Reference on EC 3.4.23.46 - memapsin 2
Please use the Reference Search for a specific query.
Please wait a moment until all data is loaded. This message will disappear when all data is loaded.
REF. 
AUTHORS
TITLE
JOURNAL
VOL.
PAGES
YEAR
ORGANISM (UNIPROT)
PUBMED ID
SOURCE
Ghosh, A.K.; Bilcer, G.; Harwood, C.; Kawahama, R.; Shin, D.; Hussain, K.A.; Hong, L.; Loy, J.A.; Nguyen, C.; Koelsch, G.; Ermolieff, J.; Tang, J.
Structure-based design: potent inhibitors of human brain memapsin 2 (beta-secretase)
J. Med. Chem.
44
2865-2868
2001
Homo sapiens
Turner, R.T.3rd.; Loy, J.A.; Nguyen, C.; Devasamudram, T.; Ghosh, A.K.; Koelsch, G.; Tang, J.
Specificity of memapsin 1 and its implications on the design of memapsin 2 (beta-secretase) inhibitor selectivity
Biochemistry
41
8742-8746
2002
Homo sapiens
Turner, R.T.; Koelsch, G.; Hong, L.; Castenheira, P.; Ghosh, A.; Tang, J.
Subsite specificity of memapsin 2 (b-secretase): implications for inhibitor design
Biochemistry
40
10001-10006
2001
Homo sapiens
Hong, L.; Turner, R.T.; Koelsch, G.; Shin, D.; Ghosh, A.K.; Tang, J.
Crystal structure of memapsin 2 (b-secretase) in complex with an inhibitor OM00-3
Biochemistry
41
10963-10967
2002
Homo sapiens
Kennedy, M.E.; Wang, W.; Song, L.; Lee, J.; Zhang, L.; Wong, G.; Wang, L.; Parker, E.
Measuring human beta-secretase (BACE1) activity using homogeneous time-resolved fluorescence
Anal. Biochem.
319
49-55
2003
Homo sapiens
Hong, L.; Koelsch, G.; Lin, X.; Wu, S.; Terzyan, S.; Ghosh, A.K.; Zhang, X.C.; Tang, J.
Structure of the protease domain of memapsin 2 (beta-secretase) complexed with inhibitor
Science
290
150-153
2000
Homo sapiens
Roggo, S.
Inhibition of BACE, a promising approach to Alzheimer's disease therapy
Curr. Top. Med. Chem.
2
359-370
2002
Homo sapiens
Ghosh, A.K.; Hong, L.; Tang, J.
beta-Secretase as a therapeutic target for inhibitor drugs
Curr. Med. Chem.
9
1135-1144
2002
Homo sapiens
Ermolieff, J.; Loy, J.A.; Koelsch, G.; Tang, J.
Proteolytic activation of recombinant pro-memapsin 2 (pro-beta-secretase) studied with new fluorogenic substrates
Biochemistry
39
12450-12456
2000
Homo sapiens
Ehehalt, R.; Michel, B.; De Pietri Tonelli, D.; Zacchetti, D.; Simons, K.; Keller, P.
Splice variants of the beta-site APP-cleaving enzyme BACE1 in human brain and pancreas
Biochem. Biophys. Res. Commun.
293
30-37
2002
Homo sapiens
Luo, Y.; Bolon, B.; Damore, M.A.; Fitzpatrick, D.; Liu, H.; Zhang, J.; Yan, Q.; Vassar, R.; Citron, M.
BACE1 (beta-secretase) knockout mice do not acquire compensatory gene expression changes or develop neural lesions over time
Neurobiol. Dis.
14
81-88
2003
Mus musculus
Yan, R.; Han, P.; Miao, H.; Greengard, P.; Xu, H.
The transmembrane domain of the Alzheimer's b-secretase (BACE1) determines its late Golgi localization and access to beta-amyloid precursor protein (APP) substrate
J. Biol. Chem.
276
36788-36796
2001
Homo sapiens, Mus musculus
Puglielli, L.; Ellis, B.C.; Saunders, A.J.; Kovacs, D.M.
Ceramide stabilizes beta-site amyloid precursor protein-cleaving enzyme 1 and promotes amyloid beta-peptide biogenesis
J. Biol. Chem.
278
19777-19783
2003
Homo sapiens
Kitazume, S.; Tachida, Y.; Oka, R.; Kotani, N.; Ogawa, K.; Suzuki, M.; Dohmae, N.; Takio, K.; Saido, T.C.; Hashimoto, Y.
Characterization of alpha 2,6-sialyltransferase cleavage by Alzheimer's beta -secretase (BACE1)
J. Biol. Chem.
278
14865-14871
2003
Homo sapiens
Tomasselli, A.G.; Qahwash, I.; Emmons, T.L.; Lu, Y.; Leone, J.W.; Lull, J.M.; Fok, K.F.; Bannow, C.A.; Smith, C.W.; Bienkowski, M.J.; Heinrikson, R.L.; Yan, R.
Employing a superior BACE1 cleavage sequence to probe cellular APP processing
J. Neurochem.
84
1006-1017
2003
Homo sapiens
Bruinzeel, W.; Yon, J.; Giovannelli, S.; Masure, S.
Recombinant insect cell expression and purification of human beta-secretase (BACE-1) for X-ray crystallography
Protein Expr. Purif.
26
139-148
2002
Homo sapiens (P56817), Homo sapiens
Beckman, M.; Holsinger, R.M.; Small, D.H.
Heparin activates beta-secretase (BACE1) of Alzheimers disease and increases autocatalysis of the enzyme
Biochemistry
45
6703-6714
2006
Homo sapiens
Kimura, T.; Hamada, Y.; Stochaj, M.; Ikari, H.; Nagamine, A.; Abdel-Rahman, H.; Igawa, N.; Hidaka, K.; Nguyen, J.T.; Saito, K.; Hayashi, Y.; Kiso, Y.
