontotemporal dementia inhibits gamma-secretase cleavage of APP and notch.
Frontotemporal Dementia
Alternative transcripts of presenilin-1 associated with frontotemporal dementia.
Frontotemporal Dementia
Biochemical and Morphological Characterization of the A?PP/PS/Tau Triple Transgenic Mouse Model and Its Relevance to Sporadic Alzheimer's Disease.
Frontotemporal Dementia
Comparing test-specific distress of susceptibility versus deterministic genetic testing for Alzheimer's disease.
Frontotemporal Dementia
Dementia mimicking Alzheimer's disease Owing to a tau mutation: CSF and PET findings.
Frontotemporal Dementia
Differential distribution of presenilin-1, Bax, and Bcl-X(L) in Alzheimer's disease and frontotemporal dementia.
Frontotemporal Dementia
Early onset autosomal dominant dementia with ataxia, extrapyramidal features, and epilepsy.
Frontotemporal Dementia
Familial frontotemporal dementia associated with a novel presenilin-1 mutation.
Frontotemporal Dementia
Familial frontotemporal dementia-associated presenilin-1 c.548G>T mutation causes decreased mRNA expression and reduced presenilin function in knock-in mice.
Frontotemporal Dementia
Las noticias de Madrid (News from Madrid).
Frontotemporal Dementia
Mutations in progranulin explain atypical phenotypes with variants in MAPT.
Frontotemporal Dementia
Presenilin-1 Mutations in Alzheimer's Disease: An Update on Genotype-Phenotype Relationships.
Frontotemporal Dementia
Presenilin/gamma-Secretase and Inflammation.
Frontotemporal Lobar Degeneration
Targeting mRNA for Alzheimer's and related dementias.
Genetic Diseases, Inborn
EEG and Granular Osmiophilic Elements in Early-Onset Alzheimer's Disease.
Glioblastoma
?-secretase inhibitor-I enhances radiosensitivity of glioblastoma cell lines by depleting CD133+ tumor cells.
Glioblastoma
Alpha-secretase inhibition reduces human glioblastoma stem cell growth in vitro and in vivo by inhibiting Notch.
Glioblastoma
Alterations in cellular metabolome after pharmacological inhibition of Notch in glioblastoma cells.
Glioblastoma
Gamma-secretase inhibitor DAPT suppresses glioblastoma growth via uncoupling of tumor vessel density from vessel function.
Glioblastoma
gamma-Secretase is differentially modulated by alterations of homocysteine cycle in neuroblastoma and glioblastoma cells.
Glioblastoma
MicroRNA-339-5p down-regulates protein expression of ?-site amyloid precursor protein-cleaving enzyme 1 (BACE1) in human primary brain cultures and is reduced in brain tissue specimens of Alzheimer disease subjects.
Glioblastoma
Putative function of ADAM9, ADAM10, and ADAM17 as APP alpha-secretase.
Glioma
A computational guided, functional validation of a novel therapeutic antibody proposes Notch signaling as a clinical relevant and druggable target in glioma.
Glioma
Analysis of presenilin 1 and presenilin 2 expression and processing by newly developed monoclonal antibodies.
Glioma
Characterization of detergent-insoluble complexes containing the familial Alzheimer's disease-associated presenilins.
Glioma
Gamma-secretase inhibitors enhance temozolomide treatment of human gliomas by inhibiting neurosphere repopulation and xenograft recurrence.
Glioma
Gamma-secretase represents a therapeutic target for the treatment of invasive glioma mediated by the p75 neurotrophin receptor.
Glioma
Gene expression analyses to explore the biomarkers and therapeutic targets for gliomas.
Glioma
Notch promotes radioresistance of glioma stem cells.
Glioma
Wild-type TP53 defined gamma-secretase inhibitor sensitivity and synergistic activity with doxorubicin in GSCs.
Glucose Intolerance
Neuronal human BACE1 knockin induces systemic diabetes in mice.
Glucose Intolerance
Susceptibility to diet-induced obesity and glucose intolerance in the APP (SWE)/PSEN1 (A246E) mouse model of Alzheimer's disease is associated with increased brain levels of protein tyrosine phosphatase 1B (PTP1B) and retinol-binding protein 4 (RBP4), and basal phosphorylation of S6 ribosomal protein.
Granulosa Cell Tumor
Effects of an inhibitor of the gamma-secretase complex on proliferation and apoptotic parameters in a FOXL2-mutated granulosa tumor cell line (KGN).
Head Injuries, Closed
Increased expression of the gamma-secretase components presenilin-1 and nicastrin in activated astrocytes and microglia following traumatic brain injury.
Hearing Loss
?-secretase BACE1 is required for normal cochlear function.
Hearing Loss, Noise-Induced
Therapeutic potential of a gamma-secretase inhibitor for hearing restoration in a guinea pig model with noise-induced hearing loss.
Hearing Loss, Sensorineural
Therapeutic potential of a gamma-secretase inhibitor for hearing restoration in a guinea pig model with noise-induced hearing loss.
Heart Failure
BACE1 levels are elevated in congestive heart failure.
Heart Failure
Cardiac adenovirus-associated viral Presenilin 1 gene delivery protects the left ventricular function of the heart via regulating RyR2 function in post-ischaemic heart failure.
Heart Septal Defects, Ventricular
Presenilin-1 Polymorphisms Are Not Relevant in Susceptibility to Ventricular Septal Defect: A Case-Control Study.
Hemangioma
Expression of HES and HEY genes in infantile hemangiomas.
Hematologic Neoplasms
Characterization of an atypical gamma-secretase complex from hematopoietic origin.
Hepatitis C
Signal peptide peptidase dependent cleavage of type II transmembrane substrates releases intracellular and extracellular signals.
Hernia, Umbilical
Presenilin genes are downregulated during somitogenesis in the cadmium-induced omphalocele chick model.
Herpes Simplex
Alzheimer's Disease: APP, Gamma Secretase, APOE, CLU, CR1, PICALM, ABCA7, BIN1, CD2AP, CD33, EPHA1, and MS4A2, and Their Relationships with Herpes Simplex, C. Pneumoniae, Other Suspect Pathogens, and the Immune System.
Herpes Simplex
Overexpression in neurons of human presenilin-1 or a presenilin-1 familial Alzheimer disease mutant does not enhance apoptosis.
Herpes Zoster
The role of intestinal endotoxemia in a rat model of aluminum neurotoxicity.
Hidradenitis Suppurativa
A new nonsense mutation in the POGLUT1 gene in two sisters with Dowling-Degos disease.
Hidradenitis Suppurativa
Gamma-secretase gene mutations link acne inversa (flexural, scarring acne) with Alzheimer's disease.
Hidradenitis Suppurativa
Genetic variations in gamma-secretase and PSTPIP1 in hidradenitis suppurativa in Singaporean Chinese.
Hidradenitis Suppurativa
Hidradenitis suppurativa: haploinsufficiency of gamma-secretase components does not affect gamma-secretase enzyme activity in vitro.
Hidradenitis Suppurativa
In silico Analysis of Gamma-Secretase-Complex Mutations in Hidradenitis Suppurativa Demonstrates Disease-Specific Substrate Recognition and Cleavage Alterations.
Hidradenitis Suppurativa
Low prevalence of gamma-secretase complex gene mutations in a large cohort of predominantly Caucasian patients with Hidradenitis Suppurativa.
Hidradenitis Suppurativa
PRESENILIN 1 Mutations Causing Early-Onset Familial Alzheimer's Disease or Familial Acne Inversa Differ in Their Effects on Genes Facilitating Energy Metabolism and Signal Transduction.
Hidradenitis Suppurativa
The possible association of hidradenitis suppurativa and Down syndrome: is increased APP expression resulting in impaired Notch signaling the missing link?
Hirschsprung Disease
Identification of Genes Associated with Hirschsprung Disease, Based on Whole-genome Sequence Analysis, and Potential Effects on Enteric Nervous System Development.
HIV Infections
Nanolipidic particles improve the bioavailability and alpha-secretase inducing ability of epigallocatechin-3-gallate (EGCG) for the treatment of Alzheimer's disease.
Huntington Disease
Apolipoprotein E and presenilin-1 genotypes in Huntington's disease.
Huntington Disease
Geriatric neurogenetics: oxymoron or reality?
Huntington Disease
Quantitative interaction proteomics of neurodegenerative disease proteins.
Hydrocephalus
Analysis of apolipoprotein E, alpha1-antichymotrypsin and presenilin-1 genes polymorphisms in dementia caused by normal pressure hydrocephalus in man.
Hydrocephalus
Hydrocephalus and abnormal subcommissural organ in mice lacking presenilin-1 in Wnt1 cell lineages.
Hydrocephalus, Normal Pressure
Analysis of apolipoprotein E, alpha1-antichymotrypsin and presenilin-1 genes polymorphisms in dementia caused by normal pressure hydrocephalus in man.
Hyperalgesia
miR-15b mediates oxaliplatin-induced chronic neuropathic pain through BACE1 down-regulation.
Hypercholesterolemia
Association analysis of genes involved in cholesterol metabolism located within the linkage region on chromosome 10 and Alzheimer's disease.
Hypercholesterolemia
Regulation of beta-amyloid levels in the brain of cholesterol-fed rabbit, a model system for sporadic Alzheimer's disease.
Hyperglycemia
Amyloid-? Production: Major Link Between Oxidative Stress and BACE1.
Hyperglycemia
Contribution of genetic and dietary insulin resistance to Alzheimer phenotype in APP/PS1 transgenic mice.
Hyperglycemia
Elevated circulating amyloid concentrations in obesity and diabetes promote vascular dysfunction.
Hyperglycemia
Pioglitazone ameliorates memory deficits in streptozotocin-induced diabetic mice by reducing brain ?-amyloid through PPAR? activation.
Hyperglycemia
PPAR? Agonist Pioglitazone Reverses Memory Impairment and Biochemical Changes in a Mouse Model of Type 2 Diabetes Mellitus.
Hyperglycemia
Telmisartan Treatment Ameliorates Memory Deficits in Streptozotocin-Induced Diabetic Mice via Attenuating Cerebral Amyloidosis.
Hyperhomocysteinemia
Hyperhomocysteinemia increases beta-amyloid by enhancing expression of gamma-secretase and phosphorylation of amyloid precursor protein in rat brain.
Hyperhomocysteinemia
S-adenosylmethionine reduces the progress of the Alzheimer-like features induced by B-vitamin deficiency in mice.
Hyperlipidemias
Elevated circulating amyloid concentrations in obesity and diabetes promote vascular dysfunction.
Hyperlipidemias
Hyperlipidemia-induced apoptosis of hippocampal neurons in apoE(-/-) mice may be associated with increased PCSK9 expression.
Hyperlipidemias
Polymorphisms of presenilin-1 gene associate with dilated cardiomyopathy susceptibility.
Hyperlipidemias
PPAR? Agonist Pioglitazone Reverses Memory Impairment and Biochemical Changes in a Mouse Model of Type 2 Diabetes Mellitus.
Hypersensitivity
Premature death in transgenic mice that overexpress a mutant amyloid precursor protein is preceded by severe neurodegeneration and apoptosis.
Hypertension
Hypertension accelerates the progression of Alzheimer-like pathology in a mouse model of the disease.
Hypertension, Pulmonary
Notch3 signaling promotes the development of pulmonary arterial hypertension.
Hypertension, Pulmonary
Propylthiouracil Attenuates Experimental Pulmonary Hypertension via Suppression of Pen-2, a Key Component of Gamma-Secretase.
hypoxanthine phosphoribosyltransferase deficiency
Correction: HPRT Deficiency Coordinately Dysregulates Canonical Wnt and Presenilin-1 Signaling: A Neuro-Developmental Regulatory Role for a Housekeeping Gene?
hypoxanthine phosphoribosyltransferase deficiency
HPRT deficiency coordinately dysregulates canonical Wnt and presenilin-1 signaling: a neuro-developmental regulatory role for a housekeeping gene?
Hypoxia, Brain
miR-124 Regulates the Expression of BACE1 in the Hippocampus Under Chronic Cerebral Hypoperfusion.
Infarction, Middle Cerebral Artery
Caspase inhibition attenuates accumulation of beta-amyloid by reducing beta-secretase production and activity in rat brains after stroke.
Infections
Astrocytes infected with Chlamydia pneumoniae demonstrate altered expression and activity of secretases involved in the generation of ?-amyloid found in Alzheimer disease.
Infections
Author Correction: HIV-1 counteracts an innate restriction by amyloid precursor protein resulting in neurodegeneration.
Infections
Cleavage and Sub-Cellular Redistribution of Nuclear Pore Protein 98 by Coxsackievirus B3 Protease 2A Impairs Cardioprotection.
Infections
Correlation between HIV-1 seropositivity and prevalence of a gamma-secretase polymorphism in two distinct ethnic populations.
Infections
Ets transcription factors ER81 and Elk1 regulate the transcription of the human presenilin 1 gene promoter.
Infections
FTY720 Attenuates Infection-Induced Enhancement of A? Accumulation in APP/PS1 Mice by Modulating Astrocytic Activation.
Infections
Presence of presenilin 1/2 affects the invasion and replication of Salmonella typhimurium.
Infections
Regulation of transcription of the human presenilin-1 gene by ets transcription factors and the p53 protooncogene.
Infections
Signal peptide peptidase dependent cleavage of type II transmembrane substrates releases intracellular and extracellular signals.
Insulin Resistance
Adipocyte-specific blockade of gamma-secretase, but not inhibition of Notch activity, reduces adipose insulin sensitivity.
Insulin Resistance
Altered amyloid precursor protein processing regulates glucose uptake and oxidation in cultured rodent myotubes.
Insulin Resistance
Alzheimer's disease And Diabetes: New Insights and Unifying Therapies.
Insulin Resistance
Amyloid-? Induces Hepatic Insulin Resistance In Vivo via JAK2.
Insulin Resistance
Associations of Plasma BACE1 Level and BACE1 C786G Gene Polymorphism with Cognitive Functions in Patients with Type 2 Diabetes: A Cross- Sectional Study.
Insulin Resistance
Biomarkers of Alzheimer disease, insulin resistance, and obesity in childhood.
Insulin Resistance
Can Ketones Help Rescue Brain Fuel Supply in Later Life? Implications for Cognitive Health during Aging and the Treatment of Alzheimer's Disease.
Insulin Resistance
Dicer1-miR-328-Bace1 signalling controls brown adipose tissue differentiation and function.
Insulin Resistance
Diet-induced insulin resistance promotes amyloidosis in a transgenic mouse model of Alzheimer's disease.
Insulin Resistance
Expression of ?-site APP-cleaving enzyme 1 in the hippocampal tissue of an insulin-resistant rat model of Alzheimer's disease.
Insulin Resistance
Increased ?-site APP cleaving enzyme 1-mediated insulin receptor cleavage in type 2 diabetes mellitus with cognitive impairment.
Insulin Resistance
Reduction in BACE1 decreases body weight, protects against diet-induced obesity and enhances insulin sensitivity in mice.
Insulin Resistance
Susceptibility to diet-induced obesity and glucose intolerance in the APP (SWE)/PSEN1 (A246E) mouse model of Alzheimer's disease is associated with increased brain levels of protein tyrosine phosphatase 1B (PTP1B) and retinol-binding protein 4 (RBP4), and basal phosphorylation of S6 ribosomal protein.
Insulin Resistance
The BACE1 inhibitor LY2886721 improves diabetic phenotypes of BACE1 knock-in mice.
Insulin Resistance
The BACE1 product sAPP? induces ER stress and inflammation and impairs insulin signaling.
Insulin Resistance
Toward prevention of Alzheimers disease--potential nutraceutical strategies for suppressing the production of amyloid beta peptides.
Intellectual Disability
Delta-catenin is required for the maintenance of neural structure and function in mature cortex in vivo.
Intellectual Disability
GSK-3 phosphorylates delta-catenin and negatively regulates its stability via ubiquitination/proteosome-mediated proteolysis.
Iron Overload
The Effect of TCM-Induced HAMP on Key Enzymes in the Hydrolysis of AD Model Cells.
Ischemic Attack, Transient
Increased beta-secretase activity and expression in rats following transient cerebral ischemia.
Ischemic Stroke
Gamma secretase-mediated Notch signaling worsens brain damage and functional outcome in ischemic stroke.
Kidney Diseases
The Notch pathway in podocytes plays a role in the development of glomerular disease.
Leishmaniasis, Cutaneous
Inhibition of gamma-secretase activity without interfering in Notch signalling decreases inflammatory response in patients with cutaneous leishmaniasis.
Leukemia
Effects of gamma-secretase inhibitors on the growth of leukemia cells.
Leukemia
Gamma Secretase Inhibitor: Therapeutic Target via NOTCH Signaling in T cell Acute Lymphoblastic Leukemia.
Leukemia
Gamma-secretase inhibitors induce erythroid differentiation in erythroid leukemia cell lines.
Leukemia
Gamma-secretase inhibitors suppress the growth of leukemia and lymphoma cells.
Leukemia
Inhibition of angiogenesis and tumor growth by beta and gamma-secretase inhibitors.
Leukemia
Inhibition of gamma-secretase affects proliferation of leukemia and hepatoma cell lines through Notch signaling.
Leukemia
Mutational loss of PTEN induces resistance to NOTCH1 inhibition in T-cell leukemia.
Leukemia
NOTCH1-RBPJ complexes drive target gene expression through dynamic interactions with superenhancers.
Leukemia
Safe targeting of T cell acute lymphoblastic leukemia by pathology-specific NOTCH inhibition.
Leukemia
The relevance of PTEN-AKT in relation to NOTCH1-directed treatment strategies in T-cell acute lymphoblastic leukemia.
Leukemia
[Inhibitors for Notch and gamma-secretase. Biology of T-cell leukemia]
Leukemia, Lymphoid
Nutlin-3 up-regulates the expression of Notch1 in both myeloid and lymphoid leukemic cells, as part of a negative feedback antiapoptotic mechanism.
Leukemia, T-Cell
Notch signals positively regulate activity of the mTOR pathway in T-cell acute lymphoblastic leukemia.
Leukemia, T-Cell
[Inhibitors for Notch and gamma-secretase. Biology of T-cell leukemia]
Leukoencephalopathies
Beta-Secretase 1 Underlies Reactive Astrocytes and Endothelial Disruption in Neurodegeneration.
Leukoencephalopathies
Dementia, pyramidal system involvement, and leukoencephalopathy with a presenilin 1 mutation.
Lewy Body Disease
Enhanced accumulation of phosphorylated alpha-synuclein and elevated beta-amyloid 42/40 ratio caused by expression of the presenilin-1 deltaT440 mutant associated with familial Lewy body disease and variant Alzheimer's disease.
Lissencephaly
Altered morphological and electrophysiological properties of Cajal-Retzius cells in cerebral cortex of embryonic Presenilin-1 knockout mice.
Lissencephaly
Presenilin-1 deficiency leads to loss of Cajal-Retzius neurons and cortical dysplasia similar to human type 2 lissencephaly.
Lung Neoplasms
Gamma-secretase inhibitor prevents Notch3 activation and reduces proliferation in human lung cancers.
Lung Neoplasms
MiR-574-3p accelerates cell migration and invasion through regulating BACE1 in Non-Small Cell Lung Cancer.
Lung Neoplasms
Rethinking Gamma-secretase Inhibitors for Treatment of Non-small-Cell Lung Cancer: Is Notch the Target?
Lymphoma
Gamma-secretase inhibitors suppress the growth of leukemia and lymphoma cells.
Lymphoma
Inhibition of KSHV infected primary effusion lymphomas in NOD/SCID mice by gamma-secretase inhibitor.
Lymphoma
Mutational loss of PTEN induces resistance to NOTCH1 inhibition in T-cell leukemia.
Lymphoma, B-Cell
Establishment of a novel B-cell lymphoma cell line with suppressed growth by gamma-secretase inhibitors.
Lymphoma, B-Cell
Notch-regulation upon Dll4-stimulation of TGFb-induced apoptosis and gene expression in human B-cell non-Hodgkin lymphomas.
Lymphoma, Primary Effusion
Inhibition of KSHV infected primary effusion lymphomas in NOD/SCID mice by gamma-secretase inhibitor.
Lymphoma, T-Cell
CUTLL1, a novel human T-cell lymphoma cell line with t(7;9) rearrangement, aberrant NOTCH1 activation and high sensitivity to gamma-secretase inhibitors.
Macular Degeneration
?-Secretase (BACE1) inhibition causes retinal pathology by vascular dysregulation and accumulation of age pigment.
Macular Degeneration
Approaches for detecting lysosomal alkalinization and impaired degradation in fresh and cultured RPE cells: evidence for a role in retinal degenerations.
Malaria
The zymogen of plasmepsin V from Plasmodium falciparum is enzymatically active.
Malformations of Cortical Development
Altered morphological and electrophysiological properties of Cajal-Retzius cells in cerebral cortex of embryonic Presenilin-1 knockout mice.
Malformations of Cortical Development
Presenilin 1 in migration and morphogenesis in the central nervous system.
Malformations of Cortical Development
Presenilin-1 deficiency leads to loss of Cajal-Retzius neurons and cortical dysplasia similar to human type 2 lissencephaly.
Malformations of Cortical Development, Group II
The function of presenilin-1 in amyloid beta-peptide generation and brain development.
Malnutrition
S-adenosyl methionine: A connection between nutritional and genetic risk factors for neurodegeneration in Alzheimer's disease.
Medulloblastoma
Inhibition of neurotrophin receptor p75 intramembran proteolysis by gamma-secretase inhibitor reduces medulloblastoma spinal metastasis.
Medulloblastoma
Notch pathway inhibition depletes stem-like cells and blocks engraftment in embryonal brain tumors.
Melanoma
Long-Term Inhibition of Notch in A-375 Melanoma Cells Enhances Tumor Growth Through the Enhancement of AXIN1, CSNK2A3, and CEBPA2 as Intermediate Genes in Wnt and Notch Pathways.
Melanoma
Notch and NOXA-related pathways in melanoma cells.
Melanoma
p53-independent NOXA induction overcomes apoptotic resistance of malignant melanomas.
Melanoma
Phase 2 study of RO4929097, a gamma-secretase inhibitor, in metastatic melanoma: SWOG 0933.
memapsin 2 deficiency
?-site amyloid precursor protein (APP) cleaving enzyme 1 (BACE1) deficient mice exhibit a close homolog of L1 (CHL1) loss-of-function phenotype involving axon guidance defects.
memapsin 2 deficiency
Alzheimer's disease neurons fail the acid test.
memapsin 2 deficiency
Axonal and Schwann Cell BACE1 Is Equally Required for Remyelination of Peripheral Nerves.
memapsin 2 deficiency
Axonal organization defects in the hippocampus of adult conditional BACE1 knockout mice.
memapsin 2 deficiency
BACE1 controls synaptic function through modulating release of synaptic vesicles.
memapsin 2 deficiency
BACE1 Deficiency Causes Abnormal Neuronal Clustering in the Dentate Gyrus.
memapsin 2 deficiency
BACE1 deficiency causes altered neuronal activity and neurodegeneration.
memapsin 2 deficiency
BACE1 deficiency rescues memory deficits and cholinergic dysfunction in a mouse model of Alzheimer's disease.
memapsin 2 deficiency
BACE1 regulates the proliferation and cellular functions of Schwann cells.
memapsin 2 deficiency
BACE1-/- mice exhibit seizure activity that does not correlate with sodium channel level or axonal localization.
memapsin 2 deficiency
Editorial: Implications for BACE1 Inhibitor Clinical Trials: Adult Conditional BACE1 Knockout Mice Exhibit Axonal Organization Defects in the Hippocampus.
memapsin 2 deficiency
Phenotypic and biochemical analyses of BACE1- and BACE2-deficient mice.
memapsin 2 deficiency
Presenilin 1 deficiency alters the activity of voltage-gated Ca2+ channels in cultured cortical neurons.
memapsin 2 deficiency
Presenilin 1 deficiency suppresses autophagy in human neural stem cells through reducing ?-secretase-independent ERK/CREB signaling.
memapsin 2 deficiency
Presenilin 2 deficiency causes a mild pulmonary phenotype and no changes in amyloid precursor protein processing but enhances the embryonic lethal phenotype of presenilin 1 deficiency.
memapsin 2 deficiency
Presenilin-1 deficiency impairs glutamate-evoked intracellular calcium responses in neurons.
memapsin 2 deficiency
Presenilin-1 deficiency leads to loss of Cajal-Retzius neurons and cortical dysplasia similar to human type 2 lissencephaly.
memapsin 2 deficiency
Presenilins: molecular switches between proteolysis and signal transduction.
memapsin 2 deficiency
Reversing hypomyelination in BACE1-null mice with Akt-DD overexpression.
Memory Disorders
7,8-dihydroxyflavone, a small-molecule TrkB agonist, reverses memory deficits and BACE1 elevation in a mouse model of Alzheimer's disease.
Memory Disorders
?-Asarone Mitigates Amyloidosis and Downregulates RAGE in a Transgenic Mouse Model of Alzheimer's Disease.
Memory Disorders
A combination Alzheimer's therapy targeting BACE1 and neprilysin in 5XFAD transgenic mice.
Memory Disorders
Alzheimer's therapy targeting the ?-secretase enzyme BACE1: Benefits and potential limitations from the perspective of animal model studies.
Memory Disorders
Amyloid suppresses induction of genes critical for memory consolidation in APP + PS1 transgenic mice.
Memory Disorders
BACE1 deficiency rescues memory deficits and cholinergic dysfunction in a mouse model of Alzheimer's disease.
Memory Disorders
BACE1 gene deletion prevents neuron loss and memory deficits in 5XFAD APP/PS1 transgenic mice.
Memory Disorders
BACE1 gene deletion: impact on behavioral function in a model of Alzheimer's disease.
Memory Disorders
BACE1 inhibition by microdose lithium formulation NP03 rescues memory loss and early stage amyloid neuropathology.
Memory Disorders
BACE1, a major determinant of selective vulnerability of the brain to amyloid-beta amyloidogenesis, is essential for cognitive, emotional, and synaptic functions.