Design and synthesis of potent beta-secretase (BACE1) inhibitors with P1 carboxylic acid bioisosteres
Bioorg. Med. Chem. Lett.
16
2380-2386
2006
Homo sapiens
von Arnim, C.A.; Kinoshita, A.; Peltan, I.D.; Tangredi, M.M.; Herl, L.; Lee, B.M.; Spoelgen, R.; Hshieh, T.T.; Ranganathan, S.; Battey, F.D.; Liu, C.X.; Bacskai, B.J.; Sever, S.; Irizarry, M.C.; Strickland, D.K.; Hyman, B.T.
The low density lipoprotein receptor-related protein (LRP) is a novel beta-secretase (BACE1) substrate
J. Biol. Chem.
280
17777-17785
2005
Homo sapiens
Angeletti, B.; Waldron, K.J.; Freeman, K.B.; Bawagan, H.; Hussain, I.; Miller, C.C.; Lau, K.F.; Tennant, M.E.; Dennison, C.; Robinson, N.J.; Dingwall, C.
BACE1 cytoplasmic domain interacts with the copper chaperone for superoxide dismutase-1 and binds copper
J. Biol. Chem.
280
17930-17937
2005
Rattus norvegicus
Wong, H.K.; Sakurai, T.; Oyama, F.; Kaneko, K.; Wada, K.; Miyazaki, H.; Kurosawa, M.; De Strooper, B.; Saftig, P.; Nukina, N.
beta Subunits of voltage-gated sodium channels are novel substrates of beta-site amyloid precursor protein-cleaving enzyme (BACE1) and gamma-secretase
J. Biol. Chem.
280
23009-23017
2005
Mus musculus
Yang, H.C.; Chai, X.; Mosior, M.; Kohn, W.; Boggs, L.N.; Erickson, J.A.; McClure, D.B.; Yeh, W.K.; Zhang, L.; Gonzalez-DeWhitt, P.; Mayer, J.P.; Martin, J.A.; Hu, J.; Chen, S.H.; Bueno, A.B.; Little, S.P.; McCarthy, J.R.; May, P.C.
Biochemical and kinetic characterization of BACE1: investigation into the putative species-specificity for beta- and beta-cleavage sites by human and murine BACE1
J. Neurochem.
91
1249-1259
2004
Homo sapiens, Mus musculus
Rossner, S.; Lange-Dohna, C.; Zeitschel, U.; Perez-Polo, J.R.
Alzheimers disease beta-secretase BACE1 is not a neuron-specific enzyme
J. Neurochem.
92
226-234
2005
Homo sapiens
Laird, F.M.; Cai, H.; Savonenko, A.V.; Farah, M.H.; He, K.; Melnikova, T.; Wen, H.; Chiang, H.C.; Xu, G.; Koliatsos, V.E.; Borchelt, D.R.; Price, D.L.; Lee, H.K.; Wong, P.C.
BACE1, a major determinant of selective vulnerability of the brain to amyloid-beta amyloidogenesis, is essential for cognitive, emotional, and synaptic functions
J. Neurosci.
25
11693-11709
2005
Mus musculus
Zuechner, T.; Perez-Polo, J.R.; Schliebs, R.
beta-Secretase BACE1 is differentially controlled through muscarinic acetylcholine receptor signaling
J. Neurosci. Res.
77
250-257
2004
Homo sapiens
Hattori, C.; Asai, M.; Onishi, H.; Sasagawa, N.; Hashimoto, Y.; Saido, T.C.; Maruyama, K.; Mizutani, S.; Ishiura, S.
BACE1 interacts with lipid raft proteins
J. Neurosci. Res.
84
912-917
2006
Homo sapiens
Harada, H.; Tamaoka, A.; Ishii, K.; Shoji, S.; Kametaka, S.; Kametani, F.; Saito, Y.; Murayama, S.
Beta-site APP cleaving enzyme 1 (BACE1) is increased in remaining neurons in Alzheimers disease brains
Neurosci. Res.
54
24-29
2006
Homo sapiens
Sardana, V.; Xu, B.; Zugay-Murphy, J.; Chen, Z.; Sardana, M.; Darke, P.L.; Munshi, S.; Kuo, L.C.
A general procedure for the purification of human beta-secretase expressed in Escherichia coli
Protein Expr. Purif.
34
190-196
2004
Homo sapiens (P56817), Homo sapiens
Willem, M.; Garratt, A.N.; Novak, B.; Citron, M.; Kaufmann, S.; Rittger, A.; Destrooper, B.; Saftig, P.; Birchmeier, C.; Haass, C.
Control of peripheral nerve myelination by the {beta}-secretase BACE1
Science
314
664-666
2006
Mus musculus
Schechter, I.; Ziv, E.
Kinetic properties of cathepsin D and BACE 1 indicate the need to search for additional beta-secretase candidate(s)
Biol. Chem.
389
313-320
2008
Homo sapiens
Choi, S.H.; Hur, J.M.; Yang, E.J.; Jun, M.; Park, H.J.; Lee, K.B.; Moon, E.; Song, K.S.
Beta-secretase (BACE1) inhibitors from Perilla frutescens var. acuta
Arch. Pharm. Res.
31
183-187
2008
Perilla frutescens
Costantini, C.; Ko, M.H.; Jonas, M.C.; Puglielli, L.
A reversible form of lysine acetylation in the ER and Golgi lumen controls the molecular stabilization of BACE1
Biochem. J.
407
383-395
2007
Homo sapiens (P56817)
Dingwall, C.
A copper-binding site in the cytoplasmic domain of BACE1 identifies a possible link to metal homoeostasis and oxidative stress in Alzheimers disease
Biochem. Soc. Trans.
35
571-573
2007
Homo sapiens (P56817)
Stockley, J.H.; O'Neill, C.
The proteins BACE1 and BACE2 and beta-secretase activity in normal and Alzheimers disease brain
Biochem. Soc. Trans.
35
574-576
2007
Homo sapiens (P56817), Homo sapiens
Hamada, Y.; Igawa, N.; Ikari, H.; Ziora, Z.; Nguyen, J.T.; Yamani, A.; Hidaka, K.; Kimura, T.; Saito, K.; Hayashi, Y.; Ebina, M.; Ishiura, S.; Kiso, Y.
beta-Secretase inhibitors: modification at the P4 position and improvement of inhibitory activity in cultured cells
Bioorg. Med. Chem. Lett.
16
4354-4359
2006
Homo sapiens (P56817)
Fobare, W.F.; Solvibile, W.R.; Robichaud, A.J.; Malamas, M.S.; Manas, E.; Turner, J.; Hu, Y.; Wagner, E.; Chopra, R.; Cowling, R.; Jin, G.; Bard, J.
Thiophene substituted acylguanidines as BACE1 inhibitors
Bioorg. Med. Chem. Lett.
17
5353-5356
2007
Homo sapiens (P56817)
Hamada, Y.; Ohta, H.; Miyamoto, N.; Yamaguchi, R.; Yamani, A.; Hidaka, K.; Kimura, T.; Saito, K.; Hayashi, Y.; Ishiura, S.; Kiso, Y.
Novel non-peptidic and small-sized BACE1 inhibitors
Bioorg. Med. Chem. Lett.
18
1643-1647
2008
Homo sapiens (P56817)
Cole, S.L.; Vassar, R.
BACE1 structure and function in health and Alzheimers disease
Curr. Alzheimer Res.
5
100-120
2008
Homo sapiens (P56817)
Ghosh, A.K.; Kumaragurubaran, N.; Hong, L.; Koelsh, G.; Tang, J.
Memapsin 2 (beta-secretase) inhibitors: drug development
Curr. Alzheimer Res.
5
121-131
2008
Homo sapiens (P56817), Mus musculus (P56818)
Stockley, J.H.; Ravid, R.; ONeill, C.
Altered beta-secretase enzyme kinetics and levels of both BACE1 and BACE2 in the Alzheimers disease brain
FEBS Lett.
580
6550-6560
2006
Homo sapiens (P56817)
Lahiri, D.K.; Maloney, B.; Ge, Y.W.
BACE1 gene promoter is differentially regulated: detection of a novel promoter region for its cell type-specific regulation
J. Mol. Neurosci.
28
193-210
2006
Homo sapiens (P56817)
Tamagno, E.; Guglielmotto, M.; Aragno, M.; Borghi, R.; Autelli, R.; Giliberto, L.; Muraca, G.; Danni, O.; Zhu, X.; Smith, M.A.; Perry, G.; Jo, D.G.; Mattson, M.P.; Tabaton, M.
Oxidative stress activates a positive feedback between the gamma- and beta-secretase cleavages of the beta-amyloid precursor protein
J. Neurochem.
104
683-695
2008
Mus musculus (P56818), Mus musculus BalbC (P56818)
Shimizu, H.; Tosaki, A.; Kaneko, K.; Hisano, T.; Sakurai, T.; Nukina, N.
Crystal structure of an active form of BACE1: an enzyme responsible for amyloid {beta} protein production
Mol. Cell. Biol.
28
3663-3671
2008
Homo sapiens (P56817)
Kim, D.Y.; Carey, B.W.; Wang, H.; Ingano, L.A.; Binshtok, A.M.; Wertz, M.H.; Pettingell, W.H.; He, P.; Lee, V.M.; Woolf, C.J.; Kovacs, D.M.
BACE1 regulates voltage-gated sodium channels and neuronal activity
Nat. Cell Biol.
9
755-764
2007
Homo sapiens (P56817), Homo sapiens, Mus musculus (P56818)
Hu, X.; Hicks, C.W.; He, W.; Wong, P.; Macklin, W.B.; Trapp, B.D.; Yan, R.
BACE1 modulates myelination in the central and peripheral nervous system
Nat. Neurosci.
9
1520-1525
2006
Mus musculus (P56818)
Fukuzaki, E.; Takuma, K.; Himeno, Y.; Yoshida, S.; Funatsu, Y.; Kitahara, Y.; Mizoguchi, H.; Ibi, D.; Koike, K.; Inoue, M.; Yamada, K.
Enhanced activity of hippocampal BACE1 in a mouse model of postmenopausal memory deficits
Neurosci. Lett.
433
141-145
2008
Mus musculus (P56818), Mus musculus
Zhu, Y.; Xiao, K.; Ma, L.; Xiong, B.; Fu, Y.; Yu, H.; Wang, W.; Wang, X.; Hu, D.; Peng, H.; Li, J.; Gong, Q.; Chai, Q.; Tang, X.; Zhang, H.; Li, J.; Shen, J.
Design, synthesis and biological evaluation of novel dual inhibitors of acetylcholinesterase and beta-secretase
Bioorg. Med. Chem.
17
1600-1613
2009
Homo sapiens, Mus musculus
Boehme, L.; Hoffmann, T.; Manhart, S.; Wolf, R.; Demuth, H.U.
Isoaspartate containing amyloid precursor protein derived peptides alter efficacy and specificity of potential beta-secretases
Biol. Chem.
389
1055-1066
2008
Homo sapiens
Ghosh, A.K.; Kumaragurubaran, N.; Hong, L.; Kulkarni, S.; Xu, X.; Miller, H.B.; Reddy, D.S.; Weerasena, V.; Turner, R.; Chang, W.; Koelsch, G.; Tang, J.
Potent memapsin 2 (beta-secretase) inhibitors: design, synthesis, protein-ligand X-ray structure, and in vivo evaluation
Bioorg. Med. Chem. Lett.