Memory Disorders
BAG-1M co-activates BACE1 transcription through NF-?B and accelerates A? production and memory deficit in Alzheimer's disease mouse model.
Memory Disorders
Beneficial effects of the ?-secretase inhibitor GRL-8234 in 5XFAD Alzheimer's transgenic mice lessen during disease progression.
Memory Disorders
CHF5074, a novel gamma-secretase modulator, restores hippocampal neurogenesis potential and reverses contextual memory deficit in a transgenic mouse model of Alzheimer's disease.
Memory Disorders
Deletion of the Cathepsin B Gene Improves Memory Deficits in a Transgenic Alzheimer's Disease Mouse Model Expressing A?PP Containing the Wild-Type ?-Secretase Site Sequence.
Memory Disorders
Deletion of the eIF2? Kinase GCN2 fails to rescue the memory decline associated with Alzheimer's disease.
Memory Disorders
Deletion of tumor necrosis factor death receptor inhibits amyloid beta generation and prevents learning and memory deficits in Alzheimer's mice.
Memory Disorders
Depletion of Caveolin-1 in Type-2 Diabetes Model Induces Alzheimer's disease Pathology Precursors.
Memory Disorders
Effects of BACE1 haploinsufficiency on APP processing and A? concentrations in male and female 5XFAD Alzheimer mice at different disease stages.
Memory Disorders
Electroacupuncture Ameliorates Neuroinflammation-Mediated Cognitive Deficits through Inhibition of NLRP3 in Presenilin1/2 Conditional Double Knockout Mice.
Memory Disorders
Enhanced activity of hippocampal BACE1 in a mouse model of postmenopausal memory deficits.
Memory Disorders
FGF2 gene transfer restores hippocampal functions in mouse models of Alzheimer's disease and has therapeutic implications for neurocognitive disorders.
Memory Disorders
Gastrodin suppresses BACE1 expression under oxidative stress condition via inhibition of the PKR/eIF2? pathway in Alzheimer's disease.
Memory Disorders
Genetic and pharmacological basis for therapeutic inhibition of beta- and gamma-secretases in mouse models of Alzheimer's memory deficits.
Memory Disorders
Hyperhomocysteinemia increases beta-amyloid by enhancing expression of gamma-secretase and phosphorylation of amyloid precursor protein in rat brain.
Memory Disorders
Indirubin-3'-monoxime rescues spatial memory deficits and attenuates beta-amyloid-associated neuropathology in a mouse model of Alzheimer's disease.
Memory Disorders
Inhibition of GSK3?-mediated BACE1 expression reduces Alzheimer-associated phenotypes.
Memory Disorders
Lack of BACE1 S-palmitoylation reduces amyloid burden and mitigates memory deficits in transgenic mouse models of Alzheimer's disease.
Memory Disorders
Long-term oral melatonin alleviates memory deficits, reduces amyloid-? deposition associated with downregulation of BACE1 and mitophagy in APP/PS1 transgenic mice.
Memory Disorders
Marginal vitamin A deficiency facilitates Alzheimer's pathogenesis.
Memory Disorders
Mechanisms that lessen benefits of ?-secretase reduction in a mouse model of Alzheimer's disease.
Memory Disorders
miRNA-31 Improves Cognition and Abolishes Amyloid-? Pathology by Targeting APP and BACE1 in an Animal Model of Alzheimer's Disease.
Memory Disorders
Overexpression of human apolipoprotein A-I preserves cognitive function and attenuates neuroinflammation and cerebral amyloid angiopathy in a mouse model of Alzheimer's disease.
Memory Disorders
Partial reduction of BACE1 improves synaptic plasticity, recent and remote memories in Alzheimer's disease transgenic mice.
Memory Disorders
Phospho-eIF2? level is important for determining abilities of BACE1 reduction to rescue cholinergic neurodegeneration and memory defects in 5XFAD mice.
Memory Disorders
Picrorhiza kurroa Prevents Memory Deficits by Inhibiting NLRP3 Inflammasome Activation and BACE1 Expression in 5xFAD Mice.
Memory Disorders
Pioglitazone ameliorates memory deficits in streptozotocin-induced diabetic mice by reducing brain ?-amyloid through PPAR? activation.
Memory Disorders
Review of synthesis, biological assay and QSAR studies of ?-secretase inhibitors.
Memory Disorders
Selectively reduced expression of synaptic plasticity-related genes in amyloid precursor protein + presenilin-1 transgenic mice.
Memory Disorders
Synaptic activity prompts gamma-secretase-mediated cleavage of EphA4 and dendritic spine formation.
Memory Disorders
Temporal memory deficits in Alzheimer's mouse models: rescue by genetic deletion of BACE1.
Memory Disorders
The Alzheimer's disease beta-secretase enzyme, BACE1.
Memory Disorders
The Cysteine Protease Inhibitor, E64d, Reduces Brain Amyloid-? and Improves Memory Deficits in Alzheimer's Disease Animal Models by Inhibiting Cathepsin B, but not BACE1, ?-Secretase Activity.
Memory Disorders
Trans-cinnamaldehyde improves neuroinflammation-mediated NMDA receptor dysfunction and memory deficits through blocking NF-?B pathway in presenilin1/2 conditional double knockout mice.
Memory Disorders
Transcriptional regulation of the presenilin-1 gene: implication in Alzheimer's disease.
Memory Disorders
Val97Leu mutant presenilin-1 induces tau hyperphosphorylation and spatial memory deficit in mice and the underlying mechanisms.
Memory Disorders
Wharton's Jelly-derived mesenchymal stem cells alleviate memory deficits and reduce amyloid-? deposition in an APP/PS1 transgenic mouse model.
Metabolic Syndrome
Dysregulation of SREBP2 induces BACE1 expression.
Metabolic Syndrome
Las noticias de Madrid (News from Madrid).
Multiple Myeloma
Belantamab mafodotin in combination with novel agents in relapsed/refractory multiple myeloma: DREAMM-5 study design.
Multiple Myeloma
Gamma-secretase inhibitor enhances the cytotoxic effect of bortezomib in multiple myeloma.
Multiple Sclerosis
Genetic deletion of BACE1 in mice affects remyelination of sciatic nerves.
Multiple Sclerosis
Inhibitors of gamma-secretase block in vivo and in vitro T helper type 1 polarization by preventing Notch upregulation of Tbx21.
Multiple Sclerosis
Reduced cerebrospinal fluid BACE1 activity in multiple sclerosis.
Muscular Diseases
Light and electron microscopic immunolocalization of presenilin 1 in abnormal muscle fibers of patients with sporadic inclusion-body myositis and autosomal-recessive inclusion-body myopathy.
Muscular Diseases
Transgenic mice over-expressing the C-99 fragment of betaPP with an alpha-secretase site mutation develop a myopathy similar to human inclusion body myositis.
Muscular Dystrophies, Limb-Girdle
Geriatric neurogenetics: oxymoron or reality?
Myoclonus
A novel mutation (L250V) in the presenilin 1 gene in a Japanese familial Alzheimer's disease with myoclonus and generalized convulsion.
Myoclonus
A novel presenilin 1 duplication mutation (Ile168dup) causing Alzheimer's disease associated with myoclonus, seizures and pyramidal features.
Myoclonus
A systematic review of familial Alzheimer's disease: Differences in presentation of clinical features among three mutated genes and potential ethnic differences.
Myoclonus
Presenilin-1 Mutations in Alzheimer's Disease: An Update on Genotype-Phenotype Relationships.
Myositis
BACE-1, PS-1 and sAPP? levels are increased in plasma from sporadic inclusion body myositis patients: surrogate biomarkers among inflammatory myopathies.
Myositis
Increased BACE1 mRNA and noncoding BACE1-antisense transcript in sporadic inclusion-body myositis muscle fibers--possibly caused by endoplasmic reticulum stress.
Myositis
Light and electron microscopic immunolocalization of presenilin 1 in abnormal muscle fibers of patients with sporadic inclusion-body myositis and autosomal-recessive inclusion-body myopathy.
Myositis
NOGO is increased and binds to BACE1 in sporadic inclusion-body myositis and in AbetaPP-overexpressing cultured human muscle fibers.
Myositis
Presence of BACE1 and BACE2 in muscle fibres of patients with sporadic inclusion-body myositis.
Myositis
Sporadic inclusion-body myositis and its similarities to Alzheimer disease brain. Recent approaches to diagnosis and pathogenesis, and relation to aging.
Myositis
Transgenic mice over-expressing the C-99 fragment of betaPP with an alpha-secretase site mutation develop a myopathy similar to human inclusion body myositis.
Myositis, Inclusion Body
BACE-1, PS-1 and sAPP? levels are increased in plasma from sporadic inclusion body myositis patients: surrogate biomarkers among inflammatory myopathies.
Myositis, Inclusion Body
Transgenic mice over-expressing the C-99 fragment of betaPP with an alpha-secretase site mutation develop a myopathy similar to human inclusion body myositis.
Nasopharyngeal Carcinoma
Tricetin Suppresses Migration and Presenilin-1 Expression of Nasopharyngeal Carcinoma through Akt/GSK-3? Pathway.
Neoplasm Metastasis
Inhibition of neurotrophin receptor p75 intramembran proteolysis by gamma-secretase inhibitor reduces medulloblastoma spinal metastasis.
Neoplasm Metastasis
The expression of presenilin 1 enhances carcinogenesis and metastasis in gastric cancer.
Neoplasms
3,5-bis(2,4-difluorobenzylidene)-4-piperidone, a novel compound that affects pancreatic cancer growth and angiogenesis.
Neoplasms
A Miniaturized 1536-Well Format gamma-Secretase Assay *
Neoplasms
A phase Ib combination study of RO4929097, a gamma-secretase inhibitor, and temsirolimus in patients with advanced solid tumors.
Neoplasms
A phase II study of single-agent RO4929097, a gamma-secretase inhibitor of Notch signaling, in patients with recurrent platinum-resistant epithelial ovarian cancer: A study of the Princess Margaret Cancer Centre, Chicago and California phase II consortia.
Neoplasms
A secreted type of beta1,6 N-acetylglucosaminyltransferase V (GnT-V), a novel angiogenesis inducer, is regulated by gamma-secretase.
Neoplasms
Activating Notch1 mutations in mouse models of T-ALL.
Neoplasms
Activation of PPARA-mediated autophagy reduces Alzheimer disease-like pathology and cognitive decline in a murine model.
Neoplasms
ADAMs family members as amyloid precursor protein alpha-secretases.
Neoplasms
Allopregnanolone Reverses Bioenergetic Deficits in Female Triple Transgenic Alzheimer's Mouse Model.
Neoplasms
An exo-cell assay for examining real-time gamma-secretase activity and inhibition.
Neoplasms
Anti-nicastrin monoclonal antibodies elicit pleiotropic anti-tumour pharmacological effects in invasive breast cancer cells.
Neoplasms
Antimalarial Drug Artemether Inhibits Neuroinflammation in BV2 Microglia Through Nrf2-Dependent Mechanisms.
Neoplasms
Antisense Oligonucleotide Therapeutic Approach for Suppression of Ataxin-1 Expression: A Safety Assessment.
Neoplasms
Apoptosis in T cell acute lymphoblastic leukemia cells after cell cycle arrest induced by pharmacological inhibition of notch signaling.
Neoplasms
Behavioral alterations associated with apoptosis and down-regulation of presenilin 1 in the brains of p53-deficient mice.
Neoplasms
Beta-Secretase 1 (BACE1) Is Down-Regulated in Invasive Ductal Carcinoma of Breast.
Neoplasms
Bisphenol A disrupts Notch signaling by inhibiting gamma-secretase activity and causes eye dysplasia of Xenopus laevis.
Neoplasms
Bromotyrosine-derived metabolites from an Indonesian marine sponge in the family Aplysinellidae (Order Verongiida).
Neoplasms
CD40/CD40L interaction induces Abeta production and increases gamma-secretase activity independently of tumor necrosis factor receptor associated factor (TRAF) signaling.
Neoplasms
CD45 deficiency drives amyloid-? peptide oligomers and neuronal loss in Alzheimer's disease mice.
Neoplasms
Characterization of activating mutations of NOTCH3 in T-cell acute lymphoblastic leukemia and anti-leukemic activity of NOTCH3 inhibitory antibodies.
Neoplasms
Cross-talk between notch and the estrogen receptor in breast cancer suggests novel therapeutic approaches.
Neoplasms
CTL Attenuation Regulated by PS1 in Cancer-Associated Fibroblast.
Neoplasms
Down-regulation of the Notch pathway mediated by a gamma-secretase inhibitor induces anti-tumour effects in mouse models of T-cell leukaemia.
Neoplasms
Effects of an inhibitor of the gamma-secretase complex on proliferation and apoptotic parameters in a FOXL2-mutated granulosa tumor cell line (KGN).
Neoplasms
Elevated serum HER-2 predicts poor prognosis in breast cancer and is correlated to ADAM10 expression.
Neoplasms
EpCAM-associated claudin-7 supports lymphatic spread and drug resistance in rat pancreatic cancer.
Neoplasms
Epidermal Growth Factor Receptor and Notch Pathways Participate in the Tumor Suppressor Function of {gamma}-Secretase.
Neoplasms
Evaluation of selective gamma-secretase inhibitor PF-03084014 for its antitumor efficacy and gastrointestinal safety to guide optimal clinical trial design.
Neoplasms
Evidence that tumor necrosis factor alpha converting enzyme is involved in regulated alpha-secretase cleavage of the Alzheimer amyloid protein precursor.
Neoplasms
Expression of nuclear Notch3 in cervical squamous cell carcinomas and its association with adverse clinical outcomes.
Neoplasms
FBW7 mutations in leukemic cells mediate NOTCH pathway activation and resistance to gamma-secretase inhibitors.
Neoplasms
Functional characterization of novel presenilin-2 variants identified in human breast cancers.
Neoplasms
Gamma-secretase and the intramembrane proteolysis of Notch.
Neoplasms
gamma-Secretase heterogeneity in the Aph1 subunit: relevance for Alzheimer's disease.
Neoplasms
gamma-Secretase in biology and medicine.
Neoplasms
Gamma-secretase inhibition attenuates oxaliplatin-induced apoptosis through increased Mcl-1 and/or Bcl-xL in human colon cancer cells.
Neoplasms
Gamma-secretase inhibitor DAPT suppresses glioblastoma growth via uncoupling of tumor vessel density from vessel function.
Neoplasms
Gamma-secretase inhibitor treatment promotes VEGF-A-driven blood vessel growth and vascular leakage but disrupts neovascular perfusion.
Neoplasms
Gamma-secretase inhibitor, a potential target therapy for MUC2-positive colorectal carcinoma.
Neoplasms
Gamma-secretase represents a therapeutic target for the treatment of invasive glioma mediated by the p75 neurotrophin receptor.
Neoplasms
Gene expression profiling in cells with enhanced gamma-secretase activity.
Neoplasms
Green tea epigallocatechin-3-gallate (EGCG) modulates amyloid precursor protein cleavage and reduces cerebral amyloidosis in Alzheimer transgenic mice.
Neoplasms
Growth inhibitory effect of rapamycin in Hodgkin-lymphoma cell lines characterized by constitutive NOTCH1 activation.
Neoplasms
GSK-3 phosphorylates delta-catenin and negatively regulates its stability via ubiquitination/proteosome-mediated proteolysis.
Neoplasms
High activities of BACE1 in brains with mild cognitive impairment.
Neoplasms
Human ROBO1 is cleaved by metalloproteinases and gamma-secretase and migrates to the nucleus in cancer cells.
Neoplasms
Huperzine A regulates amyloid precursor protein processing via protein kinase C and mitogen-activated protein kinase pathways in neuroblastoma SK-N-SH cells over-expressing wild type human amyloid precursor protein 695.
Neoplasms
Hypoxia-inducible factor 1alpha (HIF-1alpha)-mediated hypoxia increases BACE1 expression and beta-amyloid generation.
Neoplasms
Identification of key miRNA-gene pairs in gastric cancer through integrated analysis of mRNA and miRNA microarray.
Neoplasms
Increased NF-?B signalling up-regulates BACE1 expression and its therapeutic potential in Alzheimer's disease.
Neoplasms
Increased TNFR1 expression and signaling in injured peripheral nerves of mice with reduced BACE1 activity.
Neoplasms
Inducible nitric oxide synthase up-regulates Notch-1 in mouse cholangiocytes: implications for carcinogenesis.
Neoplasms
Inhibition of ?-secretase activity by a monoclonal antibody against the extracellular hydrophilic loop of presenilin 1.
Neoplasms
Inhibition of angiogenesis and tumor growth by beta and gamma-secretase inhibitors.
Neoplasms
Inhibition of gamma-secretase activity inhibits tumor progression in a mouse model of pancreatic ductal adenocarcinoma.
Neoplasms
Inhibition of gamma-secretase by the CK1 inhibitor IC261 does not depend on CK1delta.
Neoplasms
Inhibition of presenilin 1 expression is promoted by p53 and p21WAF-1 and results in apoptosis and tumor suppression.
Neoplasms
Interleukin-1 receptor type 1 is a substrate for gamma-secretase-dependent regulated intramembrane proteolysis.
Neoplasms
Isorhynchophylline ameliorates cognitive impairment via modulating amyloid pathology, tau hyperphosphorylation and neuroinflammation: Studies in a transgenic mouse model of Alzheimer's disease.
Neoplasms
Lack of association between IDE genetic variability and Down's syndrome.
Neoplasms
Lack of replication of association findings in complex disease: an analysis of 15 polymorphisms in prior candidate genes for sporadic Alzheimer's disease.
Neoplasms
MAPK-activated protein kinase 2 deficiency in microglia inhibits pro-inflammatory mediator release and resultant neurotoxicity. Relevance to neuroinflammation in a transgenic mouse model of Alzheimer disease.
Neoplasms
Metformin may antagonize Lin28 and/or Lin28B activity, thereby boosting let-7 levels and antagonizing cancer progression.
Neoplasms
Molecular dependence of estrogen receptor-negative breast cancer on a notch-survivin signaling axis.
Neoplasms
Multiple Functional Motifs Are Required for the Tumor Suppressor Activity of a Constitutively-Active ErbB4 Mutant.
Neoplasms
Nirogacestat suppresses RANKL-Induced osteoclast formation in vitro and attenuates LPS-Induced bone resorption in vivo.
Neoplasms
NMDA receptor activation inhibits alpha-secretase and promotes neuronal amyloid-beta production.
Neoplasms
Notch inhibition in Kaposi's sarcoma tumor cells leads to mitotic catastrophe through nuclear factor-kappaB signaling.
Neoplasms
NOTCH pathway blockade depletes CD133-positive glioblastoma cells and inhibits growth of tumor neurospheres and xenografts.
Neoplasms
NOTCH signaling as a novel cancer therapeutic target.
Neoplasms
Notch signaling drives stemness and tumorigenicity of esophageal adenocarcinoma.
Neoplasms
Notch signaling in breast cancer and tumor angiogenesis: cross-talk and therapeutic potentials.
Neoplasms
Notch signaling, gamma-secretase inhibitors, and cancer therapy.
Neoplasms
Notch signalling drives bone marrow stromal cell-mediated chemoresistance in acute myeloid leukemia.
Neoplasms
Notch1 expression predicts an unfavorable prognosis and serves as a therapeutic target of patients with neuroblastoma.
Neoplasms
Notch3 cooperates with the EGFR pathway to modulate apoptosis through the induction of bim.
Neoplasms
Opposing actions of endocannabinoids on cholangiocarcinoma growth is via the differential activation of Notch signaling.
Neoplasms
Oxidation of cholesterol by amyloid precursor protein and beta-amyloid peptide.
Neoplasms
Oxygen concentration determines the biological effects of NOTCH-1 signaling in adenocarcinoma of the lung.
Neoplasms
Palmitate-activated astrocytes via serine palmitoyltransferase increase BACE1 in primary neurons by sphingomyelinases.
Neoplasms
Phase I trial of weekly MK-0752 in children with refractory central nervous system malignancies: a pediatric brain tumor consortium study.
Neoplasms
Preclinical profile of a potent gamma-secretase inhibitor targeting notch signaling with in vivo efficacy and pharmacodynamic properties.
Neoplasms
Presenilin-dependent gamma-secretase processing regulates multiple ERBB4/HER4 activities.
Neoplasms
Processing of Notch and amyloid precursor protein by gamma-secretase is spatially distinct.
Neoplasms
Protein kinase C regulation of intracellular and cell surface amyloid precursor protein (APP) cleavage in CHO695 cells.
Neoplasms
Protein processing mechanisms: from angiotensin-converting enzyme to Alzheimer's disease.
Neoplasms
Proteomic profiling of gamma-secretase substrates and mapping of substrate requirements.
Neoplasms
Rational targeting of Notch signaling in cancer.
Neoplasms
Safety and efficacy of gamma-secretase inhibitor nirogacestat (PF-03084014) in desmoid tumor: Report of four pediatric/young adult cases.
Neoplasms
Shedding of the p75NTR neurotrophin receptor is modulated by lipid rafts.
Neoplasms
T cell acute lymphoblastic leukemia/lymphoma: a human cancer commonly associated with aberrant NOTCH1 signaling.
Neoplasms
The botanical origin and antioxidant, anti-BACE1 and antiproliferative properties of bee pollen from different regions of South Korea.
Neoplasms
The emerging role of ?-secretases in cancer.
Neoplasms
The molecular programme of tumour reversion: the steps beyond malignant transformation.
Neoplasms
The novel membrane protein TMEM59 modulates complex glycosylation, cell surface expression and secretion of the amyloid precursor protein.
Neoplasms
The role of proteolysis in Alzheimer's disease.
Neoplasms
Total synthesis of the dictyodendrins as an arena to highlight emerging synthetic technologies.
Neoplasms
TRAF6 promotes TGF?-induced invasion and cell-cycle regulation via Lys63-linked polyubiquitination of Lys178 in TGF? type I receptor.
Neoplasms
Tumor necrosis factor-alpha, interleukin-1beta, and interferon-gamma stimulate gamma-secretase-mediated cleavage of amyloid precursor protein through a JNK-dependent MAPK pathway.
Neoplasms
Tumor necrosis factor-alpha-elicited stimulation of gamma-secretase is mediated by c-Jun N-terminal kinase-dependent phosphorylation of presenilin and nicastrin.
Neoplasms
Tumor reversion: mesenchymal-epithelial transition as a critical step in managing the tumor-microenvironment cross-talk.
Neoplasms
z-Leucinyl-Leucinyl-Norleucinal Induces Apoptosis of Human Glioblastoma Tumor-Initiating Cells by Proteasome Inhibition and Mitotic Arrest Response.
Neoplasms
Zebrafish lacking Alzheimer presenilin enhancer 2 (Pen-2) demonstrate excessive p53-dependent apoptosis and neuronal loss.
Nephrotic Syndrome
The pathogenic role of notch activation in podocytes.
Nervous System Diseases
An Overview of ?-Amyloid Cleaving Enzyme 1 (Bace1) in Alzheimer's Disease Therapy Elucidating its Exosite-Binding Antibody and Allosteric Inhibitor.
Nervous System Diseases
BACE1 Levels Correlate with Phospho-Tau Levels in Human Cerebrospinal Fluid.
Nervous System Diseases
Can BACE1 Inhibition Mitigate Early Axonal Pathology in Neurological Diseases?
Nervous System Diseases
MicroRNA-298 and microRNA-328 regulate expression of mouse beta-amyloid precursor protein-converting enzyme 1.
Nervous System Diseases
Piperazine-substituted chalcones: a new class of MAO-B, AChE, and BACE-1 inhibitors for the treatment of neurological disorders.
Nervous System Diseases
The Ever-Changing Morphology of Hippocampal Granule Neurons in Physiology and Pathology.
Neuralgia
miR-15b mediates oxaliplatin-induced chronic neuropathic pain through BACE1 down-regulation.
Neuroblastoma
A natural squamosamide derivative FLZ reduces amyloid-beta production by increasing non-amyloidogenic AbetaPP processing.
Neuroblastoma
A?1-42-mediated down-regulation of Uch-L1 is dependent on NF-?B activation and impaired BACE1 lysosomal degradation.
Neuroblastoma
Acetylcholinesterase inhibitors increase ADAM10 activity by promoting its trafficking in neuroblastoma cell lines.
Neuroblastoma
Activation of peroxisome proliferator-activated receptor delta suppresses BACE1 expression by up-regulating SOCS1 in a JAK2/STAT1-dependent manner.
Neuroblastoma
Acyl-coenzyme A:cholesterol acyltransferase 1 blockage enhances autophagy in the neurons of triple transgenic Alzheimer's disease mouse and reduces human P301L-tau content at the presymptomatic stage.
Neuroblastoma
AGEs/RAGE complex upregulates BACE1 via NF-kappaB pathway activation.
Neuroblastoma
Aggravation of Alzheimer's disease due to the COX-2-mediated reciprocal regulation of IL-1? and A? between glial and neuron cells.
Neuroblastoma
Akt activity in presenilin 1 wild-type and mutation transfected human SH-SY5Y neuroblastoma cells after serum deprivation and high glucose stress.
Neuroblastoma
Alpha-secretase as a therapeutic target.
Neuroblastoma
Alzheimer disease Abeta production in the absence of S-palmitoylation-dependent targeting of BACE1 to lipid rafts.
Neuroblastoma
Alzheimer's disease presenilin-1 exon 9 deletion and L250S mutations sensitize SH-SY5Y neuroblastoma cells to hyperosmotic stress-induced apoptosis.
Neuroblastoma
Alzheimer's disease presenilin-1 expression modulates the assembly of neurofilaments.
Neuroblastoma
Amyloid Beta-Peptide Increases BACE1 Translation through the Phosphorylation of the Eukaryotic Initiation Factor-2?.
Neuroblastoma
Amyloid precursor protein compartmentalization restricts beta-amyloid production: therapeutic targets based on BACE compartmentalization.
Neuroblastoma
An upstream element containing an ETS binding site is crucial for transcription of the human presenilin-1 gene.
Neuroblastoma
Analysis of presenilin 1 and presenilin 2 expression and processing by newly developed monoclonal antibodies.