18
1031-1036
2008
Homo sapiens, Mus musculus
Fujimoto, T.; Matsushita, Y.; Gouda, H.; Yamaotsu, N.; Hirono, S.
In silico multi-filter screening approaches for developing novel beta-secretase inhibitors
Bioorg. Med. Chem. Lett.
18
2771-2775
2008
Homo sapiens
Machauer, R.; Veenstra, S.; Rondeau, J.M.; Tintelnot-Blomley, M.; Betschart, C.; Neumann, U.; Paganetti, P.
Structure-based design and synthesis of macrocyclic peptidomimetic beta-secretase (BACE-1) inhibitors
Bioorg. Med. Chem. Lett.
19
1361-1365
2009
Homo sapiens (P56817)
Machauer, R.; Laumen, K.; Veenstra, S.; Rondeau, J.M.; Tintelnot-Blomley, M.; Betschart, C.; Jaton, A.L.; Desrayaud, S.; Staufenbiel, M.; Rabe, S.; Paganetti, P.; Neumann, U.
Macrocyclic peptidomimetic beta-secretase (BACE-1) inhibitors with activity in vivo
Bioorg. Med. Chem. Lett.
19
1366-1370
2009
Mus musculus, Homo sapiens (P56817)
Steele, T.G.; Hills, I.D.; Nomland, A.A.; de Leon, P.; Allison, T.; McGaughey, G.; Colussi, D.; Tugusheva, K.; Haugabook, S.J.; Espeseth, A.S.; Zuck, P.; Graham, S.L.; Stachel, S.J.
Identification of a small molecule beta-secretase inhibitor that binds without catalytic aspartate engagement
Bioorg. Med. Chem. Lett.
19
17-20
2009
Homo sapiens
Yu, C.J.; Wang, W.Z.; Liu, W.
beta-Secretase inhibitor increases amyloid-beta precursor protein level in rat brain cortical primary neurons induced by okadaic acid
Chin. Med. Sci.
121
1439-1444
2008
Rattus norvegicus
Wu, G.; Sankaranarayanan, S.; Tugusheva, K.; Kahana, J.; Seabrook, G.; Shi, X.P.; King, E.; Devanarayan, V.; Cook, J.J.; Simon, A.J.
Decrease in age-adjusted cerebrospinal fluid beta-secretase activity in Alzheimer's subjects
Clin. Biochem.
41
986-996
2008
Homo sapiens, Macaca mulatta
Miyoshi, K.; Ohyagi, Y.; Sakae, N.; Motomura, K.; Ma, L.; Taniwaki, T.; Furuya, H.; Tabira, T.; Kira, J.
Enhancement of activation of caspases by presenilin 1 gene mutations and its inhibition by secretase inhibitors
J. Alzheimers Dis.
16
551-564
2009
Homo sapiens
Ma, L.; Ohyagi, Y.; Miyoshi, K.; Sakae, N.; Motomura, K.; Taniwaki, T.; Furuya, H.; Takeda, K.; Tabira, T.; Kira, J.
Increase in p53 protein levels by presenilin 1 gene mutations and its inhibition by secretase inhibitors
J. Alzheimers Dis.
16
565-575
2009
Homo sapiens
Grimm, M.O.; Grimm, H.S.; Tomic, I.; Beyreuther, K.; Hartmann, T.; Bergmann, C.
Independent inhibition of Alzheimer disease beta- and gamma-secretase cleavage by lowered cholesterol levels
J. Biol. Chem.
283
11302-11311
2008
Homo sapiens
Hook, V.Y.; Kindy, M.; Hook, G.
Inhibitors of cathepsin B improve memory and reduce beta-amyloid in transgenic Alzheimer disease mice expressing the wild-type, but not the Swedish mutant, beta-secretase site of the amyloid precursor protein
J. Biol. Chem.
283
7745-7753
2008
Mus musculus
Barrow, J.C.; Stauffer, S.R.; Rittle, K.E.; Ngo, P.L.; Yang, Z.; Selnick, H.G.; Graham, S.L.; Munshi, S.; McGaughey, G.B.; Holloway, M.K.; Simon, A.J.; Price, E.A.; Sankaranarayanan, S.; Colussi, D.; Tugusheva, K.; Lai, M.T.; Espeseth, A.S.; Xu, M.; Huang, Q.; Wolfe, A.; Pietrak, B.; Zuck, P.; Levorse, D.A.; Haz, H.a.z.u.
Discovery and X-ray crystallographic analysis of a spiropiperidine iminohydantoin inhibitor of beta-secretase
J. Med. Chem.
51
6259-6262
2008
Homo sapiens
Liu, W.W.; Todd, S.; Coulson, D.T.; Irvine, G.B.; Passmore, A.P.; McGuinness, B.; McConville, M.; Craig, D.; Johnston, J.A.
A novel reciprocal and biphasic relationship between membrane cholesterol and beta-secretase activity in SH-SY5Y cells and in human platelets
J. Neurochem.
108
341-349
2009
Homo sapiens
Faghihi, M.A.; Modarresi, F.; Khalil, A.M.; Wood, D.E.; Sahagan, B.G.; Morgan, T.E.; Finch, C.E.; St Laurent, G.; Kenny, P.J.; Wahlestedt, C.
Expression of a noncoding RNA is elevated in Alzheimers disease and drives rapid feed-forward regulation of beta-secretase
Nat. Med.
14
723-730
2008
Homo sapiens, Mus musculus
Jo, D.G.; Arumugam, T.V.; Woo, H.N.; Park, J.S.; Tang, S.C.; Mughal, M.; Hyun, D.H.; Park, J.H.; Choi, Y.H.; Gwon, A.R.; Camandola, S.; Cheng, A.; Cai, H.; Song, W.; Markesbery, W.R.; Mattson, M.P.
Evidence that gamma-secretase mediates oxidative stress-induced beta-secretase expression in Alzheimers disease
Neurobiol. Aging
31
917-925
2008
Homo sapiens, Mus musculus, Rattus norvegicus
Zhang, Q.; Yang, G.; Li, W.; Fan, Z.; Sun, A.; Luo, J.; Ke, Z.J.
Thiamine deficiency increases beta-secretase activity and accumulation of beta-amyloid peptides
Neurobiol. Aging
32
42-53
2011
Homo sapiens, Mus musculus
Laws, S.M.; Eckart, K.; Friedrich, P.; Kurz, A.; Foerstl, H.; Riemenschneider, M.
Lack of evidence to support the association of polymorphisms within the alpha- and beta-secretase genes (ADAM10/BACE1) with Alzheimers disease
Neurobiol. Aging
32
541-543
2011
Homo sapiens
Xiong, M.; Zhang, T.; Zhang, L.M.; Lu, S.D.; Huang, Y.L.; Sun, F.Y.
Caspase inhibition attenuates accumulation of beta-amyloid by reducing beta-secretase production and activity in rat brains after stroke
Neurobiol. Dis.
32
433-441
2008
Rattus norvegicus
Patey, S.J.; Edwards, E.A.; Yates, E.A.; Turnbull, J.E.
Engineered heparins: novel beta-secretase inhibitors as potential Alzheimers disease therapeutics
Neurodegener. Dis.
5
197-199
2008
Homo sapiens
Todd, S.; McKnight, A.J.; Liu, W.W.; Carson, R.; Heggarty, S.; McGuinness, B.; Irvine, G.B.; Craig, D.; Passmore, A.P.; Johnston, J.A.
BACE1 polymorphisms do not influence platelet membrane beta-secretase activity or genetic susceptibility for Alzheimers disease in the Northern Irish population
Neuromolecular Med.
10
368-376
2008
Homo sapiens
Wen, Y.; Yu, W.H.; Maloney, B.; Bailey, J.; Ma, J.; Marie, I.; Maurin, T.; Wang, L.; Figueroa, H.; Herman, M.; Krishnamurthy, P.; Liu, L.; Planel, E.; Lau, L.F.; Lahiri, D.K.; Duff, K.
Transcriptional regulation of beta-secretase by p25/cdk5 leads to enhanced amyloidogenic processing
Neuron
57
680-690
2008
Mus musculus
Ghosh, A.K.; Gemma, S.; Tang, J.
beta-Secretase as a therapeutic target for Alzheimer's disease
Neurotherapeutics
5
399-408
2008
Homo sapiens
Lv, L.; Yang, Q.Y.; Zhao, Y.; Yao, C.S.; Sun, Y.; Yang, E.J.; Song, K.S.; Mook-Jung, I.; Fang, W.S.
BACE1 (beta-secretase) inhibitory chromone glycosides from Aloe vera and Aloe nobilis
Planta Med.
74
540-545
2008
Homo sapiens, Rattus norvegicus
Augustin, S.; Huebbe, P.; Matzner, N.; Augustin, K.; Schliebs, R.; Cermak, R.; Wolffram, S.; Rimbach, G.
Ginkgo biloba extract and its flavonol and terpenelactone fractions do not affect beta-secretase mRNA and enzyme activity levels in cultured neurons and in mice
Planta Med.
74
6-13
2008
Homo sapiens
Hebert, S.S.; Horre, K.; Nicolai, L.; Papadopoulou, A.S.; Mandemakers, W.; Silahtaroglu, A.N.; Kauppinen, S.; Delacourte, A.; De Strooper, B.
Loss of microRNA cluster miR-29a/b-1 in sporadic Alzheimers disease correlates with increased BACE1/beta-secretase expression
Proc. Natl. Acad. Sci. USA
105
6415-6420
2008
Homo sapiens
Rajendran, L.; Schneider, A.; Schlechtingen, G.; Weidlich, S.; Ries, J.; Braxmeier, T.; Schwille, P.; Schulz, J.B.; Schroeder, C.; Simons, M.; Jennings, G.; Knoelker, H.J.; Simons, K.
Efficient inhibition of the Alzheimer's disease beta-secretase by membrane targeting
Science
320
520-523
2008
Homo sapiens
Chae, S.S.; Yoo, C.B.; Jo, C.; Yun, S.M.; Jo, S.A.; Koh, Y.H.
Caspases-2 and -8 are involved in the presenilin1/gamma-secretase-dependent cleavage of amyloid precursor protein after the induction of apoptosis
J. Neurosci. Res.
88
1926-1933
2010
Homo sapiens
Koike, M.A.; Green, K.N.; Blurton-Jones, M.; Laferla, F.M.
Oligemic hypoperfusion differentially affects Tau and amyloid-beta
Am. J. Pathol.
177
300-310
2010
Mus musculus
Kosicek, M.; Malnar, M.; Goate, A.; Hecimovic, S.
Cholesterol accumulation in Niemann Pick type C (NPC) model cells causes a shift in APP localization to lipid rafts
Biochem. Biophys. Res. Commun.
393
404-409
2010
Cricetulus griseus
Kihara, T.; Shimmyo, Y.; Akaike, A.; Niidome, T.; Sugimoto, H.
Abeta-induced BACE-1 cleaves N-terminal sequence of mPGES-2
Biochem. Biophys. Res. Commun.
393
728-733
2010
Homo sapiens
Kasturirangan, S.; Boddapati, S.; Sierks, M.R.
Engineered proteolytic nanobodies reduce Abeta burden and ameliorate Abeta-induced cytotoxicity
Biochemistry
49
4501-4508
2010
Homo sapiens
Malnar, M.; Kosicek, M.; Mitterreiter, S.; Omerbasic, D.; Lichtenthaler, S.F.; Goate, A.; Hecimovic, S.