Neuroblastoma
ApoE isoforms and carboxyl-terminal-truncated apoE4 forms affect neuronal BACE1 levels and A? production independently of their cholesterol efflux capacity.
Neuroblastoma
Aspartyl protease inhibitor pepstatin binds to the presenilins of Alzheimer's disease.
Neuroblastoma
Association of active gamma-secretase complex with lipid rafts.
Neuroblastoma
BACE-1 inhibition prevents the ?-secretase inhibitor evoked A? rise in human neuroblastoma SH-SY5Y cells.
Neuroblastoma
BACE1 (beta-secretase) inhibitory chromone glycosides from Aloe vera and Aloe nobilis.
Neuroblastoma
BACE1 activity impairs neuronal glucose oxidation: rescue by beta-hydroxybutyrate and lipoic acid.
Neuroblastoma
BACE1 and presenilin/?-secretase regulate proteolytic processing of KCNE1 and 2, auxiliary subunits of voltage-gated potassium channels.
Neuroblastoma
Beta-secretase BACE1 is differentially controlled through muscarinic acetylcholine receptor signaling.
Neuroblastoma
Ca(2+) stores and capacitative Ca(2+) entry in human neuroblastoma (SH-SY5Y) cells expressing a familial Alzheimer's disease presenilin-1 mutation.
Neuroblastoma
Carnosic acid suppresses the production of amyloid-? 1-42 by inducing the metalloprotease gene TACE/ADAM17 in SH-SY5Y human neuroblastoma cells.
Neuroblastoma
Caspase cleavage of exon 9 deleted presenilin-1 is an early event in apoptosis induced by calcium ionophore A 23187 in SH-SY5Y neuroblastoma cells.
Neuroblastoma
Caspase cleaved presenilin-1 is part of active gamma-secretase complexes.
Neuroblastoma
CD40/CD40L interaction induces Abeta production and increases gamma-secretase activity independently of tumor necrosis factor receptor associated factor (TRAF) signaling.
Neuroblastoma
Cellular consequences of the expression of Alzheimer's disease-causing presenilin 1 mutations in human neuroblastoma (SH-SY5Y) cells.
Neuroblastoma
Changes in cholesterol metabolism are associated with PS1 and PS2 gene regulation in SK-N-BE.
Neuroblastoma
Chinese Presenilin-1 V97L mutation enhanced Abeta42 levels in SH-SY5Y neuroblastoma cells.
Neuroblastoma
Cholinergic- and stress-induced signaling activities in cells overexpressing wild-type and mutant presenilin-1.
Neuroblastoma
Cleavage of Alzheimer's amyloid precursor protein by alpha-secretase occurs at the surface of neuronal cells.
Neuroblastoma
Constitutive and cytokine-regulated expression of presenilin-1 and presenilin-2 genes in human neural cell lines.
Neuroblastoma
Design, Synthesis, and Evaluation of Donepezil-Like Compounds as AChE and BACE-1 Inhibitors.
Neuroblastoma
Development and evaluation of multifunctional agents for potential treatment of Alzheimer's disease: application to a pyrimidine-2,4-diamine template.
Neuroblastoma
Differential effects of transforming growth factor-beta(s) and glial cell line-derived neurotrophic factor on gene expression of presenilin-1 in human post-mitotic neurons and astrocytes.
Neuroblastoma
Disrupted intracellular calcium regulates BACE1 gene expression via nuclear factor of activated T cells 1 (NFAT 1) signaling.
Neuroblastoma
Divalent cation tolerance protein binds to ?-secretase and inhibits the processing of amyloid precursor protein.
Neuroblastoma
Downregulated miR-29c correlates with increased BACE1 expression in sporadic Alzheimer's disease.
Neuroblastoma
Dysregulation of SREBP2 induces BACE1 expression.
Neuroblastoma
Effects of early maternal separation on biobehavioral and neuropathological markers of Alzheimer's disease in adult male rats.
Neuroblastoma
Effects of galantamine on ?-amyloid release and beta-site cleaving enzyme 1 expression in differentiated human neuroblastoma SH-SY5Y cells.
Neuroblastoma
Engineered Proteolytic Nanobodies Reduce Abeta Burden and Ameliorate Abeta Induced Cyto-toxicity.
Neuroblastoma
Enhanced generation of intracellular Abeta42 amyloid peptide by mutation of presenilins PS1 and PS2.
Neuroblastoma
Ethanol-induced PGE2 up-regulates A? production through PKA/CREB signaling pathway.
Neuroblastoma
Ets transcription factors ER81 and Elk1 regulate the transcription of the human presenilin 1 gene promoter.
Neuroblastoma
Extracellular release of BACE1 holoproteins from human neuronal cells.
Neuroblastoma
Gadd153 and NF-?B Crosstalk Regulates 27-Hydroxycholesterol-Induced Increase in BACE1 and ?-Amyloid Production in Human Neuroblastoma SH-SY5Y Cells.
Neuroblastoma
gamma-Secretase is differentially modulated by alterations of homocysteine cycle in neuroblastoma and glioblastoma cells.
Neuroblastoma
Histone acetyltransferase p300 mediates histone acetylation of PS1 and BACE1 in a cellular model of Alzheimer's disease.
Neuroblastoma
Human neuroblastoma cells transfected with two Chinese presenilin 1 mutations are sensitized to trophic factor withdrawal and protected by insulin-like growth factor-1.
Neuroblastoma
Hypoxia and reoxygenation increased BACE1 mRNA and protein levels in human neuroblastoma SH-SY5Y cells.
Neuroblastoma
IGF-1-induced processing of the amyloid precursor protein family is mediated by different signaling pathways.
Neuroblastoma
Indomethacin Disrupts the Formation of ?-Amyloid Plaques via an ?2-Macroglobulin-Activating lrp1-Dependent Mechanism.
Neuroblastoma
Inhibition of ?-site amyloid precursor protein cleaving enzyme 1 and cholinesterases by pterosins via a specific structure-activity relationship with a strong BBB permeability.
Neuroblastoma
Inhibition of neurite outgrowth by familial Alzheimer's disease-linked presenilin-1 mutations.
Neuroblastoma
Inhibition of prolylendopeptidase does not affect gamma-secretase processing of amyloid precursor protein in a human neuroblastoma cell line.
Neuroblastoma
Intraventricular Delivery of siRNA Nanoparticles to the Central Nervous System.
Neuroblastoma
Leptin attenuates BACE1 expression and amyloid-? genesis via the activation of SIRT1 signaling pathway.
Neuroblastoma
Luteolin Reduces BACE1 Expression through NF-?B and Estrogen Receptor Mediated Pathways in HEK293 and SH-SY5Y Cells.
Neuroblastoma
Modulation of the endoplasmic reticulum-mitochondria interface in Alzheimer's disease and related models.
Neuroblastoma
Molecular basis of neuroprotective activities of rasagiline and the anti-Alzheimer drug TV3326 [(N-propargyl-(3R)aminoindan-5-YL)-ethyl methyl carbamate].
Neuroblastoma
Morphine via nitric oxide modulates beta-amyloid metabolism: a novel protective mechanism for Alzheimer's disease.
Neuroblastoma
Morphological change by overexpression of D385A dominant negative presenilin 1 in human neuroblastoma SH-SY5Y cells.
Neuroblastoma
Multi-target inhibition ability of neohesperidin dictates its neuroprotective activity: Implication in Alzheimer's disease therapeutics.
Neuroblastoma
Muscarine enhances soluble amyloid precursor protein secretion in human neuroblastoma SH-SY5Y by a pathway dependent on protein kinase C(alpha), src-tyrosine kinase and extracellular signal-regulated kinase but not phospholipase C.
Neuroblastoma
N141I mutant presenilin-2 gene enhances neuronal cell death and decreases bcl-2 expression.
Neuroblastoma
Neuronal ?-amyloid generation is independent of lipid raft association of ?-secretase BACE1: analysis with a palmitoylation-deficient mutant.
Neuroblastoma
Neuroprotection and neurorescue against Abeta toxicity and PKC-dependent release of nonamyloidogenic soluble precursor protein by green tea polyphenol (-)-epigallocatechin-3-gallate.
Neuroblastoma
New type of BACE1 siRNA delivery to cells.
Neuroblastoma
Nicergoline stimulates protein kinase C mediated alpha-secretase processing of the amyloid precursor protein in cultured human neuroblastoma SH-SY5Y cells.
Neuroblastoma
Non-proteolytic effect of beta-site APP-cleaving enzyme 1 (BACE1) on sodium channel function.
Neuroblastoma
Non-steroidal anti-inflammatory drugs stimulate secretion of non-amyloidogenic precursor protein.
Neuroblastoma
Novel presenilin 1 and 2 double knock-out cell line for in vitro validation of PSEN1 and PSEN2 mutations.
Neuroblastoma
Oxidative stress increases BACE1 protein levels through activation of the PKR-eIF2? pathway.
Neuroblastoma
Oxidative stress promotes JNK-dependent amyloidogenic processing of normally expressed human APP by differential modification of alpha-, beta- and gamma-secretase expression.
Neuroblastoma
Oxidative stress up-regulates presenilin 1 in lipid rafts in neuronal cells.
Neuroblastoma
Palmitate Increases ?-site A?PP-Cleavage Enzyme 1 Activity and Amyloid-? Genesis by Evoking Endoplasmic Reticulum Stress and Subsequent C/EBP Homologous Protein Activation.
Neuroblastoma
Palmitate-Induced SREBP1 Expression and Activation Underlies the Increased BACE 1 Activity and Amyloid Beta Genesis.
Neuroblastoma
Phenylbutyric acid rescues endoplasmic reticulum stress-induced suppression of APP proteolysis and prevents apoptosis in neuronal cells.
Neuroblastoma
PI3-K- and PKC-dependent up-regulation of APP processing enzymes by retinoic acid.
Neuroblastoma
PPAR-? agonist regulates amyloid-? generation via inhibiting BACE-1 activity in human neuroblastoma SH-SY5Y cells transfected with APPswe gene.
Neuroblastoma
Presenilin 1 is involved in the maturation of beta-site amyloid precursor protein-cleaving enzyme 1 (BACE1).
Neuroblastoma
Presenilin attenuates receptor-mediated signaling and synaptic function.
Neuroblastoma
Presenilin-1 in neuroblastoma cells.
Neuroblastoma
Presenilin-1 mutations alter K+ currents in the human neuroblastoma cell line, SH-SY5Y.
Neuroblastoma
Presenilin/gamma-secretase-mediated cleavage of the voltage-gated sodium channel beta2-subunit regulates cell adhesion and migration.
Neuroblastoma
Proteasome-mediated effects on amyloid precursor protein processing at the gamma-secretase site.
Neuroblastoma
Regulation of transcription of the human presenilin-1 gene by ets transcription factors and the p53 protooncogene.
Neuroblastoma
Reticulons RTN3 and RTN4-B/C interact with BACE1 and inhibit its ability to produce amyloid beta-protein.
Neuroblastoma
Rosuvastatin reduces caspase-3 activity and up-regulates alpha-secretase in human neuroblastoma SH-SY5Y cells exposed to A beta.
Neuroblastoma
Serum Starvation Induces BACE1 Processing and Secretion.
Neuroblastoma
Sevoflurane But Not Propofol Provided Dual Effects of Cell Survival in Human Neuroblastoma SH-SY5Y Cells.
Neuroblastoma
Statins and the Squalene Synthase Inhibitor Zaragozic Acid Stimulate the Non-Amyloidogenic Pathway of Amyloid-beta Protein Precursor Processing by Suppression of Cholesterol Synthesis.
Neuroblastoma
Surface trafficking of sodium channels in cells and in hippocampal slices.
Neuroblastoma
Systemic administration of fibroblast growth factor-2 (FGF2) reduces BACE1 expression and amyloid pathology in APP23 mice.
Neuroblastoma
Targeting Notch pathway induces growth inhibition and differentiation of neuroblastoma cells.
Neuroblastoma
The expression of the nicotinic acetylcholine receptor ?3 subunit in the brains of patients with Alzheimer's disease and its effects on ?- and ?-secretases and Notch signal transduction in SH-SY5Y cells.
Neuroblastoma
The Molecular Mechanism of Chronic High-Dose Corticosterone-Induced Aggravation of Cognitive Impairment in APP/PS1 Transgenic Mice.
Neuroblastoma
The over-expression of the wild type or mutant forms of the presenilin-1 protein alters glycoprotein processing in a human neuroblastoma cell line.
Neuroblastoma
The presenilin 1 deltaE9 mutation gives enhanced basal phospholipase C activity and a resultant increase in intracellular calcium concentrations.
Neuroblastoma
The transmembrane domain of the Alzheimer's beta-secretase (BACE1) determines its late Golgi localization and access to beta -amyloid precursor protein (APP) substrate.
Neuroblastoma
The up-regulation of BACE1 mediated by hypoxia and ischemic injury: role of oxidative stress and HIF1alpha.
Neuroblastoma
Thiamine deficiency increases beta-secretase activity and accumulation of beta-amyloid peptides.
Neuroblastoma
Transition-state analogue gamma-secretase inhibitors stabilize a 900 kDa presenilin/nicastrin complex.
Neuroblastoma
Two novel presenilin-1 mutations (I249L and P433S) in early onset Chinese Alzheimer's pedigrees and their functional characterization.
Neuroblastoma
Unnatural amino acid-substituted (hydroxyethyl)urea peptidomimetics inhibit gamma-secretase and promote the neuronal differentiation of neuroblastoma cells.
Neuroblastoma
[The effect of two newly Chinese presenilin-1 mutations on the sensitivity to trophic factor withdrawal in human neuroblastoma cells]
Neurodegenerative Diseases
A New Decision Tree to Solve the Puzzle of Alzheimer's Disease Pathogenesis Through Standard Diagnosis Scoring System.
Neurodegenerative Diseases
Alternative transcripts of presenilin-1 associated with frontotemporal dementia.
Neurodegenerative Diseases
Alzheimer's disease-causing proline substitutions lead to presenilin 1 aggregation and malfunction.
Neurodegenerative Diseases
BACE1 and cholinesterase inhibitory activities of compounds from Cajanus cajan and Citrus reticulata: an in silico study.
Neurodegenerative Diseases
Dicer1-miR-328-Bace1 signalling controls brown adipose tissue differentiation and function.
Neurodegenerative Diseases
Divergence of human and mouse brain transcriptome highlights Alzheimer disease pathways.
Neurodegenerative Diseases
Familial Alzheimer's disease: oxidative stress, beta-amyloid, presenilins, and cell death.
Neurodegenerative Diseases
Fragment-guided approach to incorporating structural information into a CoMFA study: BACE-1 as an example.
Neurodegenerative Diseases
Gracilins: Spongionella-derived promising compounds for Alzheimer disease.
Neurodegenerative Diseases
Ibuprofen rescues abnormalities in periodontal tissues in conditional presenilin 1 and presenilin 2 double knockout mice.
Neurodegenerative Diseases
Increased Inflammatory Response Both in Brain and in Periphery in Presenilins Conditional Double Knock-Out Mice.
Neurodegenerative Diseases
Inhibition of gamma-Secretase Activity by Helical beta-Peptide Foldamers.
Neurodegenerative Diseases
Multi-Target ?-Protease Inhibitors from Andrographis paniculata: In Silico and In Vitro Studies.
Neurodegenerative Diseases
NACP/alpha-synuclein, NAC, and beta-amyloid pathology of familial Alzheimer's disease with the E184D presenilin-1 mutation: a clinicopathological study of two autopsy cases.
Neurodegenerative Diseases
Nanolipidic particles improve the bioavailability and alpha-secretase inducing ability of epigallocatechin-3-gallate (EGCG) for the treatment of Alzheimer's disease.
Neurodegenerative Diseases
Neurodegenerative disease and adult neurogenesis.
Neurodegenerative Diseases
Synaptic activity prompts gamma-secretase-mediated cleavage of EphA4 and dendritic spine formation.
Neurodegenerative Diseases
Synthesis and Pharmacological Evaluation of 8- and 9-Substituted Benzolactam-V8 Derivatives as Potent Ligands for Protein Kinase C, a Therapeutic Target for Alzheimer's Disease.
Neurodegenerative Diseases
The potential of natural product vs neurodegenerative disorders: In silico study of artoflavanocoumarin as BACE-1 inhibitor.
Neurodegenerative Diseases
Trimethoxylated Halogenated Chalcones as Dual Inhibitors of MAO-B and BACE-1 for the Treatment of Neurodegenerative Disorders.
Neurodegenerative Diseases
Widespread neuronal expression of the presenilin-1 early-onset Alzheimer's disease gene in the murine brain.
Neuroinflammatory Diseases
A novel BACE inhibitor NB-360 shows a superior pharmacological profile and robust reduction of amyloid-? and neuroinflammation in APP transgenic mice.
Neuroinflammatory Diseases
AF710B, a Novel M1/?1 Agonist with Therapeutic Efficacy in Animal Models of Alzheimers Disease.
Neuroinflammatory Diseases
Ameliorative effect of alendronate against intracerebroventricular streptozotocin induced alteration in neurobehavioral, neuroinflammation and biochemical parameters with emphasis on A? and BACE-1.
Neuroinflammatory Diseases
Astrocytes & Astrocyte derived Extracellular Vesicles in Morphine Induced Amyloidopathy: Implications for Cognitive Deficits in Opiate Abusers.
Neuroinflammatory Diseases
Deficiency of Neuronal p38? MAPK Attenuates Amyloid Pathology in Alzheimer Disease Mouse and Cell Models through Facilitating Lysosomal Degradation of BACE1.
Neuroinflammatory Diseases
Down-regulated expression of microRNA-338-5p contributes to neuropathology in Alzheimer's disease.
Neuroinflammatory Diseases
Ethanol-induced PGE2 up-regulates A? production through PKA/CREB signaling pathway.
Neuroinflammatory Diseases
Gallic Acid is a Dual ?/?-Secretase Modulator that Reverses Cognitive Impairment and Remediates Pathology in Alzheimer Mice.
Neuroinflammatory Diseases
Induced LC degeneration in APP/PS1 transgenic mice accelerates early cerebral amyloidosis and cognitive deficits.
Neuroinflammatory Diseases
Inhibitory effect of 4-O-methylhonokiol on lipopolysaccharide-induced neuroinflammation, amyloidogenesis and memory impairment via inhibition of nuclear factor-kappaB in vitro and in vivo models.
Neuroinflammatory Diseases
Inhibitory effect of ethanol extract of Nannochloropsis oceanica on lipopolysaccharide-induced neuroinflammation, oxidative stress, amyloidogenesis and memory impairment.
Neuroinflammatory Diseases
Minocycline corrects early, pre-plaque neuroinflammation and inhibits BACE-1 in a transgenic model of Alzheimer's disease-like amyloid pathology.
Neuroinflammatory Diseases
Neuroprotective effect of 1-Deoxynojirimycin on cognitive impairment, ?-amyloid deposition, and neuroinflammation in the SAMP8 mice.
Neuroinflammatory Diseases
NF-?B-regulated microRNA-574-5p underlies synaptic and cognitive impairment in response to atmospheric PM2.5 aspiration.
Neuroinflammatory Diseases
Paeoniflorin Atttenuates Amyloidogenesis and the Inflammatory Responses in a Transgenic Mouse Model of Alzheimer's Disease.
Neuroinflammatory Diseases
Relationship between ubiquilin-1 and BACE1 in human Alzheimer's disease and APdE9 transgenic mouse brain and cell-based models.
Neuroinflammatory Diseases
Repeated administration of the noradrenergic neurotoxin N-(2-chloroethyl)-N-ethyl-2-bromobenzylamine (DSP-4) modulates neuroinflammation and amyloid plaque load in mice bearing amyloid precursor protein and presenilin-1 mutant transgenes.
Neuroinflammatory Diseases
STAT3 inhibition protects against neuroinflammation and BACE1 upregulation induced by systemic inflammation.
Neuroinflammatory Diseases
Synaptic and cognitive improvements by inhibition of 2-AG metabolism are through upregulation of microRNA-188-3p in a mouse model of Alzheimer's disease.
Neuroinflammatory Diseases
The BACE inhibitor NB-360 in preclinical models: From ?-amyloid reduction to downstream disease-relevant effects.
Neuroinflammatory Diseases
The modulatory role of prime identified compounds in Geophila repens in mitigating scopolamine-induced neurotoxicity in experimental rats of Alzheimer's disease via attenuation of cholinesterase, ?-secretase, MAPt levels and inhibition of oxidative stress imparts inflammation.
Neuroinflammatory Diseases
TSPO ligand PK11195 alleviates neuroinflammation and beta-amyloid generation induced by systemic LPS administration.
Neuroinflammatory Diseases
Valproic acid potentiates curcumin-mediated neuroprotection in lipopolysaccharide induced rats.
Neurologic Manifestations
Difficult case of a rare form of familial Alzheimer's disease with PSEN1 P117L mutation.
Neuronal Ceroid-Lipofuscinoses
A novel p.Leu(381)Phe mutation in presenilin 1 is associated with very early onset and unusually fast progressing dementia as well as lysosomal inclusions typically seen in Kufs disease.
Neurosyphilis
BACE1 and Other Alzheimer's-Related Biomarkers in Cerebrospinal Fluid and Plasma Distinguish Alzheimer's Disease Patients from Cognitively-Impaired Neurosyphilis Patients.
Niemann-Pick Disease, Type C
Cholesterol-Dependent Energy Transfer between Fluorescent Proteins-Insights into Protein Proximity of APP and BACE1 in Different Membranes in Niemann-Pick Type C Disease Cells.
Obesity
American Chemical Society - 240th national meeting - chemistry for preventing and combating disease: part 1.
Obesity
Bace1-dependent amyloid processing regulates hypothalamic leptin sensitivity in obese mice.
Obesity
Neuronal human BACE1 knockin induces systemic diabetes in mice.
Obesity
Reduction in BACE1 decreases body weight, protects against diet-induced obesity and enhances insulin sensitivity in mice.
Obesity
Susceptibility to diet-induced obesity and glucose intolerance in the APP (SWE)/PSEN1 (A246E) mouse model of Alzheimer's disease is associated with increased brain levels of protein tyrosine phosphatase 1B (PTP1B) and retinol-binding protein 4 (RBP4), and basal phosphorylation of S6 ribosomal protein.
Olfaction Disorders
Differential spatial expression of peripheral olfactory neuron-derived BACE1 induces olfactory impairment by region-specific accumulation of ?-amyloid oligomer.
Osteoporosis
Dimorphic effects of Notch signaling in bone homeostasis.
Osteosarcoma
How the NOTCH Pathway Contributes to the Ability of Osteosarcoma Cells to Metastasize.
Osteosarcoma
Inhibition of Notch pathway prevents osteosarcoma growth by cell cycle regulation.
Osteosarcoma
Notch signaling contributes to the pathogenesis of human osteosarcomas.
Osteosarcoma
Tomatidine Represses Invasion and Migration of Human Osteosarcoma U2OS and HOS Cells by Suppression of Presenilin 1 and c-Raf-MEK-ERK Pathway.
Ovarian Neoplasms
A phase II study of single-agent RO4929097, a gamma-secretase inhibitor of Notch signaling, in patients with recurrent platinum-resistant epithelial ovarian cancer: A study of the Princess Margaret Cancer Centre, Chicago and California phase II consortia.
Ovarian Neoplasms
Down-regulation of Notch1 by gamma-secretase inhibition contributes to cell growth inhibition and apoptosis in ovarian cancer cells A2780.
Ovarian Neoplasms
Inhibition of gamma-secretase in Notch1 signaling pathway as a novel treatment for ovarian cancer.
Ovarian Neoplasms
Jagged-1 and Notch3 juxtacrine loop regulates ovarian tumor growth and adhesion.
Ovarian Neoplasms
PDGFB as a vascular normalization agent in an ovarian cancer model treated with a gamma-secretase inhibitor.
Ovarian Neoplasms
Proteasome inhibition reverses hedgehog inhibitor and taxane resistance in ovarian cancer.
Ovarian Neoplasms
The Role of Notch and Gamma-secretase Inhibition in an Ovarian Cancer Model.
Pancreatic Neoplasms
Activation of Notch signaling in tumorigenesis of experimental pancreatic cancer induced by dimethylbenzanthracene in mice.
Pancreatic Neoplasms
Ligand-dependent Notch signaling is involved in tumor initiation and tumor maintenance in pancreatic cancer.
Pancreatic Neoplasms
[Suppressive effects of gamma-secretase inhibitor DAPT on the proliferation of pancreatic cancer cells].
Pancreatitis
Loss of Bace1 in mice does not alter the severity of caerulein induced pancreatitis.
Pancreatitis
Notch signaling is required for exocrine regeneration after acute pancreatitis.
Paraparesis, Spastic
A novel presenilin 1 mutation (V261L) associated with presenile Alzheimer's disease and spastic paraparesis.
Paraparesis, Spastic
A novel presenilin 1 mutation (Y154N) in a patient with early onset Alzheimer's disease with spastic paraparesis.
Paraparesis, Spastic
A novel presenilin-1 mutation (Leu85Pro) in early-onset Alzheimer disease with spastic paraparesis.
Paraparesis, Spastic
A presenilin 1 mutation (Arg278Ser) associated with early onset Alzheimer's disease and spastic paraparesis.
Paraparesis, Spastic
A presenilin 1 mutation (L420R) in a family with early onset Alzheimer disease, seizures and cotton wool plaques, but not spastic paraparesis.
Paraparesis, Spastic
A systematic review of familial Alzheimer's disease: Differences in presentation of clinical features among three mutated genes and potential ethnic differences.
Paraparesis, Spastic
A variant of Alzheimer's disease with spastic paraparesis and unusual plaques due to deletion of exon 9 of presenilin 1.
Paraparesis, Spastic
Cotton wool plaques in non-familial late-onset Alzheimer disease.
Paraparesis, Spastic
Novel insertional presenilin 1 mutation causing Alzheimer disease with spastic paraparesis.
Paraparesis, Spastic
PET amyloid ligand [11C]PIB uptake shows predominantly striatal increase in variant Alzheimer's disease.
Paraparesis, Spastic
Presenilin-1 mutation (E280G), spastic paraparesis, and cranial MRI white-matter abnormalities.