Niemann Pick type C cells show cholesterol dependent decrease of APP expression at the cell surface its increased processing through the beta-secretase pathway
Biochim. Biophys. Acta
1802
682-691
2010
Cricetulus griseus
Xu, W.; Chen, G.; Liew, O.W.; Zuo, Z.; Jiang, H.; Zhu, W.
Novel non-peptide beta-secretase inhibitors derived from structure-based virtual screening and bioassay
Bioorg. Med. Chem. Lett.
19
3188-3192
2009
Homo sapiens
Huber, T.; Manzenrieder, F.; Kuttruff, C.A.; Dorner-Ciossek, C.; Kessler, H.
Prolonged stability by cyclization: Macrocyclic phosphino dipeptide isostere inhibitors of beta-secretase (BACE1)
Bioorg. Med. Chem. Lett.
19
4427-4431
2009
Homo sapiens
Hills, I.D.; Holloway, M.K.; de Leon, P.; Nomland, A.; Zhu, H.; Rajapakse, H.; Allison, T.J.; Munshi, S.K.; Colussi, D.; Pietrak, B.L.; Toolan, D.; Haugabook, S.J.; Graham, S.L.; Stachel, S.J.
A conformational constraint improves a beta-secretase inhibitor but for an unexpected reason
Bioorg. Med. Chem. Lett.
19
4993-4995
2009
Homo sapiens
Hanessian, S.; Shao, Z.; Betschart, C.; Rondeau, J.M.; Neumann, U.; Tintelnot-Blomley, M.
Structure-based design and synthesis of novel P2/P3 modified, non-peptidic beta-secretase (BACE-1) inhibitors
Bioorg. Med. Chem. Lett.
20
1924-1927
2010
Homo sapiens
Malamas, M.S.; Barnes, K.; Hui, Y.; Johnson, M.; Lovering, F.; Condon, J.; Fobare, W.; Solvibile, W.; Turner, J.; Hu, Y.; Manas, E.S.; Fan, K.; Olland, A.; Chopra, R.; Bard, J.; Pangalos, M.N.; Reinhart, P.; Robichaud, A.J.
Novel pyrrolyl 2-aminopyridines as potent and selective human beta-secretase (BACE1) inhibitors
Bioorg. Med. Chem. Lett.
20
2068-2073
2010
Homo sapiens
Huang, Y.; Strobel, E.D.; Ho, C.Y.; Reynolds, C.H.; Conway, K.A.; Piesvaux, J.A.; Brenneman, D.E.; Yohrling, G.J.; Moore Arnold, H.; Rosenthal, D.; Alexander, R.S.; Tounge, B.A.; Mercken, M.; Vandermeeren, M.; Parker, M.H.; Reitz, A.B.; Baxter, E.W.
Macrocyclic BACE inhibitors: Optimization of a micromolar hit to nanomolar leads
Bioorg. Med. Chem. Lett.
20
3158-3160
2010
Homo sapiens
Jung, H.A.; Oh, S.H.; Choi, J.S.
Molecular docking studies of phlorotannins from Eisenia bicyclis with BACE1 inhibitory activity
Bioorg. Med. Chem. Lett.
20
3211-3215
2010
Homo sapiens
Lerchner, A.; Machauer, R.; Betschart, C.; Veenstra, S.; Rueeger, H.; McCarthy, C.; Tintelnot-Blomley, M.; Jaton, A.L.; Rabe, S.; Desrayaud, S.; Enz, A.; Staufenbiel, M.; Paganetti, P.; Rondeau, J.M.; Neumann, U.
Macrocyclic BACE-1 inhibitors acutely reduce Abeta in brain after po application
Bioorg. Med. Chem. Lett.
20
603-607
2010
Homo sapiens
Bjoerklund, C.; Adolfsson, H.; Jansson, K.; Lindberg, J.; Vrang, L.; Hallberg, A.; Rosenquist, S.; Samuelsson, B.
Discovery of potent BACE-1 inhibitors containing a new hydroxyethylene (HE) scaffold: exploration of P1 alkoxy residues and an aminoethylene (AE) central core
Bioorg. Med. Chem.
18
1711-1723
2010
Homo sapiens (P56817)
Al-Nadaf, A.; Abu Sheikha, G.; Taha, M.O.
Elaborate ligand-based pharmacophore exploration and QSAR analysis guide the synthesis of novel pyridinium-based potent beta-secretase inhibitory leads
Bioorg. Med. Chem.
18
3088-3115
2010
Homo sapiens
Marumoto, S.; Miyazawa, M.
Biotransformation of isoimperatorin and imperatorin by Glomerella cingulata and beta-secretase inhibitory activity
Bioorg. Med. Chem.
18
455-459
2010
Homo sapiens
Malamas, M.S.; Barnes, K.; Johnson, M.; Hui, Y.; Zhou, P.; Turner, J.; Hu, Y.; Wagner, E.; Fan, K.; Chopra, R.; Olland, A.; Bard, J.; Pangalos, M.; Reinhart, P.; Robichaud, A.J.
Di-substituted pyridinyl aminohydantoins as potent and highly selective human beta-secretase (BACE1) inhibitors
Bioorg. Med. Chem.
18
630-639
2010
Homo sapiens
Arslanova, D.; Yang, T.; Xu, X.; Wong, S.T.; Augelli-Szafran, C.E.; Xia, W.
Phenotypic analysis of images of zebrafish treated with Alzheimers gamma-secretase inhibitors
BMC Biotechnol.
10
24
2010
Danio rerio
Miners, J.S.; van Helmond, Z.; Kehoe, P.G.; Love, S.
Changes with age in the activities of beta-secretase and the Abeta-degrading enzymes neprilysin, insulin-degrading enzyme and angiotensin-converting enzyme
Brain Pathol.