Paraparesis, Spastic
Presenilin-1 Mutations in Alzheimer's Disease: An Update on Genotype-Phenotype Relationships.
Paraparesis, Spastic
Pure spastic paraparesis associated with a novel presenilin 1 R278K mutation.
Paraparesis, Spastic
Variable phenotype of Alzheimer's disease with spastic paraparesis.
Paraparesis, Spastic
Variant Alzheimer disease with spastic paraparesis: a rare presenilin-1 mutation.
Paraparesis, Spastic
Variant Alzheimer disease with spastic paraparesis: neuropathological phenotype.
Paraparesis, Spastic
Variant Alzheimer's disease with spastic paraparesis: clinical characterization.
Paraparesis, Spastic
Very early onset Alzheimer's disease with spastic paraparesis associated with a novel presenilin 1 mutation (Phe237Ile).
Paraparesis, Spastic
Widespread white matter and conduction defects in PSEN1-related spastic paraparesis.
Paraplegia
Novel insertional presenilin 1 mutation causing Alzheimer disease with spastic paraparesis.
Paraplegia
Spastic paraplegia preceding PSEN1-related familial Alzheimer's disease.
Paraplegia
Temporal-spatial expression of presenilin 1 and the production of amyloid-beta after acute spinal cord injury in adult rat.
Parkinson Disease
American Chemical Society - 240th national meeting - chemistry for preventing and combating disease: part 1.
Parkinson Disease
Association of a BACE1 Gene Polymorphism with Parkinson's Disease in a Norwegian Population.
Parkinson Disease
Cerebrospinal fluid A?42 levels and APP processing pathway genes in Parkinson's disease.
Parkinson Disease
Downregulation of lncRNA BACE1-AS improves dopamine-dependent oxidative stress in rats with Parkinson's disease by upregulating microRNA-34b-5p and downregulating BACE1.
Parkinson Disease
Lead neurotoxicity: exploring the potential impact of lead substitution in zinc-finger proteins on mental health.
Parkinson Disease
Quantitative interaction proteomics of neurodegenerative disease proteins.
Parkinsonian Disorders
A novel mutation (G217D) in the Presenilin 1 gene ( PSEN1) in a Japanese family: presenile dementia and parkinsonism are associated with cotton wool plaques in the cortex and striatum.
Parkinsonian Disorders
A novel presenilin 1 mutation (Leu418Trp) associated with spasticity, parkinsonism, and white matter lesion in a dominant Alzheimer's family.
Parkinsonian Disorders
Dopa Responsive Parkinsonism in an Early Onset Alzheimer's Disease Patient with a Presenilin 1 Mutation (A434T).
Parkinsonian Disorders
Early onset autosomal dominant dementia with ataxia, extrapyramidal features, and epilepsy.
Parkinsonian Disorders
Multimodal Imaging in a Patient With Alzheimer Disease and Parkinsonism Because of a Presenilin-1 Mutation.
Parkinsonian Disorders
New V272A presenilin 1 mutation with very early onset subcortical dementia and parkinsonism.
Parkinsonian Disorders
Presenilin-1 Mutations in Alzheimer's Disease: An Update on Genotype-Phenotype Relationships.
Parkinsonian Disorders
Sex differences in autophagy-mediated diseases: toward precision medicine.
Peripheral Nerve Injuries
Genetic deletion of BACE1 in mice affects remyelination of sciatic nerves.
Peripheral Nervous System Diseases
Beta secretase activity in peripheral nerve regeneration.
Peritoneal Fibrosis
Preventive effect of Notch signaling inhibition by a gamma-secretase inhibitor on peritoneal dialysis fluid-induced peritoneal fibrosis in rats.
Pheochromocytoma
BACE1 inhibitory activity of fungal endophytic extracts from Malaysian medicinal plants.
Pheochromocytoma
Effects of human presenilin 1 isoforms on proliferation and survival of rat pheochromocytoma cell line PC12.
Pheochromocytoma
Isoflurane preconditioning inhibited isoflurane-induced neurotoxicity.
Pheochromocytoma
Neuroprotection and neurorescue against Abeta toxicity and PKC-dependent release of nonamyloidogenic soluble precursor protein by green tea polyphenol (-)-epigallocatechin-3-gallate.
Pheochromocytoma
Role of tyrosine phosphorylation in the antioxidant effects of the p75 neurotrophin receptor.
Pheochromocytoma
The transcription factor Yin Yang 1 is an activator of BACE1 expression.
Pick Disease of the Brain
A novel presenilin 1 mutation associated with Pick's disease but not beta-amyloid plaques.
Pick Disease of the Brain
Pick bodies in a family with presenilin-1 Alzheimer's disease.
Pick Disease of the Brain
Presenilin-1 expression in Pick's disease.
Pilonidal Sinus
Hidradenitis Suppurativa: Proposal of Classification in Two Endotypes with Two-Step Cluster Analysis.
Pituitary Neoplasms
HIF-1? Inhibition Sensitized Pituitary Adenoma Cells to Temozolomide by Regulating Presenilin 1 Expression and Autophagy.
Pneumonia
Gamma-secretase inhibitor reduces allergic pulmonary inflammation by modulating Th1 and Th2 responses.
Polymyositis
BACE-1, PS-1 and sAPP? levels are increased in plasma from sporadic inclusion body myositis patients: surrogate biomarkers among inflammatory myopathies.
Polyradiculoneuropathy
Expression analysis of BDNF, BACE1 and their antisense transcripts in inflammatory demyelinating polyradiculoneuropathy.
Polyradiculoneuropathy, Chronic Inflammatory Demyelinating
Expression analysis of BDNF, BACE1 and their antisense transcripts in inflammatory demyelinating polyradiculoneuropathy.
Pre-Eclampsia
Protein misfolding, congophilia, oligomerization, and defective amyloid processing in preeclampsia.
Precursor Cell Lymphoblastic Leukemia-Lymphoma
A Phase 1 study of the novel gamma-secretase inhibitor PF-03084014 in patients with T-cell acute lymphoblastic leukemia and T-cell lymphoblastic lymphoma.
Precursor Cell Lymphoblastic Leukemia-Lymphoma
Apoptosis in T cell acute lymphoblastic leukemia cells after cell cycle arrest induced by pharmacological inhibition of notch signaling.
Precursor Cell Lymphoblastic Leukemia-Lymphoma
CUTLL1, a novel human T-cell lymphoma cell line with t(7;9) rearrangement, aberrant NOTCH1 activation and high sensitivity to gamma-secretase inhibitors.
Precursor Cell Lymphoblastic Leukemia-Lymphoma
Evaluation of selective gamma-secretase inhibitor PF-03084014 for its antitumor efficacy and gastrointestinal safety to guide optimal clinical trial design.
Precursor Cell Lymphoblastic Leukemia-Lymphoma
Gamma-secretase inhibitors reverse glucocorticoid resistance in T cell acute lymphoblastic leukemia.
Precursor Cell Lymphoblastic Leukemia-Lymphoma
In vitro validation of gamma-secretase inhibitors alone or in combination with other anti-cancer drugs for the treatment of T-cell acute lymphoblastic leukemia.
Precursor Cell Lymphoblastic Leukemia-Lymphoma
Interconnecting molecular pathways in the pathogenesis and drug sensitivity of T-cell acute lymphoblastic leukemia.
Precursor Cell Lymphoblastic Leukemia-Lymphoma
NOTCH inhibition and glucocorticoid therapy in T-cell acute lymphoblastic leukemia.
Precursor Cell Lymphoblastic Leukemia-Lymphoma
Notch-1 regulates Akt signaling pathway and the expression of cell cycle regulatory proteins cyclin D1, CDK2 and p21 in T-ALL cell lines.
Precursor Cell Lymphoblastic Leukemia-Lymphoma
PSEN1-selective gamma-secretase inhibition in combination with kinase or XPO-1 inhibitors effectively targets T cell acute lymphoblastic leukemia.
Precursor Cell Lymphoblastic Leukemia-Lymphoma
Regulation of PTEN by CK2 and Notch1 in primary T-cell acute lymphoblastic leukemia: rationale for combined use of CK2- and gamma-secretase inhibitors.
Precursor Cell Lymphoblastic Leukemia-Lymphoma
T cell acute lymphoblastic leukemia: NOTCHing the way toward a better treatment outcome.
Precursor Cell Lymphoblastic Leukemia-Lymphoma
The role of the PTEN/AKT Pathway in NOTCH1-induced leukemia.
Precursor T-Cell Lymphoblastic Leukemia-Lymphoma
Characterization of Notch1 antibodies that inhibit signaling of both normal and mutated Notch1 receptors.
Precursor T-Cell Lymphoblastic Leukemia-Lymphoma
Downregulation of Notch signaling by gamma-secretase inhibition can abrogate chemotherapy-induced apoptosis in T-ALL cell lines.
Precursor T-Cell Lymphoblastic Leukemia-Lymphoma
Dual antitumor mechanisms of Notch signaling inhibitor in a T-cell acute lymphoblastic leukemia xenograft model.
Precursor T-Cell Lymphoblastic Leukemia-Lymphoma
Interconnecting molecular pathways in the pathogenesis and drug sensitivity of T-cell acute lymphoblastic leukemia.
Precursor T-Cell Lymphoblastic Leukemia-Lymphoma
NOTCH and PI3K-AKT pathways intertwined.
Precursor T-Cell Lymphoblastic Leukemia-Lymphoma
Notch signaling mediates G1/S cell-cycle progression in T cells via cyclin D3 and its dependent kinases.
Precursor T-Cell Lymphoblastic Leukemia-Lymphoma
Oncogenic NOTCH1 control of MYC and PI3K: challenges and opportunities for anti-NOTCH1 therapy in T-cell acute lymphoblastic leukemias and lymphomas.
Precursor T-Cell Lymphoblastic Leukemia-Lymphoma
Pathobiology of acute lymphoblastic leukemia.
Precursor T-Cell Lymphoblastic Leukemia-Lymphoma
PSEN1-selective gamma-secretase inhibition in combination with kinase or XPO-1 inhibitors effectively targets T cell acute lymphoblastic leukemia.
Precursor T-Cell Lymphoblastic Leukemia-Lymphoma
Regulation of PTEN by CK2 and Notch1 in primary T-cell acute lymphoblastic leukemia: rationale for combined use of CK2- and gamma-secretase inhibitors.
Precursor T-Cell Lymphoblastic Leukemia-Lymphoma
Relapsed T Cell ALL: Current Approaches and New Directions.
Precursor T-Cell Lymphoblastic Leukemia-Lymphoma
T cell acute lymphoblastic leukemia: NOTCHing the way toward a better treatment outcome.
Precursor T-Cell Lymphoblastic Leukemia-Lymphoma
Targeting the Notch1 and mTOR pathways in a mouse T-ALL model.
Precursor T-Cell Lymphoblastic Leukemia-Lymphoma
The challenge of targeting notch in hematologic malignancies.
Precursor T-Cell Lymphoblastic Leukemia-Lymphoma
The notch pathway promotes NF-?B activation through Asb2 in T cell acute lymphoblastic leukemia cells.
Precursor T-Cell Lymphoblastic Leukemia-Lymphoma
The role of NOTCH1 signaling in T-ALL.
Precursor T-Cell Lymphoblastic Leukemia-Lymphoma
The SCFFBW7 ubiquitin ligase complex as a tumor suppressor in T cell leukemia.
Prion Diseases
Prion protein expression alters APP cleavage without interaction with BACE-1.
Prion Diseases
PrPSc accumulation in neuronal plasma membranes links Notch-1 activation to dendritic degeneration in prion diseases.
Protein Deficiency
NF{kappa}B-dependent Control of BACE1 Promoter Transactivation by A{beta}42.
Renal Insufficiency
The pathogenic role of notch activation in podocytes.
Renal Insufficiency, Chronic
Therapeutic impact of rHuEPO on abnormal platelet APP, BACE 1, presenilin 1, ADAM 10 and A? expressions in chronic kidney disease patients with cognitive dysfunction like Alzheimer's disease: A pilot study.
Retinoblastoma
Presenilin 1 overexpressions in Chinese hamster ovary (CHO) cells decreases the phosphorylation of retinoblastoma protein: relevance for neurodegeneration.
Retinopathy of Prematurity
Gamma-Secretase Inhibitor, DAPT, Prevents the Development of Retinopathy of Prematurity in a Rat Model by Regulating the Delta-Like Ligand 4/Notch Homolog-1 (DLL4/Notch-1) Pathway.
Retinopathy of Prematurity
Presenilin-2 (PS2) expression up-regulation in a model of retinopathy of prematurity and pathoangiogenesis.
Sarcoma, Ewing
Inhibition of notch signaling induces neural differentiation in Ewing sarcoma.
Scrapie
A gamma-secretase inhibitor and quinacrine reduce prions and prevent dendritic degeneration in murine brains.
Seizures
A novel mutation (L250V) in the presenilin 1 gene in a Japanese familial Alzheimer's disease with myoclonus and generalized convulsion.
Seizures
A novel presenilin 1 duplication mutation (Ile168dup) causing Alzheimer's disease associated with myoclonus, seizures and pyramidal features.
Seizures
A presenilin 1 mutation (L420R) in a family with early onset Alzheimer disease, seizures and cotton wool plaques, but not spastic paraparesis.
Seizures
A presenilin 1 mutation (Ser169Pro) associated with early-onset AD and myoclonic seizures.
Seizures
A systematic review of familial Alzheimer's disease: Differences in presentation of clinical features among three mutated genes and potential ethnic differences.
Seizures
Association between BACE1 gene polymorphisms and focal seizures in a Chinese Han population.
Seizures
BACE1 gene deletion: impact on behavioral function in a model of Alzheimer's disease.
Seizures
BACE1-/- mice exhibit seizure activity that does not correlate with sodium channel level or axonal localization.
Seizures
BACE1-cleavage of Sez6 and Sez6L is elevated in Niemann-Pick type C disease mouse brains.
Seizures
Beta-Site Amyloid Precursor Protein Cleaving Enzyme 1 Inhibition Impairs Synaptic Plasticity via Seizure Protein 6.
Seizures
CA1 hippocampal neuronal loss in familial Alzheimer's disease presenilin-1 E280A mutation is related to epilepsy.
Seizures
Early-Onset Network Hyperexcitability in Presymptomatic Alzheimer's Disease Transgenic Mice Is Suppressed by Passive Immunization with Anti-Human APP/A? Antibody and by mGluR5 Blockade.
Seizures
Electric Stimulation of Neurogenesis Improves Behavioral Recovery After Focal Ischemia in Aged Rats.
Seizures
Epilepsy and cognitive impairments in Alzheimer disease.
Seizures
Epileptic Seizures in AD Patients.
Seizures
Low brain ascorbic acid increases susceptibility to seizures in mouse models of decreased brain ascorbic acid transport and Alzheimer's disease.
Seizures
Presenilin-1 Mutations in Alzheimer's Disease: An Update on Genotype-Phenotype Relationships.
Seizures
Seizure protein 6 and its homolog seizure 6-like protein are physiological substrates of BACE1 in neurons.
Seizures
Seizure protein 6 controls glycosylation and trafficking of kainate receptor subunits GluK2 and GluK3.
Sepsis
Lipopolysaccharide-induced Notch signaling activation through JNK-dependent pathway regulates inflammatory response.
Sepsis
The Role of Secretase Pathway in Long-term Brain Inflammation and Cognitive Impairment in an Animal Model of Severe Sepsis.
Skin Neoplasms
Tau and mTOR: The Hotspots for Multifarious Diseases in Alzheimer's Development.
Spinal Cord Injuries
Inhibition of Gamma-Secretase Promotes Axon Regeneration After a Complete Spinal Cord Injury.
Spinal Cord Injuries
Nogo BACE jumps on the exosome.
Spinal Cord Injuries
Temporal-spatial expression of presenilin 1 and the production of amyloid-beta after acute spinal cord injury in adult rat.
Spinal Cord Injuries
Treatment with a Gamma-Secretase Inhibitor Promotes Functional Recovery in Human iPSC- Derived Transplants for Chronic Spinal Cord Injury.
Spinocerebellar Ataxias
Early-onset familial Alzheimer's disease related to presenilin 1 mutation resembling autosomal dominant spinocerebellar ataxia.
Spinocerebellar Ataxias
Geriatric neurogenetics: oxymoron or reality?
Spinocerebellar Ataxias
Quantitative interaction proteomics of neurodegenerative disease proteins.
Spinocerebellar Ataxias
Regulation of BACE1 by miR-29a/b in a cellular model of Spinocerebellar ataxia 17.
Squamous Cell Carcinoma of Head and Neck
Presenilin 1 is frequently overexpressed and positively associates with epidermal growth factor receptor expression in head and neck squamous cell carcinoma.
Starvation
Fibroblast growth factor rescues brain endothelial cells lacking presenilin 1 from apoptotic cell death following serum starvation.
Starvation
Presenilins in the heart: presenilin-2 expression is increased by low glucose and by hypoxia in cardiac cells.
Starvation
Serum Starvation Induces BACE1 Processing and Secretion.
Stomach Neoplasms
?-Secretase 1 and its Naturally Occurring Anti-Sense RNA are Down-Regulated in Gastric Cancer.
Stomach Neoplasms
MicroRNA-133a inhibits gastric cancer cells growth, migration, and epithelial-mesenchymal transition process by targeting presenilin 1.
Stomach Neoplasms
Notch signaling in gastrointestinal tract (review).
Stomach Neoplasms
The expression of presenilin 1 enhances carcinogenesis and metastasis in gastric cancer.
Stroke
Alzheimer's associated amyloid and tau deposition co-localizes with a homeostatic myelin repair pathway in two mouse models of post-stroke mixed dementia.
Stroke
Atorvastatin promotes presenilin-1 expression and Notch1 activity and increases neural progenitor cell proliferation after stroke.
Stroke
DAPT protects brain against cerebral ischemia by down-regulating the expression of Notch 1 and Nuclear factor kappa B in rats.
Stroke
Development of molecular tools for diagnosis of Alzheimer's disease that are based on detection of amyloidogenic proteins.
Stroke
Early biomarkers for post-stroke cognitive impairment.
Stroke
Hypoxia-inducible factor 1alpha (HIF-1alpha)-mediated hypoxia increases BACE1 expression and beta-amyloid generation.
Stroke
Presenilin-1 polymorphism and hereditary cerebral hemorrhage with amyloidosis, Dutch type.
Stroke
Proliferating Reactive Astrocytes Are Regulated by Notch-1 in the Peri-Infarct Area After Stroke.
Stroke
Self-renewal and differentiation of reactive astrocyte-derived neural stem/progenitor cells isolated from the cortical peri-infarct area after stroke.
Subarachnoid Hemorrhage
Gamma-secretase inhibitor (GSI1) attenuates morphological cerebral vasospasm in 24h after experimental subarachnoid hemorrhage in rats.
Synucleinopathies
Enhanced accumulation of phosphorylated alpha-synuclein in double transgenic mice expressing mutant beta-amyloid precursor protein and presenilin-1.
Tauopathies
cPLA2 and desaturases underlie the tau hyperphosphorylation offset induced by BACE knock-down in neuronal primary cultures.
Tauopathies
Early functional connectivity deficits and progressive microstructural alterations in the TgF344-AD rat model of Alzheimer's Disease: A longitudinal MRI study.
Tauopathies
Enhanced accumulation of tau in doubly transgenic mice expressing mutant betaAPP and presenilin-1.
Tauopathies
Mutations in progranulin explain atypical phenotypes with variants in MAPT.
Teratocarcinoma
Differential effects of transforming growth factor-beta(s) and glial cell line-derived neurotrophic factor on gene expression of presenilin-1 in human post-mitotic neurons and astrocytes.
Thiamine Deficiency
Thiamine deficiency alters APP but not presenilin-1 immunoreactivity in vulnerable brain regions.
Thymoma
Electroacupuncture ameliorates beta-amyloid pathology and cognitive impairment in Alzheimer disease via a novel mechanism involving activation of TFEB (transcription factor EB).
Toxic Optic Neuropathy
Chemoproteomic profiling reveals that cathepsin D off-target activity drives ocular toxicity of ?-secretase inhibitors.
Trauma, Nervous System
Inhibition of Gamma-Secretase Promotes Axon Regeneration After a Complete Spinal Cord Injury.
Triple Negative Breast Neoplasms
DR5 antibody conjugated lipid-based nanocarriers of gamma-secretase inhibitor for the treatment of triple negative breast cancer.
Triple Negative Breast Neoplasms
Phase I study of the gamma secretase inhibitor PF-03084014 in combination with docetaxel in patients with advanced triple-negative breast cancer.
Uterine Cervical Neoplasms
Expression of nuclear Notch3 in cervical squamous cell carcinomas and its association with adverse clinical outcomes.
Uterine Cervical Neoplasms
[Expression of Notch intracellular domain in cervical cancer and effect of DAPT on cervical cancer cell]
Vascular Diseases
Elevated circulating amyloid concentrations in obesity and diabetes promote vascular dysfunction.
Vascular Diseases
Linking vascular disorders and Alzheimer's disease: Potential involvement of BACE1.
Vascular Diseases
The Alzheimer's disease beta-secretase enzyme, BACE1.
Vascular System Injuries
The Decrease of Uch-L1 Activity Is a Common Mechanism Responsible for A? 42 Accumulation in Alzheimer's and Vascular Disease.
Vasospasm, Intracranial
Gamma-secretase inhibitor (GSI1) attenuates morphological cerebral vasospasm in 24h after experimental subarachnoid hemorrhage in rats.
Whooping Cough
FTY720 Attenuates Infection-Induced Enhancement of A? Accumulation in APP/PS1 Mice by Modulating Astrocytic Activation.
Whooping Cough
Multiple pathways of apolipoprotein E signaling in primary neurons.
Whooping Cough
Neurotoxic mechanisms triggered by Alzheimer's disease-linked mutant M146L presenilin 1: involvement of NO synthase via a novel pertussis toxin target.
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0.03359
(+)-corynoline
Homo sapiens
at pH 4.0 and 25°C
0.00225
(+)-N-((4S,4aS,6S,8aR)-10-amino-4,4a,5,6,7,8-hexahydro-1H,3H-4,8a-(epithiomethenoazeno)isochromen-6-yl)-3-chlorobenzamide
Homo sapiens
pH and temperature not specified in the publication
0.04116
(-)-corycavamine
Homo sapiens
at pH 4.0 and 25°C
0.00015
(2R,4S)-N-butyl-4-hydroxy-2-methyl-4-[(2S,5S,7R)-1,2,7-trimethyl-3,16-dioxo-1,4-diazacyclohexadecan-5-yl]butanamide
Homo sapiens
-
0.00059
(2R,4S)-N-butyl-4-[(2S,5S,7R)-2,7-dimethyl-3,15-dioxo-1,4-diazacyclopentadecan-5-yl]-4-hydroxy-2-methylbutanamide
Homo sapiens
-
0.00025
(2R,4S)-N-butyl-4-[(2S,5S,7R)-2,7-dimethyl-3,16-dioxo-1,4-diazacyclohexadecan-5-yl]-4-hydroxy-2-methylbutanamide
Homo sapiens
-
0.000008
(2S)-2-((3R)-3-acetamido-3-isobutyl-2-oxo-1-pyrrolidinyl)-N-((1S,2R)-1-(3,5-difluorobenzyl)-2-hydroxy-2-(1,2,3,4-tetrahydro-3-isoquinolinyl)ethyl)-4-phenylbutanamide
Homo sapiens
pH not specified in the publication, temperature not specified in the publication
0.0056
(2S,5S,8S,11S,14S)-14-amino-5-benzyl-8-(cyclohexylmethyl)-16-(5-fluoro-2,6-dioxo-1,2,3,6-tetrahydropyrimidin-4-yl)-2-hydroxy-11-(1-methylethyl)-4,7,10,13,16-pentaoxo-N-[3-(2H-tetrazol-5-yl)phenyl]-3,6,9,12-tetraazahexadecan-1-amide
Homo sapiens
i.e. KMI-574, used as a substrate transition-state mimic
0.000022
(3S,14R,16S)-16-[(1R)-1-hydroxy-2-([3-(1-methylethyl)benzyl]amino)ethyl]-3,4,14-trimethyl-1,4-diazacyclohexadecane-2,5-dione
Homo sapiens
-
0.000002
(3S,14R,16S)-16-[(1S)-2-[[(1R)-3,3-dimethyl-7-(1-methylethyl)-1,2,3,4-tetrahydronaphthalen-1-yl]amino]-1-hydroxyethyl]-3,4,14-trimethyl-1,4-diazacyclohexadecane-2,5-dione
Homo sapiens
-
0.00001
(3S,5R)-3-(4-amino-3-fluoro-5-[[(2R)-1,1,1-trifluoro-3-hydroxypropan-2-yl]oxy]benzyl)-5-[(3-tert-butylbenzyl)amino]-4-hydroxytetrahydro-2H-thiopyranium-1-olate
Homo sapiens
pH not specified in the publication, temperature not specified in the publication
0.00107
(4aR,6R,8aS)-8a-(2,4-difluorophenyl)-6-(fluoromethyl)-4,4a,5,6,8,8a-hexahydropyrano[3,4-d][1,3]thiazin-2-amine
Homo sapiens
pH 4.5, 37°C
0.000045
(4aS,4'S,10aR)-8-(2-fluoropyridin-3-yl)-4a-methyl-3,4,4a,10a-tetrahydro-2H,5'H-spiro[pyrano[3,2-b]chromene-10,4'-thiazol]-2'-amine
Homo sapiens
pH 4.4, 22°C
0.00001
(5S)-2-amino-5-[3-fluoro-5-(2-fluoropyridin-3-yl)phenyl]-5-(4-methoxy-3-methylphenyl)-3-methyl-3,5-dihydro-4H-imidazol-4-one
Homo sapiens
pH not specified in the publication, temperature not specified in the publication
0.034
(6R)-2-amino-3,6-dimethyl-6-(2-phenylethyl)-5,6-dihydropyrimidin-4(3H)-one
Homo sapiens
pH and temperature not specified in the publication
0.00008
(6R)-2-amino-6-[2-(3'-methoxybiphenyl-4-yl)ethyl]-3,6-dimethyl-5,6-dihydropyrimidin-4(3H)-one
Homo sapiens
pH and temperature not specified in the publication
0.0016
(6R)-2-amino-6-[2-(biphenyl-4-yl)ethyl]-3,6-dimethyl-5,6-dihydropyrimidin-4(3H)-one
Homo sapiens
pH and temperature not specified in the publication
0.00038
(6S)-2-amino-6-(3'-methoxybiphenyl-3-yl)-3,6-dimethyl-5,6-dihydropyrimidin-4(3H)-one
Homo sapiens
pH and temperature not specified in the publication
0.000015
(R)-N-(3-(3-amino-1-methyl-9-oxa-4-thia-2-azaspiro[5.5]undec-2-en-1-yl)-4-fluorophenyl)-5-(fluoromethoxy)pyrazine-2-carboxamide
Homo sapiens
pH and temperature not specified in the publication
0.0000038
(R)-N-(3-(3-amino-5-methyl-9,9-dioxido-2,9-dithia-4-azaspiro[5.5]undec-3-en-5-yl)-4-fluorophenyl)-5-(fluoromethoxy)pyrazine-2-carboxamide
Homo sapiens
pH and temperature not specified in the publication
0.000016
(R)-N-(3-(3-amino-9,9-difluoro-5-methyl-2-thia-4-azaspiro[5.5]undec-3-en-5-yl)-4-fluorophenyl)-5-(fluoromethoxy)pyrazine-2-carboxamide
Homo sapiens
pH and temperature not specified in the publication
0.0000055
(R)-N-(3-(7-amino-2,2-difluoro-9-methyl-6-thia-8-azaspiro[3.5]non-7-en-9-yl)-4-fluorophenyl)-5-(fluoromethoxy)pyrazine-2-carboxamide
Homo sapiens
pH and temperature not specified in the publication
0.0000009
(S)-3-(6,6-dimethyl-3,6-dihydro-2H-pyran-4-yl)-7-(2-fluoropyridin-3-yl)-5'H-spiro[chromeno[2,3-b]pyridine-5,4'-oxazol]-2'-amine
Homo sapiens
pH not specified in the publication, temperature not specified in the publication
0.0000007
(S)-7-(2-fluoropyridin-3-yl)-3-((3-methyloxetan-3-yl)ethynyl)-5H-spiro[chromeno[2,3-b]pyridine-5,4-oxazol]-2-amine
Homo sapiens
pH not specified in the publication, temperature not specified in the publication
0.0000072
(S)-N-(3-(2-amino-4-methyl-5,6-dihydro-4H-1,3-thiazin-4-yl)-4-fluorophenyl)-5-(2,2,2-trifluoroethoxy)pyrazine-2-carboxamide
Homo sapiens
pH and temperature not specified in the publication
0.00002
(S)-N-(3-(2-amino-4-methyl-5,6-dihydro-4H-1,3-thiazin-4-yl)-4-fluorophenyl)-5-(difluoromethyl)pyrazine-2-carboxamide
Homo sapiens
pH and temperature not specified in the publication
0.0000049
(S)-N-(3-(2-amino-4-methyl-5,6-dihydro-4H-1,3-thiazin-4-yl)-4-fluorophenyl)-5-(fluoromethoxy)pyrazine-2-carboxamide
Homo sapiens
pH and temperature not specified in the publication
0.0000046
(S)-N-(3-(2-amino-4-methyl-5,6-dihydro-4H-1,3-thiazin-4-yl)-4-fluorophenyl)-5-chloropicolinamide
Homo sapiens
pH and temperature not specified in the publication
0.0000032
(S)-N-(3-(2-amino-4-methyl-5,6-dihydro-4H-1,3-thiazin-4-yl)-4-fluorophenyl)-5-cyanopicolinamide
Homo sapiens
pH and temperature not specified in the publication
0.000013
(S)-N-(3-(2-amino-4-methyl-5,6-dihydro-4H-1,3-thiazin-4-yl)-4-fluorophenyl)-5-fluoropicolinamide
Homo sapiens
pH and temperature not specified in the publication
0.000011
(S)-N-(3-(2-amino-4-methyl-5,6-dihydro-4H-1,3-thiazin-4-yl)-4-fluorophenyl)-5-methoxypyrazine-2-carboxamide
Homo sapiens
pH and temperature not specified in the publication
0.04863
15,16-dihydrotanshinone
Homo sapiens
at pH 4.5 and 23°C
0.00035
2,3-dihydro-6-methylginkgetin
Homo sapiens
pH not specified in the publication, temperature not specified in the publication
0.00075
2,3-dihydroamentoflavone
Homo sapiens
pH not specified in the publication, temperature not specified in the publication
0.0386
2-((5-cyano-4-(2-methoxyphenyl)-6-oxo-1,6-dihydropyrimidin-2-yl)thio)eN-(4-(3-nitrophenyl)thiazol-2-yl)acetamide
Homo sapiens
at pH 4.5 and 25°C
0.0276
2-((5-cyano-4-(2-methoxyphenyl)-6-oxo-1,6-dihydropyrimidin-2-yl)thio)eN-(4-(4-nitrophenyl)thiazol-2-yl)acetamide
Homo sapiens
at pH 4.5 and 25°C
0.015
2-((5-cyano-4-(3-ethoxyphenyl)-6-oxo-1,6-dihydropyrimidin-2-yl)thio)eN-(4-(4-nitrophenyl)thiazol-2-yl)acetamide
Homo sapiens
at pH 4.5 and 25°C
0.0046
2-((5-cyano-4-(3-ethoxyphenyl)-6-oxo-1,6-dihydropyrimidin-2-yl)thio)eN-(4-phenyl-1H-imidazol-2-yl)acetamide
Homo sapiens
at pH 4.5 and 25°C
0.015
2-((5-cyano-4-(3-methoxyphenyl)-6-oxo-1,6-dihydropyrimidin-2-yl)thio)eN-(4-(3-(2-fluoropyridin-3-yl)phenyl)thiazol-2-yl)acetamide
Homo sapiens
at pH 4.5 and 25°C
0.0243
2-((5-cyano-4-(3-methoxyphenyl)-6-oxo-1,6-dihydropyrimidin-2-yl)thio)eN-(4-(3-nitrophenyl)thiazol-2-yl)acetamide
Homo sapiens
at pH 4.5 and 25°C
0.0261
2-((5-cyano-4-(3-methoxyphenyl)-6-oxo-1,6-dihydropyrimidin-2-yl)thio)eN-(4-(4-nitrophenyl)thiazol-2-yl)acetamide
Homo sapiens
at pH 4.5 and 25°C
0.0042
2-((5-cyano-4-(3-methoxyphenyl)-6-oxo-1,6-dihydropyrimidin-2-yl)thio)eN-(4-phenyl-1H-imidazol-2-yl)acetamide
Homo sapiens
at pH 4.5 and 25°C
0.0374
2-((5-cyano-4-(3-methoxyphenyl)-6-oxo-1,6-dihydropyrimidin-2-yl)thio)eN-(4-phenylthiazol-2-yl)acetamide
Homo sapiens
at pH 4.5 and 25°C
0.0296
2-((5-cyano-6-oxo-4-(3-(trifluoromethoxy)phenyl)-1,6-dihydropyrimidin-2-yl)thio)eN-(4-phenylthiazol-2-yl)acetamide
Homo sapiens
at pH 4.5 and 25°C
0.0191
2-((5-cyano-6-oxo-4-(3-(trifluoromethyl)phenyl)-1,6-dihydropyrimidin-2-yl)thio)eN-(4-phenylthiazol-2-yl)acetamide
Homo sapiens
at pH 4.5 and 25°C
0.00593
2-(3-(4-(3-(cyclohexylamino)-5-methylimidazo[1,2-a]pyridin-2-yl)phenoxy)propyl)isoindoline-1,3-dione
Homo sapiens
at pH 4.5 and 23°C
0.02942
2-(3-(4-(3-(cyclohexylamino)-6-methylimidazo[1,2-a]pyridin-2-yl)phenoxy)propyl)isoindoline-1,3-dione
Homo sapiens
at pH 4.5 and 23°C
0.00284
2-(3-(4-(3-(cyclohexylamino)-7-methylimidazo[1,2-a]pyridin-2-yl)phenoxy)propyl)isoindoline-1,3-dione
Homo sapiens
at pH 4.5 and 23°C
0.0149
2-(3-(4-(6-chloro-3-(cyclohexylamino)imidazo[1,2-a]pyridin-2-yl)-2-methoxyphenoxy)propyl) isoindoline-1,3-dione
Homo sapiens
at pH 4.5 and 23°C
0.000026
2-(3-(imidazo[1,2-a]pyridin-2-yl)phenyl)-6-methoxy-1Hbenzo[d]imidazole
Homo sapiens
pH 4.5, 25°C
0.036
2-amino-3-methyl-6-(naphthalen-2-ylmethyl)pyrimidin-4(3H)-one
Homo sapiens
pH and temperature not specified in the publication
0.00002
2-amino-5-[4-fluoro-3-(pyrimidin-5-yl)phenyl]-5-(4-methoxy-3-methylphenyl)-3-methyl-3,5-dihydro-4H-imidazol-4-one
Homo sapiens
pH not specified in the publication, temperature not specified in the publication
0.077
2-amino-6-(3a,7a-dihydro-1H-indol-6-ylmethyl)-3-methylpyrimidin-4(3H)-one
Homo sapiens
pH and temperature not specified in the publication
0.13
2-amino-6-(3a,7a-dihydro-1H-indol-6-ylmethyl)pyrimidin-4(3H)-one
Homo sapiens
pH and temperature not specified in the publication
0.22
2-amino-6-benzyl-3-methylpyrimidin-4(3H)-one
Homo sapiens
pH and temperature not specified in the publication
0.23
2-amino-8-(2-nitrophenyl)-9-phenyl-1,9-dihydro-6H-purin-6-one
Homo sapiens
pH and temperature not specified in the publication
0.21
2-amino-8-(4-bromophenyl)-9-phenyl-1,9-dihydro-6H-purin-6-one
Homo sapiens
pH and temperature not specified in the publication
0.096
2-[[(1S,2S)-1-benzyl-2-hydroxy-3-oxo-3-[[3-(2H-tetrazol-5-yl)phenyl]amino]propyl]carbamoyl]-6-[[(4S)-4-phenyl-1,3-oxazolidin-3-yl]carbonyl]pyridin-4-yl methanesulfonate
Homo sapiens
i.e. KMI-1036, BACE1 inhibitors with a 5-membered ring at the P3 position and their BACE1 inhibitory activities summarized
0.000004
3-(5-((7aR)-6-(5-fluoropyrimidin-2-yl)-2-imino-3-methyl-4-oxooctahydro-1H-pyrrolo[3,4-d]pyrimidin-7a-yl)thiophen-3-yl)benzonitrile
Homo sapiens
pH not specified in the publication, temperature not specified in the publication
0.0012
3-[(2H-tetrazol-5-ylcarbonyl)amino]-L-alanyl-L-valyl-N-((1S,2R)-1-benzyl-3-[(3,5-di-2H-tetrazol-5-ylphenyl)amino]-2-hydroxy-3-oxopropyl)-L-leucinamide
Homo sapiens
i.e. KMI-684, used as a substrate transition-state mimic
0.0039
3-[(2H-tetrazol-5-ylcarbonyl)amino]-L-alanyl-L-valyl-N-((1S,2R)-1-benzyl-3-[(3,5-dicarboxyphenyl)amino]-2-hydroxy-3-oxopropyl)-L-leucinamide
Homo sapiens
i.e. KMI-429, used as a substrate transition-state mimic
0.0082
3-[(2H-tetrazol-5-ylcarbonyl)amino]-L-alanyl-L-valyl-N-((1S,2R)-1-benzyl-3-[(3-carboxyphenyl)amino]-2-hydroxy-3-oxopropyl)-L-leucinamide
Homo sapiens
i.e. KMI-420, used as a substrate transition-state mimic
0.0048
3-[(2H-tetrazol-5-ylcarbonyl)amino]-L-alanyl-L-valyl-N-[(1S,2R)-1-benzyl-2-hydroxy-3-oxo-3-([3-(2H-tetrazol-5-yl)phenyl]amino)propyl]-L-leucinamide
Homo sapiens
i.e. KMI-570, used as a substrate transition-state mimic
4
4a,5,6,7,8,8a-hexahydro-4H-3,1-benzothiazin-2-amine
Homo sapiens
pH and temperature not specified in the publication
0.02
5-[(E)-benzylideneamino]-6-methoxy-N4-phenylpyrimidine-2,4-diamine
Homo sapiens
pH and temperature not specified in the publication
0.012
5-[(E)-[(2,4,-diclorophenyl)methylidene]amino]-6-methoxy-N4-phenylpyrimidine-2,4-diamine
Homo sapiens
pH and temperature not specified in the publication
0.075
5-[(E)-[(2-chlorophenyl)methylidene]amino]-6-methoxy-N4-phenylpyrimidine-2,4-diamine
Homo sapiens
pH and temperature not specified in the publication
0.0018
6-fluoro-2-(3-(7-fluoroimidazo[1,2-a]pyridin-2-yl)phenyl)-1H-benzo[d]imidazole
Homo sapiens
pH 4.5, 25°C
0.000035
6-fluoro-2-(3-(imidazo[1,2-a]pyridin-2-yl)phenyl)-1H-benzo-[d]imidazole
Homo sapiens
pH 4.5, 25°C
0.044
6-methoxy-5-[(E)-(4-methylbenzylidene)amino]-N4-phenylpyrimidine-2,4-diamine
Homo sapiens
pH and temperature not specified in the publication
0.05
6-methoxy-5-[(E)-[(2-nitrophenyl)methylidene]amino]-N4-phenylpyrimidine-2,4-diamine
Homo sapiens
pH and temperature not specified in the publication
0.038
6-methoxy-N4-phenyl-5-[(E)-[4-(trifluoromethyl)benzylidene]amino]pyrimidine-2,4-diamine
Homo sapiens
pH and temperature not specified in the publication
0.2
caffeic acid
Homo sapiens
at pH 4.5 and 23°C
0.03995
cryptotanshinone
Homo sapiens
at pH 4.5 and 23°C
0.03034
dehydrodanshenol A
Homo sapiens
at pH 4.5 and 23°C
0.01153
deoxyneocryptotanshinone
Homo sapiens
at pH 4.5 and 23°C
0.2
ferruginol
Homo sapiens
at pH 4.5 and 23°C
0.10306
grandifolia F
Homo sapiens
at pH 4.5 and 23°C
-
0.001
GRL-8234
Homo sapiens
i.e. inhibitor 24, in Chinese hamster ovary cells
0.041
KTEETSEVN(statine)VAEF
Homo sapiens
i.e. P10-P40 StatVal, dose-dependent inhibition shown, cleavage determined by fluoresence assay
0.03035
magnesium lithospermate
Homo sapiens
at pH 4.5 and 23°C
0.0356
methyl tanshinonate
Homo sapiens
at pH 4.5 and 23°C
0.0361
N-((4aRS,6RS,8aSR)-2-amino-5,6,7,8-tetrahydro-4H-4a,8a-(methanooxymethano)benzo[d][1,3]thiazin-6-yl)-3-chlorobenzamide
Homo sapiens
pH and temperature not specified in the publication
0.00183
N-(2-amino-4a,5,6,7,8,8a-hexahydro-4H-3,1-benzothiazin-6-yl)-3-chlorobenzamide
Homo sapiens
pH and temperature not specified in the publication
0.0000083
N-(3-((4R,5R)-2-amino-5-methoxy-4-methyl-5,6-dihydro-4H-1,3-thiazin-4-yl)-4-fluorophenyl)-5-(fluoromethoxy)pyrazine-2-carboxamide
Homo sapiens
pH and temperature not specified in the publication
0.0000032
N-(3-((4S,5R)-2-amino-4-methyl-5-(tetrahydro-2H-pyran-4-yl)-5,6-dihydro-4H-1,3-thiazin-4-yl)-4-fluorophenyl)-5-(fluoromethoxy)pyrazine-2-carboxamide
Homo sapiens
pH and temperature not specified in the publication
0.0000017
N-(3-((4S,5R)-2-amino-4-methyl-5-phenyl-5,6-dihydro-4H-1,3-thiazin-4-yl)-4-fluorophenyl)-5-(fluoromethoxy)pyrazine-2-carboxamide
Homo sapiens
pH and temperature not specified in the publication
0.0000033
N-(3-((4S,5S)-2-amino-4-methyl-5-phenyl-5,6-dihydro-4H-1,3-thiazin-4-yl)-4-fluorophenyl)-5-(fluoromethoxy)pyrazine-2-carboxamide
Homo sapiens
pH and temperature not specified in the publication
0.0175
N-(4-(3-bromophenyl)thiazol-2-yl)-2-((5-cyano-4-(3-methoxyphenyl)-6-oxo-1,6-dihydropyrimidin-2-yl)thio)acetamide
Homo sapiens
at pH 4.5 and 25°C
0.0032
N-(4-(4-amino-3,5-dichlorophenyl)-1H-imidazol-2-yl)-2-((5-cyano-4-(3-methoxyphenyl)-6-oxo-1,6-dihydropyrimidin-2-yl)thio)acetamide
Homo sapiens
at pH 4.5 and 25°C
0.0135
N-(4-(4-amino-3,5-dichlorophenyl)thiazol-2-yl)-2-((5-cyano-4-(3-ethoxyphenyl)-6-oxo-1,6-dihydropyrimidin-2-yl)thio)acetamide
Homo sapiens
at pH 4.5 and 25°C
0.0077
N-(4-(4-amino-3,5-dichlorophenyl)thiazol-2-yl)-2-((5-cyano-4-(3-methoxyphenyl)-6-oxo-1,6-dihydropyrimidin-2-yl)thio)acetamide
Homo sapiens
at pH 4.5 and 25°C
0.0134
N-(4-(4-amino-3,5-dichlorophenyl)thiazol-2-yl)-2-((5-cyano-6-oxo-4-(3-(trifluoromethyl)phenyl)-1,6-dihydropyrimidin-2-yl)thio)acetamide
Homo sapiens
at pH 4.5 and 25°C
0.36
N-[(1S,2S)-1-benzyl-2-hydroxy-3-oxo-3-[[3-(2H-tetrazol-5-yl)phenyl]amino]propyl]-4-oxo-6-[[(4S)-4-phenyl-1,3-oxazolidin-3-yl]carbonyl]-1,4-dihydropyridine-2-carboxamide
Homo sapiens
i.e. KMI-1030, BACE1 inhibitors with a 5-membered ring at the P3 position and their BACE1 inhibitory activities summarized
0.05
N-[(1S,2S)-1-benzyl-2-hydroxy-3-oxo-3-[[3-(2H-tetrazol-5-yl)phenyl]amino]propyl]-4-oxo-6-[[(4S)-4-phenyl-1,3-oxazolidin-3-yl]carbonyl]-4H-pyran-2-carboxamide
Homo sapiens
i.e. KMI-1027, BACE1 inhibitors with a 5-membered ring at the P3 position and their BACE1 inhibitory activities summarized
0.14
N-[(1S,2S)-1-benzyl-2-hydroxy-3-oxo-3-[[3-(2H-tetrazol-5-yl)phenyl]amino]propyl]-6-[[(4S)-4-phenyl-1,3-oxazolidin-3-yl]carbonyl]pyridine-2-carboxamide
Homo sapiens
i.e. KMI-1023, BACE1 inhibitors with a 5-membered ring at the P3 position and their BACE1 inhibitory activities summarized
0.00012
N-[2-(3,4-dimethoxyphenyl)ethyl]-2-[(6-[[4,6-di(piperidin-1-yl)-1,3,5-triazin-2-yl]amino]-1,3-benzothiazol-2-yl)sulfanyl]acetamide
Homo sapiens
pH not specified in the publication, temperature not specified in the publication
0.0000025
N-[3-(9H-carbazol-9-yl)-2-hydroxypropyl]-3,4-dichloro-N-phenylbenzamide
Homo sapiens
pH not specified in the publication, temperature not specified in the publication
0.0000038
N-[3-(9H-carbazol-9-yl)-2-hydroxypropyl]-4-methoxy-N-phenylbenzamide
Homo sapiens
pH not specified in the publication, temperature not specified in the publication
0.0000048
N-[3-(9H-carbazol-9-yl)-2-hydroxypropyl]-N-(2-phenylethyl)benzamide
Homo sapiens
pH not specified in the publication, temperature not specified in the publication
0.00023
N1-((2S,3S)-4-(4-(diethylcarbamoyl)-1H-pyrazol-1-yl)-3-hydroxy-1-phenylbutan-2-yl)-N3-((R)-1-(4-fluorophenyl)ethyl)-5-(N-methylmethylsulfonamido)isophthalamide
Homo sapiens
pH not specified in the publication, temperature not specified in the publication
0.000036
N1-((R)-1-(4-fluorophenyl)ethyl)-N3-((2S,3S)-3-hydroxy-4-(4-((R)-1-hydroxy ethyl)-1H-1,2,3-triazol-1-yl)-1-phenylbutan-2-yl)-5-(N-methylmethylsulfonamido)isophthalamide
Homo sapiens
pH not specified in the publication, temperature not specified in the publication
0.000014
OM99-2
Homo sapiens
at pH 4.5 and 23°C
0.01049
quercetin
Homo sapiens
at pH 4.5 and 23°C
0.02977
rosmarinic acid
Homo sapiens
at pH 4.5 and 23°C
0.01301
salvianolic acid A
Homo sapiens
at pH 4.5 and 23°C
0.00918
salvianolic acid C
Homo sapiens
at pH 4.5 and 23°C
0.09822
tanshinol B
Homo sapiens
at pH 4.5 and 23°C
0.03402
tanshinonal
Homo sapiens
at pH 4.5 and 23°C
0.02846
tanshinone I
Homo sapiens
at pH 4.5 and 23°C
0.09186
tanshinone IIA
Homo sapiens
at pH 4.5 and 23°C
0.2
tanshinone IIB
Homo sapiens
at pH 4.5 and 23°C
0.2197
(+)-byakangelicin
Homo sapiens
-
in 50 mM sodium acetate, pH 4.5, at 25°C
0.1049
(+)-byakangelicol
Homo sapiens
-
in 50 mM sodium acetate, pH 4.5, at 25°C
0.3592
(+)-oxypeucedanin
Homo sapiens
-
in 50 mM sodium acetate, pH 4.5, at 25°C
0.00311 - 0.1275
(-)-gallocatechin gallate
0.00017 - 0.0008
(1R,3S)-3-[(1S)-1-(acetylamino)-2-methylpropyl]-N-[(2S,3S,5R)-6-(butylamino)-3-hydroxy-5-methyl-6-oxo-1-phenylhexan-2-yl]cyclohexanecarboxamide
0.0015 - 0.0027
(1R,3S)-3-[1-(acetylamino)cyclopentyl]-N-[(2S,3S,5R)-6-(butylamino)-3-hydroxy-5-methyl-6-oxo-1-phenylhexan-2-yl]cyclohexanecarboxamide
0.0038 - 0.0042