20
794-802
2010
Homo sapiens
Burgos, P.V.; Mardones, G.A.; Rojas, A.L.; daSilva, L.L.; Prabhu, Y.; Hurley, J.H.; Bonifacino, J.S.
Sorting of the Alzheimers disease amyloid precursor protein mediated by the AP-4 complex
Dev. Cell
18
425-436
2010
Homo sapiens
Niu, Y.; Wang, Y.; Zou, X.; Yang, X.; Ma, C.; Lue, Y.; Zhou, B.; Yuan, Y.; Du, G.; Xu, P.
Synthesis and preliminary evaluation of peptidomimetic inhibitors of human beta-secretase
Eur. J. Med. Chem.
45
2089-2094
2010
Homo sapiens
Choi, S.J.; Cho, J.H.; Im, I.; Lee, S.D.; Jang, J.Y.; Oh, Y.M.; Jung, Y.K.; Jeon, E.S.; Kim, Y.C.
Design and synthesis of 1,4-dihydropyridine derivatives as BACE-1 inhibitors
Eur. J. Med. Chem.
45
2578-2590
2010
Homo sapiens
Devi, L.; Ohno, M.
Genetic reductions of beta-site amyloid precursor protein-cleaving enzyme 1 and amyloid-beta ameliorate impairment of conditioned taste aversion memory in 5XFAD Alzheimers disease model mice
Eur. J. Neurosci.
31
110-118
2010
Mus musculus
Nie, J.; Luo, Y.; Huang, X.N.; Gong, Q.H.; Wu, Q.; Shi, J.S.
Icariin inhibits beta-amyloid peptide segment 25-35 induced expression of beta-secretase in rat hippocampus
Eur. J. Pharmacol.
626
213-218
2010
Rattus norvegicus
Drott, J.; Desire, L.; Drouin, D.; Pando, M.; Haun, F.
Etazolate improves performance in a foraging and homing task in aged rats
Eur. J. Pharmacol.
634
95-100
2010
Rattus norvegicus
Lazarov, O.; Marr, R.A.
Neurogenesis and Alzheimers disease: at the crossroads
Exp. Neurol.
223
267-281
2010
Homo sapiens
Portelius, E.; Brinkmalm, G.; Tran, A.; Andreasson, U.; Zetterberg, H.; Westman-Brinkmalm, A.; Blennow, K.; Ohrfelt, A.
Identification of novel N-terminal fragments of amyloid precursor protein in cerebrospinal fluid
Exp. Neurol.
223
351-358
2010
Homo sapiens
Sala Frigerio, C.; Fadeeva, J.V.; Minogue, A.M.; Citron, M.; Van Leuven, F.; Staufenbiel, M.; Paganetti, P.; Selkoe, D.J.; Walsh, D.M.
beta-Secretase cleavage is not required for generation of the intracellular C-terminal domain of the amyloid precursor family of proteins
FEBS J.
277
1503-1518
2010
Homo sapiens
Bloch, L.; Sineshchekova, O.; Reichenbach, D.; Reiss, K.; Saftig, P.; Kuro-o, M.; Kaether, C.
Klotho is a substrate for alpha-, beta- and gamma-secretase
FEBS Lett.
583
3221-3224
2009
Homo sapiens
Lee, S.; Das, H.K.
Transcriptional regulation of the presenilin-1 gene controls gamma-secretase activity
Front. Biosci.
2
22-35
2010
Homo sapiens
Marumoto, S.; Miyazawa, M.
Biotransformation of bergapten and xanthotoxin by Glomerella cingulata
J. Agric. Food Chem.
58
7777-7781
2010
Homo sapiens
Kojro, E.; Fueger, P.; Prinzen, C.; Kanarek, A.M.; Rat, D.; Endres, K.; Fahrenholz, F.; Postina, R.
Statins and the squalene Ssnthase inhibitor zaragozic acid stimulate the non-amyloidogenic pathway of amyloid-beta protein precursor processing by suppression of cholesterol synthesis
J. Alzheimers Dis.
20
1215-1231
2010
Homo sapiens
Yamakawa, H.; Yagishita, S.; Futai, E.; Ishiura, S.
beta-Secretase inhibitor potency is decreased by aberrant beta-cleavage location of the "Swedish mutant" amyloid precursor protein
J. Biol. Chem.
285
1634-1642
2010
Homo sapiens
Heilig, E.A.; Xia, W.; Shen, J.; Kelleher, R.J.
A presenilin-1 mutation identified in familial Alzheimers disease with cotton wool plaques causes nearly complete loss of gamma-secretase activity
J. Biol. Chem.
285
22350-22359
2010
Homo sapiens
Zhang, C.; Browne, A.; Child, D.; Divito, J.R.; Stevenson, J.A.; Tanzi, R.E.
Loss of function of ATXN1 increases amyloid beta-protein levels by potentiating beta-secretase processing of beta-amyloid precursor protein
J. Biol. Chem.
285
8515-8526
2010
Homo sapiens
Al-Tel, T.H.; Al-Qawasmeh, R.A.; Schmidt, M.F.; Al-Aboudi, A.; Rao, S.N.; Sabri, S.S.; Voelter, W.
Rational design and synthesis of potent dibenzazepine motifs as beta-secretase inhibitors
J. Med. Chem.
52
6484-6488
2009
Homo sapiens
Malamas, M.S.; Erdei, J.; Gunawan, I.; Turner, J.; Hu, Y.; Wagner, E.; Fan, K.; Chopra, R.; Olland, A.; Bard, J.; Jacobsen, S.; Magolda, R.L.; Pangalos, M.; Robichaud, A.J.
Design and synthesis of 5,5-disubstituted aminohydantoins as potent and selective human beta-secretase (BACE1) inhibitors
J. Med. Chem.
53
1146-1158
2010
Homo sapiens, Homo sapiens (P56817), Mus musculus
Ahmed, R.R.; Holler, C.J.; Webb, R.L.; Li, F.; Beckett, T.L.; Murphy, M.P.