(1R,3S)-3-[2-(acetylamino)propan-2-yl]-N-[(2S,3S)-3-hydroxy-1-phenyl-4-[[3-(propan-2-yl)benzyl]amino]butan-2-yl]cyclohexanecarboxamide
0.00037 - 0.0037
(1R,3S)-3-[2-(acetylamino)propan-2-yl]-N-[(2S,3S,5R)-6-(butylamino)-3-hydroxy-5-methyl-6-oxo-1-phenylhexan-2-yl]cyclohexanecarboxamide
0.0000025 - 0.00014
(1R,3S)-N-[(2S,3S)-3-hydroxy-1-phenyl-4-[[3-(propan-2-yl)benzyl]amino]butan-2-yl]-3-[2-(2-oxopiperidin-1-yl)propan-2-yl]cyclohexanecarboxamide
0.000025 - 0.00096
(1R,3S)-N-[(2S,3S)-3-hydroxy-1-phenyl-4-[[3-(propan-2-yl)benzyl]amino]butan-2-yl]-3-[2-(2-oxopyrrolidin-1-yl)propan-2-yl]cyclohexanecarboxamide
0.00058 - 0.0037
(1R,3S)-N-[(2S,3S)-3-hydroxy-1-phenyl-4-[[3-(propan-2-yl)benzyl]amino]butan-2-yl]-3-[2-(propanoylamino)propan-2-yl]cyclohexanecarboxamide
0.00015 - 0.0002
(1R,3S)-N-[(2S,3S)-3-hydroxy-1-phenyl-4-[[3-(propan-2-yl)benzyl]amino]butan-2-yl]-3-[2-[methyl(propanoyl)amino]propan-2-yl]cyclohexanecarboxamide
0.000511
(1S,2R)-N-[1-benzyl-2-hydroxy-3-(S)-[(1-benzylpiperidin-4-yl)amino]-propyl]-5-[methyl(methylsulfonyl)amino]-N'-[(R)-1-phenylethyl]isophthalamide
Homo sapiens
-
pH 4.0
0.000222
(1S,2R)-N-[1-benzyl-2-hydroxy-3-(S)-[2-(1-benzylpiperidin-4-yl)ethylamino]-propyl]-5-[methyl(methylsulfonyl)-amino]-N'-[(R)-1-(4-fluorophenyl)ethyl]isophthalamide
Homo sapiens
-
pH 4.0
0.000567
(1S,2R)-N-[1-benzyl-2-hydroxy-3-(S)-[2-(1-benzylpiperidin-4-yl)ethylamino]-propyl]-5-[methyl(methylsulfonyl)amino]-N'-[(R)-1-phenylethyl]isophthalamide
Homo sapiens
-
pH 4.0
0.000001
(4S)-4-[(1R)-1-hydroxy-2-([1-[3-(propan-2-yl)phenyl]cyclopropyl]amino)ethyl]-19-(2-oxopyrrolidin-1-yl)-11,16-dioxa-3-azatricyclo[15.3.1.1(6,10)]docosa-1(21),6(22),7,9,17,19-hexaen-2-one
Homo sapiens
-
pH and temperature not specified in the publication
0.000009
(4S)-4-[(1R)-1-hydroxy-2-([1-[3-(propan-2-yl)phenyl]cyclopropyl]amino)ethyl]-19-(methoxymethyl)-11,16-dioxa-3,18-diazatricyclo[15.3.1.1(6,10)]docosa-1(21),6(22),7,9,17,19-hexaen-2-one
Homo sapiens
-
pH and temperature not specified in the publication
0.000017
(4S)-4-[(1R)-1-hydroxy-2-([1-[3-(propan-2-yl)phenyl]cyclopropyl]amino)ethyl]-19-methyl-11,16-dioxa-3,18-diazatricyclo[15.3.1.1(6,10)]docosa-1(21),6(22),7,9,17,19-hexaen-2-one
Homo sapiens
-
pH and temperature not specified in the publication
0.000083
(4S)-4-[(1R)-1-hydroxy-2-([1-[3-(propan-2-yl)phenyl]ethyl]amino)ethyl]-19-methyl-11,16-dioxa-3,18-diazatricyclo[15.3.1.1(6,10)]docosa-1(21),6(22),7,9,17,19-hexaen-2-one
Homo sapiens
-
pH and temperature not specified in the publication
0.00005
(4S)-4-[(1R)-1-hydroxy-2-([2-[3-(propan-2-yl)phenyl]propan-2-yl]amino)ethyl]-19-(methoxymethyl)-11-oxa-3,16-diazatricyclo[15.3.1.1(6,10)]docosa-1(21),6(22),7,9,17,19-hexaen-2-one
Homo sapiens
-
pH and temperature not specified in the publication
0.000292
(4S)-4-[(1R)-1-hydroxy-2-[[3-(propan-2-yl)benzyl]amino]ethyl]-11-oxa-3,16-diazatricyclo[15.3.1.1(6,10)]docosa-1(21),6(22),7,9,17,19-hexaen-2-one
Homo sapiens
-
pH and temperature not specified in the publication
0.00006
(4S)-4-[(1R)-1-hydroxy-2-[[3-(propan-2-yl)benzyl]amino]ethyl]-19-(methoxymethyl)-11-oxa-3,16-diazatricyclo[15.3.1.1(6,10)]docosa-1(21),6(22),7,9,17,19-hexaen-2-one
Homo sapiens
-
pH and temperature not specified in the publication
0.000042
(4S)-4-[(1R)-1-hydroxy-2-[[3-(propan-2-yl)benzyl]amino]ethyl]-19-methyl-11,16-dioxa-3,18-diazatricyclo[15.3.1.1(6,10)]docosa-1(21),6(22),7,9,17,19-hexaen-2-one
Homo sapiens
-
pH and temperature not specified in the publication
0.000027
(4S)-4-[(1R)-1-hydroxy-2-[[3-(propan-2-yl)benzyl]amino]ethyl]-19-methyl-11-oxa-3,16,18-triazatricyclo[15.3.1.1(6,10)]docosa-1(21),6(22),7,9,17,19-hexaen-2-one
Homo sapiens
-
pH and temperature not specified in the publication
0.01
(4S)-4-[(1R)-2-[[1-(3-tert-butylphenyl)-2,2,2-trifluoroethyl]amino]-1-hydroxyethyl]-19-(methoxymethyl)-11-oxa-3,16-diazatricyclo[15.3.1.1(6,10)]docosa-1(21),6(22),7,9,17,19-hexaen-2-one
Homo sapiens
-
IC50 above 0.01 mM, pH and temperature not specified in the publication
0.000177
(4S)-4-[(1R)-2-[[1-(3-tert-butylphenyl)-2-fluoroethyl]amino]-1-hydroxyethyl]-19-(methoxymethyl)-11-oxa-3,16-diazatricyclo[15.3.1.1(6,10)]docosa-1(21),6(22),7,9,17,19-hexaen-2-one
Homo sapiens
-
pH and temperature not specified in the publication
0.000668
(4S)-4-[(1R)-2-[[1-(3-tert-butylphenyl)-2-methoxyethyl]amino]-1-hydroxyethyl]-19-(methoxymethyl)-11-oxa-3,16-diazatricyclo[15.3.1.1(6,10)]docosa-1(21),6(22),7,9,17,19-hexaen-2-one
Homo sapiens
-
pH and temperature not specified in the publication
0.000067
(4S)-4-[(1R)-2-[[1-(3-tert-butylphenyl)cyclobutyl]amino]-1-hydroxyethyl]-19-(methoxymethyl)-11-oxa-3,16-diazatricyclo[15.3.1.1(6,10)]docosa-1(21),6(22),7,9,17,19-hexaen-2-one
Homo sapiens
-
pH and temperature not specified in the publication
0.00005
(4S)-4-[(1R)-2-[[1-(3-tert-butylphenyl)cyclopentyl]amino]-1-hydroxyethyl]-19-(methoxymethyl)-11-oxa-3,16-diazatricyclo[15.3.1.1(6,10)]docosa-1(21),6(22),7,9,17,19-hexaen-2-one
Homo sapiens
-
pH and temperature not specified in the publication
0.00002
(5S)-2-amino-5-(2',4'-difluorobiphenyl-3-yl)-3-methyl-5-(pyridin-4-yl)-3,5-dihydro-4H-imidazol-4-one
Homo sapiens
-
pH not specified in the publication, temperature not specified in the publication
0.039
(6R)-2,6-anhydro-5-O-[(E)-2-(4-hydroxyphenyl)ethenyl]-6-[2-[(2R)-2-hydroxypropyl]-7-methoxy-5-methyl-4-oxo-4H-chromen-8-yl]-L-glucitol
Homo sapiens
-
pH 4.0, 25°C
0.0205
(6R)-2,6-anhydro-6-[7-methoxy-5-methyl-4-oxo-2-[(1E)-prop-1-en-1-yl]-4H-chromen-8-yl]-L-glucitol
Homo sapiens
-
pH 4.0, 25°C
0.000011
(R)-3-(2-amino-6-(3-chloropyridin-2-yl)quinolin-3-yl)-N-(3,3-dimethylbutyl)-2-methylpropanamide
Homo sapiens
-
pH not specified in the publication, temperature not specified in the publication
0.000016
(R)-3-(2-amino-6-(3-methylpyridin-2-yl)quinolin-3-yl)-N-(3,3-dimethylbutyl)-2-methylpropanamide
Homo sapiens
-
pH not specified in the publication, temperature not specified in the publication
0.0059
1-(2-chlorobenzyl)-4-(4-(dibenzo[b,d]furan-1-yl)benzyl)-1H-imidazol-2-amine
Homo sapiens
-
pH not specified in the publication, temperature not specified in the publication
0.0056
1-(4-fluorobenzyl)-4-((30,50-dimethoxybiphenyl-4-yl)methyl)-1H-imidazol-2-amine
Homo sapiens
-
pH not specified in the publication, temperature not specified in the publication
0.0447
1-[(3-benzoylamino-phenylcarbamoyl)-methyl]-3-carbamoyl-pyridiniumchloride
Homo sapiens
-
in 50 mM sodium acetate, pH 4.5, at 37°C
0.003
1-[(E)-[(4-methylquinazolin-2-yl)amino][(phenylcarbamoyl)amino]methylidene]-3-phenylurea
Homo sapiens
-
in 50 mM Tris (pH 7.5), at 25°C
0.012
1-[[3-(4-chloro-phenylcarbamoyl)-phenylcarbamoyl]-methyl]-3-phenethylcarbamoyl-pyridinium chloride
Homo sapiens
-
in 50 mM sodium acetate, pH 4.5, at 37°C
0.001
1-[[3-(4-chloro-phenylcarbamoyl)-phenylcarbamoyl]-methyl]-pyridinium chloride
Homo sapiens
-
in 50 mM sodium acetate, pH 4.5, at 37°C
0.0037
1-[[3-(4-methoxy-phenylcarbamoyl)-phenylcarbamoyl]-methyl]-pyridinium chloride
Homo sapiens
-
in 50 mM sodium acetate, pH 4.5, at 37°C
0.0022
1-[[3-(4-methyl-benzoylamino)-phenylcarbamoyl]-methyl]-3-phenethylcarbamoyl-pyridinium chloride
Homo sapiens
-
in 50 mM sodium acetate, pH 4.5, at 37°C
0.013
1-[[3-(4-methyl-benzoylamino)-phenylcarbamoyl]-methyl]-pyridinium chloride
Homo sapiens
-
in 50 mM sodium acetate, pH 4.5, at 37°C
0.0606
2-(2,4-dihydroxyphenyl)-5,7-dihydroxy-4H-chromen-4-one
Homo sapiens
-
prenylated flavone from the stem bark of Morus lhou, pH not specified in the publication, temperature not specified in the publication
0.00516
2-amino-3-ethyl-5,5-diphenyl-3,5-dihydro-4H-imidazol-4-one
Homo sapiens
pH and temperature not specified in the publication
0.00077
2-amino-3-methyl-5,5-diphenyl-3,5-dihydro-4H-imidazol-4-one
Homo sapiens
-
temperature not specified in the publication, in 20 mM Tris-HCl, pH 7.4
0.00117
2-amino-3-methyl-5-(2-methylpyridin-4-yl)-5-[3-(pyridin-3-yl)phenyl]-3,5-dihydro-4H-imidazol-4-one
Homo sapiens
-
temperature not specified in the publication, in 20 mM Tris-HCl, pH 7.4
0.0022
2-amino-3-methyl-5-(2-methylpyridin-4-yl)-5-[3-(pyrimidin-5-yl)phenyl]-3,5-dihydro-4H-imidazol-4-one
Homo sapiens
-
temperature not specified in the publication, in 20 mM Tris-HCl, pH 7.4
0.00048
2-amino-3-methyl-5-(pyridin-4-yl)-5-[3-(pyridin-3-yl)phenyl]-3,5-dihydro-4H-imidazol-4-one
Homo sapiens
-
temperature not specified in the publication, in 20 mM Tris-HCl, pH 7.4
0.00387
2-amino-3-methyl-5-(tricyclo[3.3.1.1(3,7)]dec-1-yl)-5-[3-(trifluoromethoxy)phenyl]-3,5-dihydro-4H-imidazol-4-one
Homo sapiens
pH and temperature not specified in the publication
0.00201
2-amino-3-methyl-5-phenyl-5-(pyridin-4-yl)-3,5-dihydro-4H-imidazol-4-one
Homo sapiens
-
temperature not specified in the publication, in 20 mM Tris-HCl, pH 7.4
0.00083
2-amino-3-methyl-5-phenyl-5-(tricyclo[3.3.1.13,7]dec-1-yl)-3,5-dihydro-4H-imidazol-4-one
Homo sapiens
pH and temperature not specified in the publication
0.00613
2-amino-3-methyl-5-[2-(propan-2-yl)pyridin-4-yl]-5-[3-(pyrimidin-5-yl)phenyl]-3,5-dihydro-4H-imidazol-4-one
Homo sapiens
-
temperature not specified in the publication, in 20 mM Tris-HCl, pH 7.4
0.08719
2-amino-5,5-diphenyl-3,5-dihydro-4H-imidazol-4-one
Homo sapiens
pH and temperature not specified in the publication
0.00054
2-amino-5-(1,3-benzodioxol-5-yl)-3-methyl-5-[3-(pyridin-3-yl)phenyl]-3,5-dihydro-4H-imidazol-4-one
Homo sapiens
pH and temperature not specified in the publication
0.0005
2-amino-5-(2,3-dihydro-1,4-benzodioxin-6-yl)-3-methyl-5-[3-(pyridin-3-yl)phenyl]-3,5-dihydro-4H-imidazol-4-one
Homo sapiens
pH and temperature not specified in the publication
0.00113
2-amino-5-(2,3-dihydro-1-benzofuran-5-yl)-3-methyl-5-[3-(pyridin-3-yl)phenyl]-3,5-dihydro-4H-imidazol-4-one
Homo sapiens
pH and temperature not specified in the publication
0.0236
2-amino-5-(2,6-diethylpyridin-4-yl)-3-methyl-5-[3-(pyrimidin-5-yl)phenyl]-3,5-dihydro-4H-imidazol-4-one
Homo sapiens
-
temperature not specified in the publication, in 20 mM Tris-HCl, pH 7.4
0.0241
2-amino-5-(2,6-dimethylpyridin-4-yl)-3-methyl-5-[3-(pyrimidin-5-yl)phenyl]-3,5-dihydro-4H-imidazol-4-one
Homo sapiens
-
temperature not specified in the publication, in 20 mM Tris-HCl, pH 7.4
0.00102
2-amino-5-(2-ethylpyridin-4-yl)-3-methyl-5-[3-(pyrimidin-5-yl)phenyl]-3,5-dihydro-4H-imidazol-4-one
Homo sapiens
-
temperature not specified in the publication, in 20 mM Tris-HCl, pH 7.4
0.00959
2-amino-5-(3,4-dimethoxyphenyl)-3-methyl-5-(tricyclo[3.3.1.1(3,7)]dec-1-yl)-3,5-dihydro-4H-imidazol-4-one
Homo sapiens
pH and temperature not specified in the publication
0.00555
2-amino-5-(3-butoxyphenyl)-3-methyl-5-(tricyclo[3.3.1.1(3,7)]dec-1-yl)-3,5-dihydro-4H-imidazol-4-one
Homo sapiens
pH and temperature not specified in the publication
0.00042
2-amino-5-(3-chlorophenyl)-3-methyl-5-phenyl-3,5-dihydro-4H-imidazol-4-one
Homo sapiens
pH and temperature not specified in the publication
0.00253
2-amino-5-(3-ethoxyphenyl)-3-methyl-5-(tricyclo[3.3.1.1(3,7)]dec-1-yl)-3,5-dihydro-4H-imidazol-4-one
Homo sapiens
pH and temperature not specified in the publication
0.00629
2-amino-5-(3-methoxy-4-methylphenyl)-3-methyl-5-(tricyclo[3.3.1.1(3,7)]dec-1-yl)-3,5-dihydro-4H-imidazol-4-one
Homo sapiens
pH and temperature not specified in the publication
0.00068
2-amino-5-(3-methoxyphenyl)-3-methyl-5-(tricyclo[3.3.1.1(3,7)]dec-1-yl)-3,5-dihydro-4H-imidazol-4-one
Homo sapiens
pH and temperature not specified in the publication
0.00119
2-amino-5-(3-methoxyphenyl)-3-methyl-5-phenyl-3,5-dihydro-4H-imidazol-4-one
Homo sapiens
pH and temperature not specified in the publication
0.00184
2-amino-5-(4-chlorophenyl)-3-methyl-5-phenyl-3,5-dihydro-4H-imidazol-4-one
Homo sapiens
pH and temperature not specified in the publication
0.00433
2-amino-5-(4-ethyl-3-methoxyphenyl)-3-methyl-5-(tricyclo[3.3.1.1(3,7)]dec-1-yl)-3,5-dihydro-4H-imidazol-4-one
Homo sapiens
pH and temperature not specified in the publication
0.00096
2-amino-5-(4-methoxy-3-methylphenyl)-3-methyl-5-(6-methylbiphenyl-3-yl)-3,5-dihydro-4H-imidazol-4-one
Homo sapiens
pH and temperature not specified in the publication
0.00079
2-amino-5-(4-methoxy-3-methylphenyl)-3-methyl-5-[3-(pyridin-3-yl)phenyl]-3,5-dihydro-4H-imidazol-4-one
Homo sapiens
-
temperature not specified in the publication, in 20 mM Tris-HCl, pH 7.4
0.00159
2-amino-5-(4-methoxy-3-methylphenyl)-3-methyl-5-[3-(pyrimidin-5-yl)phenyl]-3,5-dihydro-4H-imidazol-4-one
Homo sapiens
pH and temperature not specified in the publication
0.00172
2-amino-5-(4-methoxyphenyl)-3-methyl-5-phenyl-3,5-dihydro-4H-imidazol-4-one
Homo sapiens
pH and temperature not specified in the publication
0.00014
2-amino-5-(biphenyl-3-yl)-3-methyl-5-(pyridin-4-yl)-3,5-dihydro-4H-imidazol-4-one
Homo sapiens
-
temperature not specified in the publication, in 20 mM Tris-HCl, pH 7.4
0.00417
2-amino-5-(biphenyl-3-yl)-5-(3,4-dimethoxyphenyl)-3-methyl-3,5-dihydro-4H-imidazol-4-one
Homo sapiens
pH and temperature not specified in the publication
0.00017
2-amino-5-(biphenyl-3-yl)-5-(3-butoxy-4-methoxyphenyl)-3-methyl-3,5-dihydro-4H-imidazol-4-one
Homo sapiens
pH and temperature not specified in the publication
0.00056
2-amino-5-(biphenyl-3-yl)-5-(3-chloro-4-methoxyphenyl)-3-methyl-3,5-dihydro-4H-imidazol-4-one
Homo sapiens
pH and temperature not specified in the publication
0.00096
2-amino-5-(biphenyl-3-yl)-5-(3-cyclopentyl-4-methoxyphenyl)-3-methyl-3,5-dihydro-4H-imidazol-4-one
Homo sapiens
pH and temperature not specified in the publication
0.0006
2-amino-5-(biphenyl-3-yl)-5-(3-ethoxy-4-methoxyphenyl)-3-methyl-3,5-dihydro-4H-imidazol-4-one
Homo sapiens
pH and temperature not specified in the publication
0.0002
2-amino-5-(biphenyl-3-yl)-5-(3-ethoxy-4-propoxyphenyl)-3-methyl-3,5-dihydro-4H-imidazol-4-one
Homo sapiens
pH and temperature not specified in the publication
0.00052
2-amino-5-(biphenyl-3-yl)-5-(3-fluoro-4-methoxyphenyl)-3-methyl-3,5-dihydro-4H-imidazol-4-one
Homo sapiens
pH and temperature not specified in the publication
0.00078
2-amino-5-(biphenyl-3-yl)-5-(4-methoxy-3-methylphenyl)-3-methyl-3,5-dihydro-4H-imidazol-4-one
Homo sapiens
pH and temperature not specified in the publication
0.0003
2-amino-5-(biphenyl-3-yl)-5-[3-(cyclopentyloxy)-4-methoxyphenyl]-3-methyl-3,5-dihydro-4H-imidazol-4-one
Homo sapiens
pH and temperature not specified in the publication
0.00184
2-amino-5-(biphenyl-3-yl)-5-[4-methoxy-3-(propan-2-yloxy)phenyl]-3-methyl-3,5-dihydro-4H-imidazol-4-one
Homo sapiens
pH and temperature not specified in the publication
0.001
2-amino-5-(biphenyl-3-yl)-5-[4-methoxy-3-(trifluoromethyl)phenyl]-3-methyl-3,5-dihydro-4H-imidazol-4-one
Homo sapiens
pH and temperature not specified in the publication
0.00504
2-amino-5-[2-fluoro-3-(pyrimidin-5-yl)phenyl]-3-methyl-5-[4-(trifluoromethoxy)phenyl]-3,5-dihydro-4H-imidazol-4-one
Homo sapiens
pH and temperature not specified in the publication
0.00078
2-amino-5-[3-(2-fluoropyridin-3-yl)phenyl]-5-(4-methoxy-3-methylphenyl)-3-methyl-3,5-dihydro-4H-imidazol-4-one
0.00251
2-amino-5-[3-(2-methoxypyridin-3-yl)phenyl]-3-methyl-5-[4-(trifluoromethoxy)phenyl]-3,5-dihydro-4H-imidazol-4-one
Homo sapiens
pH and temperature not specified in the publication
0.00248
2-amino-5-[3-(6-fluoropyridin-3-yl)phenyl]-3-methyl-5-[4-(trifluoromethoxy)phenyl]-3,5-dihydro-4H-imidazol-4-one
Homo sapiens
pH and temperature not specified in the publication
0.00599
2-amino-5-[3-(6-methoxypyridin-3-yl)phenyl]-3-methyl-5-[4-(trifluoromethoxy)phenyl]-3,5-dihydro-4H-imidazol-4-one
Homo sapiens
pH and temperature not specified in the publication
0.00126
2-amino-5-[3-fluoro-5-(pyrimidin-5-yl)phenyl]-3-methyl-5-[4-(trifluoromethoxy)phenyl]-3,5-dihydro-4H-imidazol-4-one
Homo sapiens
pH and temperature not specified in the publication
0.00184
2-amino-5-[4-fluoro-3-(2-fluoropyridin-3-yl)phenyl]-5-(4-methoxy-3-methylphenyl)-3-methyl-3,5-dihydro-4H-imidazol-4-one
Homo sapiens
pH and temperature not specified in the publication
0.00969
2-amino-5-[4-fluoro-3-(pyrimidin-5-yl)phenyl]-3-methyl-5-[4-(trifluoromethoxy)phenyl]-3,5-dihydro-4H-imidazol-4-one
Homo sapiens
pH and temperature not specified in the publication
0.0028
2-amino-5-[4-fluoro-3-(pyrimidin-5-yl)phenyl]-5-(4-methoxy-3-methylphenyl)-3-methyl-3,5-dihydro-4H-imidazol-4-one
Homo sapiens
pH and temperature not specified in the publication
0.0345
2-[(3-cyano-4,5,6,7-tetrahydro-1-benzothiophen-2-yl)amino]-2-oxoethyl [(4,6-diphenylpyrimidin-2-yl)sulfanyl]acetate
Homo sapiens
-
in 50 mM Tris (pH 7.5), at 25°C
0.02
2-[(3-cyano-4,6-diphenylpyridin-2-yl)sulfanyl]-N-(3-nitrophenyl)acetamide
Homo sapiens
-
in 50 mM Tris (pH 7.5), at 25°C
0.021
2-[(4-methyl-5-[2-[(4-methylphenyl)amino]-2-oxoethyl]-4H-1,2,4-triazol-3-yl)sulfanyl]-N-(4-phenyl-1,3-thiazol-2-yl)acetamide
Homo sapiens
-
in 50 mM Tris (pH 7.5), at 25°C
0.0102
2-[(6-[[4,6-di(piperidin-1-yl)-1,3,5-triazin-2-yl]amino]-1,3-benzothiazol-2-yl)sulfanyl]-N-(2-fluorophenyl)acetamide
Homo sapiens
-
in 50 mM Tris (pH 7.5), at 25°C
0.001
2-[[2-amino-6-([2-(2-chlorophenyl)-5-[4-(pentyloxy)phenyl]-1H-pyrrol-1-yl]methyl)pyridin-3-yl]amino]ethanol
Homo sapiens
-
pH and temperature not specified in the publication
0.118
2-[[3-cyano-4-(4-fluorophenyl)-6-phenylpyridin-2-yl]sulfanyl]-N-(tricyclo[3.3.1.1(3,7)]dec-1-yl)acetamide
Homo sapiens
-
in 50 mM Tris (pH 7.5), at 25°C
0.05
2-[[3-cyano-6-(4-fluorophenyl)-4-phenylpyridin-2-yl]sulfanyl]-N-(5-ethyl-1,3,4-thiadiazol-2-yl)acetamide
Homo sapiens
-
in 50 mM Tris (pH 7.5), at 25°C
0.05
2-[[4-(4-chlorophenyl)-3-cyano-6-(4-methoxyphenyl)pyridin-2-yl]sulfanyl]-N-(naphthalen-2-yl)-N-phenylacetamide
Homo sapiens
-
in 50 mM Tris (pH 7.5), at 25°C
0.1
2-[[4-benzyl-5-(1H-indol-3-ylmethyl)-4H-1,2,4-triazol-3-yl]sulfanyl]-1-(1H-indol-3-yl)ethanone
Homo sapiens
-
in 50 mM Tris (pH 7.5), at 25°C
0.00005
3-(6-(2-acetylphenyl)-2-aminoquinolin-3-yl)-N-(3,3-dimethylbutyl)-2-methylpropanamide
Homo sapiens
-
pH not specified in the publication, temperature not specified in the publication
0.1
3-(benzylsulfanyl)-6-(5-chloro-3-methyl-1-phenyl-1H-pyrazol-4-yl)-6,7-dihydro[1,2,4]triazino[5,6-d][3,1]benzoxazepine
Homo sapiens
-
in 50 mM Tris (pH 7.5), at 25°C
0.000004
3-(butylsulfonyl)-N-[(2S,3R)-1-(3,5-difluorophenyl)-4-[(3-ethylbenzyl)amino]-3-hydroxybutan-2-yl]-N2-(3,3,3-trifluoropropanoyl)-D-alaninamide
Homo sapiens
-
pH and temperature not specified in the publication
0.000022
3-(butylsulfonyl)-N-[(2S,3R)-1-(3,5-difluorophenyl)-4-[(3-ethylbenzyl)amino]-3-hydroxybutan-2-yl]-N2-(methoxyacetyl)-D-alaninamide
Homo sapiens
-
pH and temperature not specified in the publication
0.00001
3-(butylsulfonyl)-N-[(2S,3R)-1-(3,5-difluorophenyl)-4-[(3-ethylbenzyl)amino]-3-hydroxybutan-2-yl]-N2-(pyridin-3-ylacetyl)-D-alaninamide
Homo sapiens
-
pH and temperature not specified in the publication
0.000011
3-(butylsulfonyl)-N-[(2S,3R)-1-(3,5-difluorophenyl)-4-[(3-ethylbenzyl)amino]-3-hydroxybutan-2-yl]-N2-(pyridin-4-ylacetyl)-D-alaninamide
Homo sapiens
-
pH and temperature not specified in the publication
0.000008
3-(butylsulfonyl)-N2-(3-cyanopropanoyl)-N-[(2S,3R)-1-(3,5-difluorophenyl)-4-[(3-ethylbenzyl)amino]-3-hydroxybutan-2-yl]-D-alaninamide
Homo sapiens
-
pH and temperature not specified in the publication
0.00001
3-(butylsulfonyl)-N2-(cyclopropylcarbonyl)-N-[(2S,3R)-1-(3,5-difluorophenyl)-4-[(3-ethylbenzyl)amino]-3-hydroxybutan-2-yl]-D-alaninamide
Homo sapiens
-
pH and temperature not specified in the publication
0.00367
3-(cyclohexylsulfonyl)-N-[(2S,3R)-3-hydroxy-4-[(3-methoxybenzyl)amino]-1-phenylbutan-2-yl]propanamide
Homo sapiens
-
pH and temperature not specified in the publication
0.000484
3-(dibutylsulfamoyl)-N-[(2S,3R)-3-hydroxy-4-[(3-methoxybenzyl)amino]-1-phenylbutan-2-yl]propanamide
Homo sapiens
-
pH and temperature not specified in the publication
0.00109
3-(dipropylsulfamoyl)-N-[(2S,3R)-3-hydroxy-4-[(3-methoxybenzyl)amino]-1-phenylbutan-2-yl]propanamide
Homo sapiens
-
pH and temperature not specified in the publication
0.000596
3-(heptan-4-ylsulfonyl)-N-[(2S,3R)-3-hydroxy-4-[(3-methoxybenzyl)amino]-1-phenylbutan-2-yl]propanamide
Homo sapiens
-
pH and temperature not specified in the publication
0.0302
3-carbamoyl-1-[[3-(4-chloro-phenylcarbamoyl)-phenylcarbamoyl]-methyl]-pyridinium chloride
Homo sapiens
-
in 50 mM sodium acetate, pH 4.5, at 37°C
0.0019
3-carbamoyl-1-[[3-(4-methoxy-phenylcarbamoyl)-phenylcarbamoyl]-methyl]-pyridinium chloride
Homo sapiens
-
in 50 mM sodium acetate, pH 4.5, at 37°C
0.000005
3-chloro-N-[(2R)-1-([1-(3,5-difluorophenyl)-4-[(3-ethylbenzyl)amino]-3-hydroxybutan-2-yl]amino)-3-(heptan-4-ylsulfonyl)-1-oxopropan-2-yl]benzamide
Homo sapiens
-
pH and temperature not specified in the publication
0.004
3-phenethylcarbamoyl-1-[(3-p-tolylcarbamoyl-phenylcarbamoyl)-methyl]-pyridinium chloride
Homo sapiens
-
in 50 mM sodium acetate, pH 4.5, at 37°C
0.0000012
3-[(2H-tetrazol-5-ylcarbonyl)amino]-L-alanyl-L-valyl-N-((1S,2R)-1-benzyl-3-[(3,5-di-2H-tetrazol-5-ylphenyl)amino]-2-hydroxy-3-oxopropyl)-L-leucinamide
Homo sapiens
-
0.0002 mM, complete inhibition, IC50: 1.2 nM
0.0000039
3-[(2H-tetrazol-5-ylcarbonyl)amino]-L-alanyl-L-valyl-N-((1S,2R)-1-benzyl-3-[(3,5-dicarboxyphenyl)amino]-2-hydroxy-3-oxopropyl)-L-leucinamide
Homo sapiens
-
0.0002 mM, 98.1% inhibition, IC50: 3.9 nM
0.0000082
3-[(2H-tetrazol-5-ylcarbonyl)amino]-L-alanyl-L-valyl-N-((1S,2R)-1-benzyl-3-[(3-carboxyphenyl)amino]-2-hydroxy-3-oxopropyl)-L-leucinamide
Homo sapiens
-
0.002 mM, 87.1% inhibition, IC50: 8.2 nM
0.0000048
3-[(2H-tetrazol-5-ylcarbonyl)amino]-L-alanyl-L-valyl-N-[(1S,2R)-1-benzyl-2-hydroxy-3-oxo-3-([3-(2H-tetrazol-5-yl)phenyl]amino)propyl]-L-leucinamide
Homo sapiens
-
0.0002 mM, 98.1% inhibition, IC50: 4.8 nM
0.0000066
3-[(2H-tetrazol-5-ylcarbonyl)amino]-L-alanyl-L-valyl-N-[(1S,2R)-1-benzyl-2-hydroxy-3-oxo-3-([3-(5-oxo-4,5-dihydro-1,2,4-oxadiazol-3-yl)phenyl]amino)propyl]-L-leucinamide
Homo sapiens
-
0.0002 mM, 94.2% inhibition, IC50: 6.6 nM
0.0000064
3-[(2H-tetrazol-5-ylcarbonyl)amino]-L-alanyl-L-valyl-N-[(1S,2R)-1-benzyl-2-hydroxy-3-oxo-3-([3-(5-thioxo-4,5-dihydro-1,2,4-oxadiazol-3-yl)phenyl]amino)propyl]-L-leucinamide
Homo sapiens
-
0.0002 mM, 97.2% inhibition, IC50: 6.4 nM
0.0000048
3-[(2H-tetrazol-5-ylcarbonyl)amino]alanyl-L-valyl-N-(1-benzyl-2-hydroxy-3-oxo-3-[[3-(2H-tetrazol-5-yl)phenyl]amino]propyl)leucinamide
Homo sapiens
-
-
0.0000012
3-[(2H-tetrazol-5-ylcarbonyl)amino]alanyl-L-valyl-N-[1-benzyl-3-[(3,5-di-2H-tetrazol-5-ylphenyl)amino]-2-hydroxy-3-oxopropyl]leucinamide
Homo sapiens
-
-
0.00012
3-[5-[(1R)-1-amino-1-methyl-2-phenylethyl]-1,3,4-oxadiazol-2-yl]-N-[1-(4-fluorophenyl)ethyl]-5-[methyl(methylsulfonyl)amino]benzamide
Homo sapiens
-
-
0.0000056
3-[[(5-fluoro-2,6-dioxo-1,2,3,6-tetrahydropyrimidin-4-yl)carbonyl]amino]alanyl-L-valyl-N-[(1S)-1-benzyl-2-hydroxy-3-oxo-3-[[3-(2H-tetrazol-5-yl)phenyl]amino]propyl]phenylalaninamide
Homo sapiens
-
-
0.00047
3-[[2-amino-6-([2-(2-chlorophenyl)-5-[4-(pentyloxy)phenyl]-1H-pyrrol-1-yl]methyl)pyridin-3-yl]amino]propan-1-ol
Homo sapiens
-
pH and temperature not specified in the publication
0.0071
4-(4-[1-[(6-aminopyridin-2-yl)methyl]-5-(2-chlorophenyl)-1H-pyrrol-2-yl]phenoxy)butanenitrile
Homo sapiens
-
pH and temperature not specified in the publication
0.00011
4-(cyclohexylamino)-1-(4-fluorobenzyl)-8-[(2'-methylbiphenyl-4-yl)methyl]-1,3,8-triazaspiro[4.5]dec-3-en-2-one
Homo sapiens
-
-
0.00795
4-(dipropylsulfamoyl)-N-[(2S,3R)-3-hydroxy-4-[(3-methoxybenzyl)amino]-1-phenylbutan-2-yl]butanamide
Homo sapiens
-
pH and temperature not specified in the publication
0.09
4-bromo-N-[(4-bromophenyl)sulfonyl]-N-[1-(3,4-dichlorobenzyl)-1H-pyrazol-4-yl]benzenesulfonamide
Homo sapiens
-
in 50 mM Tris (pH 7.5), at 25°C
0.0018
4-[1-(4-methoxyphenyl)-2-[4-(trifluoromethyl)phenyl]ethyl]-1-methyl-1H-imidazol-2-amine
Homo sapiens
-
pH and temperature not specified in the publication
0.00047
4-[2-(2-methoxy-5-nitrophenyl)-1-(4-methoxyphenyl)ethyl]-1-methyl-1H-imidazol-2-amine
Homo sapiens
-
pH and temperature not specified in the publication
0.000063
4-[4-fluoro-5-methoxy-2-[4-(trifluoromethyl)phenyl]-2,3-dihydro-1H-inden-1-yl]-1-methyl-1H-imidazol-2-amine
Homo sapiens
-
pH and temperature not specified in the publication
0.0032
4-[5-methoxy-2-(2-methoxy-5-nitrophenyl)-2,3-dihydro-1H-inden-1-yl]-1-methyl-1H-imidazol-2-amine
Homo sapiens
-
pH and temperature not specified in the publication
0.00035
4-[5-methoxy-2-[4-(trifluoromethyl)phenyl]-2,3-dihydro-1H-inden-1-yl]-1-methyl-1H-imidazol-2-amine
Homo sapiens
-
pH and temperature not specified in the publication
0.008
4-[8-benzyl-4-(cyclohexylamino)-2-oxo-1,3,8-triazaspiro[4.5]dec-3-en-1-yl]benzamide
Homo sapiens
-
-
0.00232
5-[2-amino-4-(4-methoxy-3-methylphenyl)-1-methyl-5-oxo-4,5-dihydro-1H-imidazol-4-yl]biphenyl-2-carbonitrile
Homo sapiens
pH and temperature not specified in the publication
0.00055
5-[2-amino-4-(biphenyl-3-yl)-1-methyl-5-oxo-4,5-dihydro-1H-imidazol-4-yl]-2-methoxybenzonitrile
Homo sapiens
pH and temperature not specified in the publication
0.64
6,7-furano-5,8a-dimethoxy hydrocoumaric acid methyl ester
Homo sapiens
-
in 50 mM sodium acetate, pH 4.5, at 25°C
0.1856
6,7-furano-5-prenyloxy hydrocoumaric acid
Homo sapiens
-
in 50 mM sodium acetate, pH 4.5, at 25°C
0.0305
6,7-furano-5-prenyloxy hydrocoumaric acid methyl ester
Homo sapiens
-
in 50 mM sodium acetate, pH 4.5, at 25°C
0.2033
6,7-furano-8a-methoxy-5-prenyloxy hydrocoumaric acid
Homo sapiens
-
in 50 mM sodium acetate, pH 4.5, at 25°C
0.0162
6,7-furano-8a-methoxy-5-prenyloxy hydrocoumaric acid methyl ester
Homo sapiens
-
in 50 mM sodium acetate, pH 4.5, at 25°C
0.00859
7-phloroethol
Homo sapiens
-
in 50 mM sodium acetate, pH 4.5, at 25°C
0.0383
8,8-diphenyl-2,3,4,8-tetrahydroimidazo[1,5-a]pyrimidin-6-amine
Homo sapiens
-
temperature not specified in the publication, in 20 mM Tris-HCl, pH 7.4
0.0046
8-(biphenyl-4-ylmethyl)-4-(cyclohexylamino)-1-(4-fluorobenzyl)-1,3,8-triazaspiro[4.5]dec-3-en-2-one
Homo sapiens
-
-
0.011
8-benzyl-4-(cyclohexylamino)-1-(3-fluorophenyl)-1,3,8-triazaspiro[4.5]dec-3-en-2-one
Homo sapiens
-
-
0.0269
benzyl 1-(3-acetoxypropyl)-5-((2S,3R)-4-(cyclopropylamino)-3-hydroxy-1-phenylbutan-2-ylcarbamoyl)-2,4,6-trimethyl-1,4-dihydropyridine-3-carboxylate
Homo sapiens
-
pH and temperature not specified in the publication
0.0391
benzyl 5-((2S,3R)-4-(cyclopropylamino)-3-hydroxy-1-phenylbutan-2-ylcarbamoyl)-1-(2-(dimethylamino)-2-oxoethyl)-2,4,6-trimethyl-1,4-dihydropyridine-3-carboxylate
Homo sapiens
-
pH and temperature not specified in the publication
0.0282
benzyl 5-((2S,3R)-4-(cyclopropylamino)-3-hydroxy-1-phenylbutan-2-ylcarbamoyl)-1-(2-(isopropyl(methyl)amino)-2-oxoethyl)-2,4,6-trimethyl-1,4-dihydropyridine-3-carboxylate
Homo sapiens
-
pH and temperature not specified in the publication
0.0155
benzyl 5-((2S,3R)-4-(cyclopropylamino)-3-hydroxy-1-phenylbutan-2-ylcarbamoyl)-1-(2-ethoxy-2-oxoethyl)-2,4,6-trimethyl-1,4-dihydropyridine-3-carboxylate
Homo sapiens
-
pH and temperature not specified in the publication
0.009
benzyl 5-((2S,3R)-4-(cyclopropylamino)-3-hydroxy-1-phenylbutan-2-ylcarbamoyl)-1-(2-isopropoxy-2-oxoethyl)-2,4,6-trimethyl-1,4-dihydropyridine-3-carboxylate
Homo sapiens
-
pH and temperature not specified in the publication
0.0161
benzyl 5-((2S,3R)-4-(cyclopropylamino)-3-hydroxy-1-phenylbutan-2-ylcarbamoyl)-1-(2-isopropoxy-2-oxoethyl)-2,4-dimethyl-1,4-dihydropyridine-3-carboxylate
Homo sapiens
-
pH and temperature not specified in the publication
0.0152
benzyl 5-((2S,3R)-4-(cyclopropylamino)-3-hydroxy-1-phenylbutan-2-ylcarbamoyl)-1-(2-methoxy-2-oxoethyl)-2,4,6-trimethyl-1,4-dihydropyridine-3-carboxylate
Homo sapiens
-
pH and temperature not specified in the publication
0.0284
benzyl 5-((2S,3R)-4-(cyclopropylamino)-3-hydroxy-1-phenylbutan-2-ylcarbamoyl)-2,4,6-trimethyl-1-(2-morpholino-2-oxoethyl)-1,4-dihydropyridine-3-carboxylate
Homo sapiens
-
pH and temperature not specified in the publication
0.0149
benzyl 5-((2S,3R)-4-(cyclopropylamino)-3-hydroxy-1-phenylbutan-2-ylcarbamoyl)-2,4,6-trimethyl-1-(methylsulfonyl)-1,4-dihydropyridine-3-carboxylate
Homo sapiens
-
pH and temperature not specified in the publication
0.0214
benzyl 5-((2S,3R)-4-(cyclopropylamino)-3-hydroxy-1-phenylbutan-2-ylcarbamoyl)-2,6-dimethyl-1-(methylsulfonyl)-4-phenyl-1,4-dihydropyridine-3-carboxylate
Homo sapiens
-
pH and temperature not specified in the publication
0.0081
benzyl 5-((2S,3R)-4-(cyclopropylamino)-3-hydroxy-1-phenylbutan-2-ylcarbamoyl)-2,6-dimethyl-1-(methylsulfonyl)-4-propyl-1,4-dihydropyridine-3-carboxylate
Homo sapiens
-
pH and temperature not specified in the publication
0.0095
benzyl 5-((2S,3R)-4-(cyclopropylamino)-3-hydroxy-1-phenylbutan-2-ylcarbamoyl)-4-ethyl-2,6-dimethyl-1-(methylsulfonyl)-1,4-dihydropyridine-3-carboxylate
Homo sapiens
-
pH and temperature not specified in the publication
0.011
benzyl 5-((2S,3R)-4-(cyclopropylamino)-3-hydroxy-1-phenylbutan-2-ylcarbamoyl)-4-isopropyl-2,6-dimethyl-1-(methylsulfonyl)-1,4-dihydropyridine-3-carboxylate
Homo sapiens
-
pH and temperature not specified in the publication
0.000003
benzyl [(2S)-1-([(2S,3R)-1-(3,5-difluorophenyl)-4-[(3-ethylbenzyl)amino]-3-hydroxybutan-2-yl]amino)-3-(heptan-4-ylsulfonyl)-1-oxopropan-2-yl]carbamate
Homo sapiens
-
pH and temperature not specified in the publication
0.0000098 - 0.0000124
beta-secretase inhibitor IV
0.00221
dieckol
Homo sapiens
-
in 50 mM sodium acetate, pH 4.5, at 25°C
0.00535
dioxinodehydroeckol
Homo sapiens
-
in 50 mM sodium acetate, pH 4.5, at 25°C
0.0122
eckol
Homo sapiens
-
in 50 mM sodium acetate, pH 4.5, at 25°C
0.000651
EVD(statine)VAEF
Homo sapiens
-
IC50: 0.000651 mM
0.00045
EVE(statine)VAEF
Homo sapiens
-
IC50: 0.00045 mM
0.005319
EVG(statine)VAEF
Homo sapiens
-
IC50: 0.005319 mM
0.000265
EVL(statine)VAEF
Homo sapiens
-
IC50: 0.000265 mM
0.0000016
EVNLAAEF
Homo sapiens
-
Leu in the transition state isostere, i.e. OM99-2, IC50: 0.0000016 mM
0.00754
EVW(statine)VAEF
Homo sapiens
-
IC50: 0.00754 mM
0.000118
EVY(statine)VAEF
Homo sapiens
-
IC50: 0.000118 mM
0.0918
imperatorin
Homo sapiens
-
in 50 mM sodium acetate, pH 4.5, at 25°C
0.2442
isoimperatorin
Homo sapiens
-
in 50 mM sodium acetate, pH 4.5, at 25°C
0.0312
isopropyl 2-(3-((2S,3R)-3-hydroxy-4-(3-methoxyphenylamino)-1-phenylbutan-2-ylcarbamoyl)-5-((R)-1-phenylethylcarbamoyl)-4-propylpyridin-1(4H)-yl)acetate
Homo sapiens
-
pH and temperature not specified in the publication
0.0328
isopropyl 2-(3-((2S,3R)-4-(cyclopropylamino)-3-hydroxy-1-phenylbutan-2-ylcarbamoyl)-4-methyl-5-((R)-1-phenylethylcarbamoyl)pyridin-1(4H)-yl) acetate
Homo sapiens
-
pH and temperature not specified in the publication
0.0296
isopropyl 2-(3-((2S,3R)-4-(cyclopropylamino)-3-hydroxy-1-phenylbutan-2-ylcarbamoyl)-5-((R)-1-phenylethylcarbamoyl)-4-propylpyridin-1(4H)-yl)acetate
Homo sapiens
-
pH and temperature not specified in the publication
0.0232
isopropyl 2-(3-acetyl-5-((2S,3R)-3-hydroxy-4-(3-methoxybenzylamino)-1-phenyl butan-2-ylcarbamoyl)-2,6-dimethyl-4-propylpyridin-1(4H)-yl)acetate
Homo sapiens
-
pH and temperature not specified in the publication
0.0261
isopropyl 2-(3-acetyl-5-((2S,3R)-3-hydroxy-4-(3-methoxybenzylamino)-1-phenylbutan-2-ylcarbamoyl)-2,4-dimethylpyridin-1(4H)-yl)acetate
Homo sapiens
-
pH and temperature not specified in the publication
0.0266
isopropyl 2-(3-acetyl-5-((2S,3R)-3-hydroxy-4-(3-methoxyphenylamino)-1-phenylbutan-2-ylcarbamoyl)-2,6-dimethyl-4-propylpyridin-1(4H)-yl)acetate
Homo sapiens
-
pH and temperature not specified in the publication
0.0264
isopropyl 2-(3-acetyl-5-((2S,3R)-4-(3-fluorophenylamino)-3-hydroxy-1-phenylbutan-2-ylcarbamoyl)-2,4,6-trimethylpyridin-1(4H)-yl)acetate
Homo sapiens
-
pH and temperature not specified in the publication
0.0293
isopropyl 2-(3-acetyl-5-((2S,3R)-4-(3-fluorophenylamino)-3-hydroxy-1-phenylbutan-2-ylcarbamoyl)-2,4-dimethylpyridin-1(4H)-yl)acetate
Homo sapiens
-
pH and temperature not specified in the publication
0.0271
isopropyl 2-(3-acetyl-5-((2S,3R)-4-(3-fluorophenylamino)-3-hydroxy-1-phenylbutan-2-ylcarbamoyl)-2,6-dimethyl-4-propylpyridin-1(4H)-yl)acetate
Homo sapiens
-
pH and temperature not specified in the publication
0.0293
isopropyl 2-(3-acetyl-5-((2S,3R)-4-(cyclopropylamino)-3-hydroxy-1-phenylbutan-2-ylcarbamoyl)-2,4,6-trimethylpyridin-1(4H)-yl)acetate
Homo sapiens
-
pH and temperature not specified in the publication
0.0331
isopropyl 2-(3-acetyl-5-((2S,3R)-4-(cyclopropylamino)-3-hydroxy-1-phenylbutan-2-ylcarbamoyl)-2,6-dimethyl-4-propylpyridin-1(4H)-yl)acetate
Homo sapiens
-
pH and temperature not specified in the publication
0.0034
kuwanon
Homo sapiens
-
prenylated flavone from the stem bark of Morus lhou, pH not specified in the publication, temperature not specified in the publication
0.0053
kuwanon A
Homo sapiens
-
pH not specified in the publication, temperature not specified in the publication
0.000012
L-alpha-glutamyl-L-leucyl-N-[(2S,5S,8S,14R)-2-carboxy-5-(carboxymethoxy)-13-hydroxy-11,16-dimethyl-13-oxido-4,7,10-trioxo-1-phenyl-8-(propan-2-yl)-3,6,9-triaza-13-lambda5-phosphaheptadecan-14-yl]-L-alpha-asparagine
Homo sapiens
-
pH and temperature not specified in the publication
0.0002
Lys-Thr-Glu-Glu-Ile-Ser-Glu-Val-Asn-(statine)-Val-Ala-Glu-Phe-OH
Homo sapiens
-
in 50 mM sodium acetate, pH 4.5, at 25°C
0.00012
Lys-Thr-Glu-Glu-Ile-Ser-Glu-Val-Asn-Sta-Val-Ala-Glu-Phe
Homo sapiens
-
in 50 mM Tris (pH 7.5), at 25°C
0.00014
Lys-Thr-Glu-Glu-Ile-Ser-Glu-Val-Asn-[statine(3S,4S)]-Val-Ala-Glu-Phe-OH
0.000003
methyl [(2S)-1-([(2S,3R)-1-(3,5-difluorophenyl)-4-[(3-ethylbenzyl)amino]-3-hydroxybutan-2-yl]amino)-3-(heptan-4-ylsulfonyl)-1-oxopropan-2-yl]carbamate
Homo sapiens
-
pH and temperature not specified in the publication
0.0594
morusin
Homo sapiens
-
prenylated flavone from the stem bark of Morus lhou, pH not specified in the publication, temperature not specified in the publication
0.000005
N'-[(2S,3R)-1-(3,5-difluorophenyl)-3-hydroxy-4-[(3-iodobenzyl)amino]butan-2-yl]-5-methyl-N,N-dipropylbenzene-1,3-dicarboxamide
Homo sapiens
-
pH and temperature not specified in the publication
0.00031
N'-[(2S,3R)-3-hydroxy-4-[(3-iodobenzyl)amino]-1-phenylbutan-2-yl]-N,N-dipropylbenzene-1,3-dicarboxamide
Homo sapiens
-
pH and temperature not specified in the publication
0.0005
N'-[(2S,3R)-3-hydroxy-4-[(3-methoxybenzyl)amino]-1-phenylbutan-2-yl]-N,N-dipropylbenzene-1,3-dicarboxamide
Homo sapiens
-
pH and temperature not specified in the publication
0.0122
N,N'-bis(3-cyano-4,5,6,7,8,9-hexahydrocycloocta[b]thiophen-2-yl)-2,2,3,3,4,4,5,5-octafluorohexanediamide
Homo sapiens
-
in 50 mM Tris (pH 7.5), at 25°C
0.000015 - 0.00046
N-((1S,2R)-1-benzyl-3-cyclopropylamino-2-hydroxy-propyl)-5-(methanesulfonyl-methyl-amino)-N'-((R)-1-phenyl-ethyl)-isophthalamide
0.024
N-(2-methyl-5-[(6-phenylpyrimidin-4-yl)amino]phenyl)methanesulfonamide
Homo sapiens
-
-
0.000076
N-(2-methylpropyl)-N2-([17-[(methylsulfonyl)(propyl)amino]-2-oxo-3-azatricyclo[13.3.1.16,10]icosa-1(19),6(20),7,9,15,17-hexaen-4-yl]methyl)-L-norleucinamide
Homo sapiens
-
-
0.0028
N-(4-([4-(cyclohexylamino)-1-(3-fluorophenyl)-2-oxo-1,3,8-triazaspiro[4.5]dec-3-en-8-yl]methyl)phenyl)acetamide
Homo sapiens
-
-
0.015
N-(5-([6-(4-(N,N-dimethyl)aminophenyl)pyrimidin-4-yl]amino)-2-methylphenyl)-N-methylmethanesulfonamide
Homo sapiens
-
-
0.021
N-(5-[[6-(2,3-dihydro-1,4-benzodioxin-6-yl)pyrimidin-4-yl]amino]-2-methylphenyl)-N-methylmethanesulfonamide
Homo sapiens
-
-
0.00231
N-(tert-butoxycarbonyl)-L-leucyl-N-[(4S,5S,7R)-5-hydroxy-2,7-dimethyl-8-[(2-methylpropyl)amino]-8-oxooctan-4-yl]-L-phenylalaninamide
Homo sapiens
-
pH and temperature not specified in the publication
0.000027
N-acetyl-beta-alanyl-3-(butylsulfonyl)-N-[(2S,3R)-1-(3,5-difluorophenyl)-4-[(3-ethylbenzyl)amino]-3-hydroxybutan-2-yl]-D-alaninamide
Homo sapiens
-
pH and temperature not specified in the publication
0.004
N-acetyl-L-alanyl-N-[(4S,5S,7R)-8-(butylamino)-5-hydroxy-2,7-dimethyl-8-oxooctan-4-yl]-L-methioninamide
Homo sapiens
-
pH and temperature not specified in the publication
0.00012
N-acetyl-L-leucyl-N-[(4S,5S,7R)-8-(butylamino)-5-hydroxy-2,7-dimethyl-8-oxooctan-4-yl]-L-alaninamide
Homo sapiens
-
pH and temperature not specified in the publication
0.000053
N-acetyl-L-leucyl-N-[(4S,5S,7R)-8-(butylamino)-5-hydroxy-2,7-dimethyl-8-oxooctan-4-yl]-L-methioninamide
Homo sapiens
-
pH and temperature not specified in the publication
0.00037
N-acetyl-L-valyl-N-[(4S,5S,7R)-8-(butylamino)-5-hydroxy-2,7-dimethyl-8-oxooctan-4-yl]-L-methioninamide
Homo sapiens
-
pH and temperature not specified in the publication
0.000005
N-[(1R,2S)-1-benzyl-2-hydroxy-3-[[3-(trifluoromethyl)benzyl]amino]propyl]-3-(1,1-dioxido-1,2-thiazinan-2-yl)-5-(ethylamino)-2-fluorobenzamide
Homo sapiens
-
-
0.000002
N-[(1S)-1-[(butylsulfonyl)methyl]-2-([1-(3,5-difluorobenzyl)-3-[(3-ethylbenzyl)amino]-2-hydroxypropyl]amino)-2-oxoethyl]benzamide
Homo sapiens
-
-
0.00011
N-[(1Z)-amino(butylamino)methylidene]-2-[2-(2-chlorophenyl)-5-(4-propoxyphenyl)-1H-pyrrol-1-yl]acetamide
Homo sapiens
-
-
0.000015
N-[(2R)-1-([1-(3,5-difluorophenyl)-4-[(3-ethylbenzyl)amino]-3-hydroxybutan-2-yl]amino)-3-(heptan-4-ylsulfonyl)-1-oxopropan-2-yl]-2-methylbenzamide
Homo sapiens
-
pH and temperature not specified in the publication
0.000002
N-[(2R)-1-([1-(3,5-difluorophenyl)-4-[(3-ethylbenzyl)amino]-3-hydroxybutan-2-yl]amino)-3-(heptan-4-ylsulfonyl)-1-oxopropan-2-yl]-3-hydroxybenzamide
Homo sapiens
-
pH and temperature not specified in the publication
0.000053
N-[(2R)-1-([1-(3,5-difluorophenyl)-4-[(3-ethylbenzyl)amino]-3-hydroxybutan-2-yl]amino)-3-(heptan-4-ylsulfonyl)-1-oxopropan-2-yl]-4-(trifluoromethyl)benzamide
Homo sapiens
-
pH and temperature not specified in the publication
0.000002
N-[(2R)-1-([1-(3,5-difluorophenyl)-4-[(3-ethylbenzyl)amino]-3-hydroxybutan-2-yl]amino)-3-(heptan-4-ylsulfonyl)-1-oxopropan-2-yl]-4-methoxybenzamide
Homo sapiens
-
pH and temperature not specified in the publication
0.000004
N-[(2R)-1-([1-(3,5-difluorophenyl)-4-[(3-ethylbenzyl)amino]-3-hydroxybutan-2-yl]amino)-3-(heptan-4-ylsulfonyl)-1-oxopropan-2-yl]-4-methylbenzamide
Homo sapiens
-
pH and temperature not specified in the publication
0.000002
N-[(2R)-1-([1-(3,5-difluorophenyl)-4-[(3-ethylbenzyl)amino]-3-hydroxybutan-2-yl]amino)-3-(heptan-4-ylsulfonyl)-1-oxopropan-2-yl]benzamide
Homo sapiens
-
pH and temperature not specified in the publication
0.000001
N-[(2R)-1-([1-(3,5-difluorophenyl)-4-[(3-ethylbenzyl)amino]-3-hydroxybutan-2-yl]amino)-3-(heptan-4-ylsulfonyl)-1-oxopropan-2-yl]pyridine-2-carboxamide
Homo sapiens
-
pH and temperature not specified in the publication
0.000049
N-[(2R)-2-amino-1-benzyl-3-fluoropropyl]-2-[[(2-methylcyclopropyl)methyl]amino]-6-[methyl[(1-methylethyl)sulfonyl]amino]pyridine-4-carboxamide
Homo sapiens
-
-
0.00467
N-[(2S)-1-([(4S,5S,7R)-5-hydroxy-2,7-dimethyl-8-[(2-methylpropyl)amino]-8-oxooctan-4-yl]amino)-1-oxo-3-phenylpropan-2-yl]naphthalene-1-carboxamide
Homo sapiens
-
pH and temperature not specified in the publication
0.000004
N-[(2S)-3-(butylsulfonyl)-1-([(2S,3R)-1-(3,5-difluorophenyl)-4-[(3-ethylbenzyl)amino]-3-hydroxybutan-2-yl]amino)-1-oxopropan-2-yl]-1H-imidazole-2-carboxamide
Homo sapiens
-
pH and temperature not specified in the publication
0.000005
N-[(2S)-3-(butylsulfonyl)-1-([(2S,3R)-1-(3,5-difluorophenyl)-4-[(3-ethylbenzyl)amino]-3-hydroxybutan-2-yl]amino)-1-oxopropan-2-yl]-4-hydroxypyridine-3-carboxamide
Homo sapiens
-
pH and temperature not specified in the publication
0.000004
N-[(2S)-3-(butylsulfonyl)-1-([(2S,3R)-1-(3,5-difluorophenyl)-4-[(3-ethylbenzyl)amino]-3-hydroxybutan-2-yl]amino)-1-oxopropan-2-yl]-5-methyl-1H-pyrazole-3-carboxamide
Homo sapiens
-
pH and temperature not specified in the publication
0.000004
N-[(2S)-3-(butylsulfonyl)-1-([(2S,3R)-1-(3,5-difluorophenyl)-4-[(3-ethylbenzyl)amino]-3-hydroxybutan-2-yl]amino)-1-oxopropan-2-yl]pyrazine-2-carboxamide
Homo sapiens
-
pH and temperature not specified in the publication
0.000002
N-[(2S)-3-(butylsulfonyl)-1-([(2S,3R)-1-(3,5-difluorophenyl)-4-[(3-ethylbenzyl)amino]-3-hydroxybutan-2-yl]amino)-1-oxopropan-2-yl]pyridine-3-carboxamide
Homo sapiens
-
pH and temperature not specified in the publication
0.000005
N-[(2S)-3-(butylsulfonyl)-1-([(2S,3R)-1-(3,5-difluorophenyl)-4-[(3-ethylbenzyl)amino]-3-hydroxybutan-2-yl]amino)-1-oxopropan-2-yl]pyridine-4-carboxamide
Homo sapiens
-
pH and temperature not specified in the publication
0.0041
N-[(2S,3R)-1-(3,5-difluorophenyl)-3-hydroxy-4-[(3-iodobenzyl)amino]butan-2-yl]-3-methylbenzamide
Homo sapiens
-
pH and temperature not specified in the publication
0.005214
N-[(2S,3R)-3-hydroxy-4-[(3-methoxybenzyl)amino]-1-phenylbutan-2-yl]-3-(phenylsulfonyl)propanamide
Homo sapiens
-
pH and temperature not specified in the publication
0.003785
N-[(2S,3R)-3-hydroxy-4-[(3-methoxybenzyl)amino]-1-phenylbutan-2-yl]-3-(piperidin-1-ylsulfonyl)propanamide
Homo sapiens
-
pH and temperature not specified in the publication
0.005015
N-[(2S,3R)-3-hydroxy-4-[(3-methoxybenzyl)amino]-1-phenylbutan-2-yl]-3-[(3-methylbutyl)sulfamoyl]propanamide
Homo sapiens
-
pH and temperature not specified in the publication
0.005614
N-[(2S,3R)-3-hydroxy-4-[(3-methoxybenzyl)amino]-1-phenylbutan-2-yl]-3-[(3-methylbutyl)sulfonyl]propanamide
Homo sapiens
-
pH and temperature not specified in the publication
0.004131
N-[(2S,3R)-3-hydroxy-4-[(3-methoxybenzyl)amino]-1-phenylbutan-2-yl]-4-(phenylsulfonyl)butanamide
Homo sapiens
-
pH and temperature not specified in the publication
0.006461
N-[(2S,3R)-3-hydroxy-4-[(3-methoxybenzyl)amino]-1-phenylbutan-2-yl]-4-(piperidin-1-ylsulfonyl)butanamide
Homo sapiens
-
pH and temperature not specified in the publication
0.000002
N-[(4S)-4-[(1R)-1-hydroxy-2-([1-[3-(propan-2-yl)phenyl]cyclopropyl]amino)ethyl]-2-oxo-11-oxa-3,16-diazatricyclo[15.3.1.1(6,10)]docosa-1(21),6(22),7,9,17,19-hexaen-19-yl]-N-methylpropane-1-sulfonamide
Homo sapiens
-
pH and temperature not specified in the publication
0.000001
N-[(4S)-4-[(1R)-1-hydroxy-2-[[3-(propan-2-yl)benzyl]amino]ethyl]-2-oxo-11-oxa-3,16-diazatricyclo[15.3.1.1(6,10)]docosa-1(21),6(22),7,9,17,19-hexaen-19-yl]-N-methylpropane-1-sulfonamide
Homo sapiens
-
pH and temperature not specified in the publication
0.000616
N-[(4S,5S,7R)-2-[7-(1-benzylpiperidin-4-yl)]methylcarbamoyl-5-hydroxy-2-methyloct-4-yl]-N'-[(R)-1-(4-fluorophenyl)ethyl-5-methyl(methylsulfonyl)amino]isophthalamide
Homo sapiens
-
pH 4.0
0.00264
N-[(4S,5S,7R)-5-hydroxy-2,7-dimethyl-8-[(2-methylpropyl)amino]-8-oxooctan-4-yl]-4-nitro-Nalpha-(4-nitrobenzoyl)-L-phenylalaninamide
Homo sapiens
-
pH and temperature not specified in the publication
0.00379
N-[(4S,5S,7R)-5-hydroxy-2,7-dimethyl-8-[(2-methylpropyl)amino]-8-oxooctan-4-yl]-4-nitro-Nalpha-[(2Z)-3-[4-(trifluoromethyl)phenyl]prop-2-enoyl]-L-phenylalaninamide
Homo sapiens
-
pH and temperature not specified in the publication
0.01573
N-[(4S,5S,7R)-5-hydroxy-2,7-dimethyl-8-[(2-methylpropyl)amino]-8-oxooctan-4-yl]-Nalpha-(4-nitrobenzoyl)-L-phenylalaninamide
Homo sapiens
-
pH and temperature not specified in the publication
0.01954
N-[(4S,5S,7R)-5-hydroxy-2,7-dimethyl-8-[(2-methylpropyl)amino]-8-oxooctan-4-yl]-Nalpha-[(2Z)-3-[4-(trifluoromethyl)phenyl]prop-2-enoyl]-L-phenylalaninamide
Homo sapiens
-
pH and temperature not specified in the publication
0.000002
N-[(5R)-5-amino-5-methyl-4,16-dioxo-14-phenyl-3-oxa-15-azatricyclo[15.3.1.17,11]docosa-1(21),7(22),8,10,17,19-hexaen-19-yl]-N-methylmethanesulfonamide
Homo sapiens
-
-
0.0286
N-[(Z)-[(4,6-dimethylpyrimidin-2-yl)amino][(3-nitrophenyl)amino]methylidene]-10H-phenothiazine-10-carboxamide
Homo sapiens
-
in 50 mM Tris (pH 7.5), at 25°C
0.000005
N-[1-(3,5-difluorobenzyl)-2-hydroxy-3-[(3-iodobenzyl)amino]propyl]-5-methyl-N'-propylbenzene-1,3-dicarboxamide
Homo sapiens
-
-
0.0028
N-[2-(3,4-dimethoxyphenyl)ethyl]-2-[(6-[[4,6-di(piperidin-1-yl)-1,3,5-triazin-2-yl]amino]-1,3-benzothiazol-2-yl)sulfanyl]acetamide
Homo sapiens
-
in 50 mM Tris (pH 7.5), at 25°C
0.1
N-[5-(2,3-dichlorobenzyl)-1,3-thiazol-2-yl]-4-([[4-phenyl-5-(pyridin-4-yl)-4H-1,2,4-triazol-3-yl]sulfanyl]methyl)benzamide
Homo sapiens
-
IC50 above 0.1 mM, in 50 mM Tris (pH 7.5), at 25°C
0.000004 - 0.000013
N2-acetyl-3-(butylsulfonyl)-N-[(2S,3R)-1-(3,5-difluorophenyl)-4-[(3-ethylbenzyl)amino]-3-hydroxybutan-2-yl]-D-alaninamide
0.0161
N3-((2S,3R)-4-(cyclopropylamino)-3-hydroxy-1-phenylbutan-2-yl)-2,4,6-trimethyl-1-(methylsulfonyl)-N5-((R)-1-phenylethyl)-1,4-dihydropyridine-3,5-dicarboxamide
Homo sapiens
-
pH and temperature not specified in the publication
0.0162
N3-((2S,3R)-4-(cyclopropylamino)-3-hydroxy-1-phenylbutan-2-yl)-4-ethyl-2,6-dimethyl-1-(methylsulfonyl)-N5-((R)-1-phenylethyl)-1,4-dihydropyridine-3,5-dicarboxamide
Homo sapiens
-
pH and temperature not specified in the publication
0.00807
Nalpha-(1,3-benzodioxol-5-ylcarbonyl)-N-[(4S,5S,7R)-5-hydroxy-2,7-dimethyl-8-[(2-methylpropyl)amino]-8-oxooctan-4-yl]-L-phenylalaninamide
Homo sapiens
-
pH and temperature not specified in the publication
0.00424
Nalpha-(2,4-dichlorobenzoyl)-N-[(4S,5S,7R)-5-hydroxy-2,7-dimethyl-8-[(2-methylpropyl)amino]-8-oxooctan-4-yl]-4-nitro-L-phenylalaninamide
Homo sapiens
-
pH and temperature not specified in the publication
0.00381
Nalpha-(3,4-dimethoxybenzoyl)-N-[(4S,5S,7R)-5-hydroxy-2,7-dimethyl-8-[(2-methylpropyl)amino]-8-oxooctan-4-yl]-4-nitro-L-phenylalaninamide
Homo sapiens
-
pH and temperature not specified in the publication
0.00693
Nalpha-benzoyl-N-[(4S,5S,7R)-5-hydroxy-2,7-dimethyl-8-[(2-methylpropyl)amino]-8-oxooctan-4-yl]-L-phenylalaninamide
Homo sapiens
-
pH and temperature not specified in the publication
0.000017
NB-216
Homo sapiens
-
pH and temperature not specified in the publication
0.000006
OM00-3
Homo sapiens
-
pH and temperature not specified in the publication
0.0000024 - 0.0007
OM99-2
0.02119 - 0.482
pepstatin A
0.00213
phlorofurofucoeckol-A
Homo sapiens
-
in 50 mM sodium acetate, pH 4.5, at 25°C
0.03647
phloroglucinol
Homo sapiens
-
in 50 mM sodium acetate, pH 4.5, at 25°C
0.000004
pyridin-3-ylmethyl [(2S)-1-([(2S,3R)-1-(3,5-difluorophenyl)-4-[(3-ethylbenzyl)amino]-3-hydroxybutan-2-yl]amino)-3-(heptan-4-ylsulfonyl)-1-oxopropan-2-yl]carbamate
Homo sapiens
-
pH and temperature not specified in the publication
0.000003
pyridin-4-ylmethyl [(2S)-1-([(2S,3R)-1-(3,5-difluorophenyl)-4-[(3-ethylbenzyl)amino]-3-hydroxybutan-2-yl]amino)-3-(heptan-4-ylsulfonyl)-1-oxopropan-2-yl]carbamate
Homo sapiens
-
pH and temperature not specified in the publication
0.01082
quercetin
Homo sapiens
-
in 50 mM sodium acetate, pH 4.5, at 25°C
0.000015
S-(tetrahydrofuran-3-yl) [(2S)-3-(butylsulfonyl)-1-([(2S,3R)-1-(3,5-difluorophenyl)-4-[(3-ethylbenzyl)amino]-3-hydroxybutan-2-yl]amino)-1-oxopropan-2-yl]carbamothioate
Homo sapiens
-
pH and temperature not specified in the publication
0.0304
tert-butyl 5-((2S,3R)-3-hydroxy-4-(3-methoxyphenylamino)-1-phenylbutan-2-ylcarbamoyl)-1-(2-isopropoxy-2-oxoethyl)-4-propyl-1,4-dihydropyridine-3-carboxylate
Homo sapiens
-
pH and temperature not specified in the publication
0.0319
tert-butyl 5-((2S,3R)-4-(cyclopropylamino)-3-hydroxy-1-phenylbutan-2-ylcarbamoyl)-1-(2-isopropoxy-2-oxoethyl)-4-methyl-1,4-dihydropyridine-3-carboxylate
Homo sapiens
-
pH and temperature not specified in the publication
0.0246
tert-butyl 5-((2S,3R)-4-(cyclopropylamino)-3-hydroxy-1-phenylbutan-2-ylcarbamoyl)-1-(2-isopropoxy-2-oxoethyl)-4-propyl-1,4-dihydropyridine-3-carboxylate
Homo sapiens
-
pH and temperature not specified in the publication
0.01168
triphloroethol A
Homo sapiens
-
in 50 mM sodium acetate, pH 4.5, at 25°C
additional information
additional information
Homo sapiens
beta-secretase inhibitors with a hydroxymethylcarbonyl (HMC) isostere used as a substrate transition-state mimic, potent BACE1 inhibitory activities of about 0.0012 mM IC50 shown, BACE1 inhibitors with a 5-membered ring at the P3 position and their BACE1 inhibitory activities summarized
-
0.00311
(-)-gallocatechin gallate
Homo sapiens
-
free enzyme, pH and temperature not specified in the publication
0.1275
(-)-gallocatechin gallate
Homo sapiens
-
enzyme reactor-immobilized enzyme, pH and temperature not specified in the publication
0.00017
(1R,3S)-3-[(1S)-1-(acetylamino)-2-methylpropyl]-N-[(2S,3S,5R)-6-(butylamino)-3-hydroxy-5-methyl-6-oxo-1-phenylhexan-2-yl]cyclohexanecarboxamide
Homo sapiens
-
pH and temperature not specified in the publication
0.0008
(1R,3S)-3-[(1S)-1-(acetylamino)-2-methylpropyl]-N-[(2S,3S,5R)-6-(butylamino)-3-hydroxy-5-methyl-6-oxo-1-phenylhexan-2-yl]cyclohexanecarboxamide
Homo sapiens
-
pH and temperature not specified in the publication
0.0015
(1R,3S)-3-[1-(acetylamino)cyclopentyl]-N-[(2S,3S,5R)-6-(butylamino)-3-hydroxy-5-methyl-6-oxo-1-phenylhexan-2-yl]cyclohexanecarboxamide
Homo sapiens
-
pH and temperature not specified in the publication
0.0027
(1R,3S)-3-[1-(acetylamino)cyclopentyl]-N-[(2S,3S,5R)-6-(butylamino)-3-hydroxy-5-methyl-6-oxo-1-phenylhexan-2-yl]cyclohexanecarboxamide
Homo sapiens
-
pH and temperature not specified in the publication
0.0038
(1R,3S)-3-[2-(acetylamino)propan-2-yl]-N-[(2S,3S)-3-hydroxy-1-phenyl-4-[[3-(propan-2-yl)benzyl]amino]butan-2-yl]cyclohexanecarboxamide
Homo sapiens
-
pH and temperature not specified in the publication
0.0042
(1R,3S)-3-[2-(acetylamino)propan-2-yl]-N-[(2S,3S)-3-hydroxy-1-phenyl-4-[[3-(propan-2-yl)benzyl]amino]butan-2-yl]cyclohexanecarboxamide
Homo sapiens
-
pH and temperature not specified in the publication
0.00037
(1R,3S)-3-[2-(acetylamino)propan-2-yl]-N-[(2S,3S,5R)-6-(butylamino)-3-hydroxy-5-methyl-6-oxo-1-phenylhexan-2-yl]cyclohexanecarboxamide
Homo sapiens
-
pH and temperature not specified in the publication
0.0037
(1R,3S)-3-[2-(acetylamino)propan-2-yl]-N-[(2S,3S,5R)-6-(butylamino)-3-hydroxy-5-methyl-6-oxo-1-phenylhexan-2-yl]cyclohexanecarboxamide
Homo sapiens
-
pH and temperature not specified in the publication
0.0000025
(1R,3S)-N-[(2S,3S)-3-hydroxy-1-phenyl-4-[[3-(propan-2-yl)benzyl]amino]butan-2-yl]-3-[2-(2-oxopiperidin-1-yl)propan-2-yl]cyclohexanecarboxamide
Homo sapiens
-
pH and temperature not specified in the publication
0.00014
(1R,3S)-N-[(2S,3S)-3-hydroxy-1-phenyl-4-[[3-(propan-2-yl)benzyl]amino]butan-2-yl]-3-[2-(2-oxopiperidin-1-yl)propan-2-yl]cyclohexanecarboxamide
Homo sapiens
-
pH and temperature not specified in the publication
0.000025
(1R,3S)-N-[(2S,3S)-3-hydroxy-1-phenyl-4-[[3-(propan-2-yl)benzyl]amino]butan-2-yl]-3-[2-(2-oxopyrrolidin-1-yl)propan-2-yl]cyclohexanecarboxamide
Homo sapiens
-
pH and temperature not specified in the publication
0.00096
(1R,3S)-N-[(2S,3S)-3-hydroxy-1-phenyl-4-[[3-(propan-2-yl)benzyl]amino]butan-2-yl]-3-[2-(2-oxopyrrolidin-1-yl)propan-2-yl]cyclohexanecarboxamide
Homo sapiens
-
pH and temperature not specified in the publication
0.00058
(1R,3S)-N-[(2S,3S)-3-hydroxy-1-phenyl-4-[[3-(propan-2-yl)benzyl]amino]butan-2-yl]-3-[2-(propanoylamino)propan-2-yl]cyclohexanecarboxamide
Homo sapiens
-
pH and temperature not specified in the publication
0.0037
(1R,3S)-N-[(2S,3S)-3-hydroxy-1-phenyl-4-[[3-(propan-2-yl)benzyl]amino]butan-2-yl]-3-[2-(propanoylamino)propan-2-yl]cyclohexanecarboxamide
Homo sapiens
-
pH and temperature not specified in the publication
0.00015
(1R,3S)-N-[(2S,3S)-3-hydroxy-1-phenyl-4-[[3-(propan-2-yl)benzyl]amino]butan-2-yl]-3-[2-[methyl(propanoyl)amino]propan-2-yl]cyclohexanecarboxamide
Homo sapiens
-
pH and temperature not specified in the publication
0.0002
(1R,3S)-N-[(2S,3S)-3-hydroxy-1-phenyl-4-[[3-(propan-2-yl)benzyl]amino]butan-2-yl]-3-[2-[methyl(propanoyl)amino]propan-2-yl]cyclohexanecarboxamide
Homo sapiens
-
pH and temperature not specified in the publication
0.00078
2-amino-5-[3-(2-fluoropyridin-3-yl)phenyl]-5-(4-methoxy-3-methylphenyl)-3-methyl-3,5-dihydro-4H-imidazol-4-one
Homo sapiens
pH and temperature not specified in the publication
0.00078
2-amino-5-[3-(2-fluoropyridin-3-yl)phenyl]-5-(4-methoxy-3-methylphenyl)-3-methyl-3,5-dihydro-4H-imidazol-4-one
Homo sapiens
-
temperature not specified in the publication, in 20 mM Tris-HCl, pH 7.4
0.0000098
beta-secretase inhibitor IV
Homo sapiens
-
using SEVNLDAEFRHDSGYEK-biotin as substrate, in 50 mM sodium acetate, pH 4.5, containing 0.25 mg/ml bovine serum albumin, temperature not specified in the publication
0.0000124
beta-secretase inhibitor IV
Homo sapiens
-
using SEVKMDAEFRHDSGYEK-biotin as substrate, in 50 mM sodium acetate, pH 4.5, containing 0.25 mg/ml bovine serum albumin, temperature not specified in the publication
0.00014
Lys-Thr-Glu-Glu-Ile-Ser-Glu-Val-Asn-[statine(3S,4S)]-Val-Ala-Glu-Phe-OH
Homo sapiens
-
enzyme reactor-immobilized enzyme, pH and temperature not specified in the publication
0.00014
Lys-Thr-Glu-Glu-Ile-Ser-Glu-Val-Asn-[statine(3S,4S)]-Val-Ala-Glu-Phe-OH
Homo sapiens
-
free enzyme, pH and temperature not specified in the publication
0.000015
N-((1S,2R)-1-benzyl-3-cyclopropylamino-2-hydroxy-propyl)-5-(methanesulfonyl-methyl-amino)-N'-((R)-1-phenyl-ethyl)-isophthalamide
Homo sapiens
-
pH and temperature not specified in the publication
0.00046
N-((1S,2R)-1-benzyl-3-cyclopropylamino-2-hydroxy-propyl)-5-(methanesulfonyl-methyl-amino)-N'-((R)-1-phenyl-ethyl)-isophthalamide
Homo sapiens
-
enzyme reactor-immobilized enzyme, pH and temperature not specified in the publication
0.000004
N2-acetyl-3-(butylsulfonyl)-N-[(2S,3R)-1-(3,5-difluorophenyl)-4-[(3-ethylbenzyl)amino]-3-hydroxybutan-2-yl]-D-alaninamide
Homo sapiens
-
pH and temperature not specified in the publication
0.000013
N2-acetyl-3-(butylsulfonyl)-N-[(2S,3R)-1-(3,5-difluorophenyl)-4-[(3-ethylbenzyl)amino]-3-hydroxybutan-2-yl]-D-alaninamide
Homo sapiens
-
pH and temperature not specified in the publication
0.0000024
OM99-2
Homo sapiens
-
using SEVNLDAEFRHDSGYEK-biotin as substrate, in 50 mM sodium acetate, pH 4.5, containing 0.25 mg/ml bovine serum albumin, temperature not specified in the publication
0.0000033
OM99-2
Homo sapiens
-
using SEVKMDAEFRHDSGYEK-biotin as substrate, in 50 mM sodium acetate, pH 4.5, containing 0.25 mg/ml bovine serum albumin, temperature not specified in the publication
0.00004
OM99-2
Homo sapiens
-
free enzyme, pH and temperature not specified in the publication
0.0007
OM99-2
Homo sapiens
-
enzyme reactor-immobilized enzyme, pH and temperature not specified in the publication
0.02119
pepstatin A
Homo sapiens
-
free enzyme, pH and temperature not specified in the publication
0.482
pepstatin A
Homo sapiens
-
enzyme reactor-immobilized enzyme, pH and temperature not specified in the publication
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3.4.23.46 memapsin 2
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The reliability class of the localization prediction ranges from 1 (very reliable) to 5 (not reliable). 