BACE1 and BACE2 enzymatic activities in Alzheimers disease
J. Neurochem.
112
1045-1053
2010
Homo sapiens
Klaver, D.W.; Wilce, M.C.; Gasperini, R.; Freeman, C.; Juliano, J.P.; Parish, C.; Foa, L.; Aguilar, M.I.; Small, D.H.
Glycosaminoglycan-induced activation of the beta-secretase (BACE1) of Alzheimers disease
J. Neurochem.
112
1552-1561
2010
Homo sapiens (P56817)
McAllister, C.; Long, J.; Bowers, A.; Walker, A.; Cao, P.; Honda, S.; Harada, N.; Staufenbiel, M.; Shen, Y.; Li, R.
Genetic targeting aromatase in male amyloid precursor protein transgenic mice down-regulates beta-secretase (BACE1) and prevents Alzheimer-like pathology and cognitive impairment
J. Neurosci.
30
7326-7334
2010
Mus musculus
Mancini, F.; Andrisano, V.
Development of a liquid chromatographic system with fluorescent detection for beta-secretase immobilized enzyme reactor on-line enzymatic studies
J. Pharm. Biomed. Anal.
52
355-361
2010
Homo sapiens
Pandey, A.; Mungalpara, J.; Mohan, C.G.
Comparative molecular field analysis and comparative molecular similarity indices analysis of hydroxyethylamine derivatives as selective human BACE-1 inhibitor
Mol. Divers.
14
39-49
2010
Homo sapiens
Kobayashi, S.; Sasaki, T.; Katayama, T.; Hasegawa, T.; Nagano, A.; Sato, K.
Temporal-spatial expression of presenilin 1 and the production of amyloid-beta after acute spinal cord injury in adult rat
Neurochem. Int.
56
387-393
2010
Rattus norvegicus
Carson, R.; McKnight, A.J.; Todd, S.; Liu, W.W.; Heggarty, S.; Craig, D.; McGuinness, B.; Irvine, G.B.; Passmore, A.P.; Johnston, J.A.
Variation in RTN3 and PPIL2 genes does not influence platelet membrane beta-secretase activity or susceptibility to Alzheimers disease in the northern Irish population
Neuromolecular Med.
11
337-344
2009
Homo sapiens
Heath, J.E.; Siedlak, S.L.; Zhu, X.; Lee, H.G.; Thakur, A.; Yan, R.; Perry, G.; Smith, M.A.; Castellani, R.J.
Widespread distribution of reticulon-3 in various neurodegenerative diseases
Neuropathology
30
574-579
2010
Homo sapiens
Ray, B.; Banerjee, P.K.; Greig, N.H.; Lahiri, D.K.
Memantine treatment decreases levels of secreted Alzheimers amyloid precursor protein (APP) and amyloid beta (Abeta) peptide in the human neuroblastoma cells
Neurosci. Lett.
470
1-5
2010
Homo sapiens
Zhang, T.; Pan, B.S.; Zhao, B.; Zhang, L.M.; Huang, Y.L.; Sun, F.Y.
Exacerbation of poststroke dementia by type 2 diabetes is associated with synergistic increases of beta-secretase activation and beta-amyloid generation in rat brains
Neuroscience
161
1045-1056
2009
Rattus norvegicus
Huebbe, P.; Wagner, A.E.; Boesch-Saadatmandi, C.; Sellmer, F.; Wolffram, S.; Rimbach, G.
Effect of dietary quercetin on brain quercetin levels and the expression of antioxidant and Alzheimers disease relevant genes in mice
Pharmacol. Res.
61
242-246
2010
Mus musculus
Marumoto, S.; Miyazawa, M.
beta-Secretase inhibitory effects of furanocoumarins from the root of Angelica dahurica
Phytother. Res.
24
510-513
2010
Homo sapiens
Hemming, M.L.; Elias, J.E.; Gygi, S.P.; Selkoe, D.J.
Identification of beta-secretase (BACE1) substrates using quantitative proteomics
PLoS ONE
4
e8477
2009
Homo sapiens
Chen, T.J.; Hung, H.S.; Wang, D.C.; Chen, S.S.
The protective effect of ROCK inhibitor on aluminum-induced neurotoxicity in rat cortical neurons
Toxicol. Sci.
116
264-272
2010
Rattus norvegicus
Zhou, P.; Li, Y.; Fan, Y.; Wang, Z.; Chopra, R.; Olland, A.; Hu, Y.; Magolda, R.L.; Pangalos, M.; Reinhart, P.H.; Turner, M.J.; Bard, J.; Malamas, M.S.; Robichaud, A.J.
Pyridinyl aminohydantoins as small molecule BACE1 inhibitors
Bioorg. Med. Chem. Lett.
20
2326-2329
2010
Homo sapiens
Sasaki, H.; Miki, K.; Kinoshita, K.; Koyama, K.; Juliawaty, L.D.; Achmad, S.A.; Hakim, E.H.; Kaneda, M.; Takahashi, K.
beta-Secretase (BACE-1) inhibitory effect of biflavonoids
Bioorg. Med. Chem. Lett.
20
4558-4560
2010
Homo sapiens (P56817)
Xu, W.; Chen, G.; Zhu, W.; Zuo, Z.
Molecular docking and structure-activity relationship studies on benzothiazole based non-peptidic BACE-1 inhibitors
Bioorg. Med. Chem. Lett.
20
6203-6207
2010
Homo sapiens (P56817)
Cho, J.K.; Ryu, Y.B.; Curtis-Long, M.J.; Kim, J.Y.; Kim, D.; Lee, S.; Lee, W.S.; Park, K.H.
Inhibition and structural reliability of prenylated flavones from the stem bark of Morus lhou on beta-secretase (BACE-1)
Bioorg. Med. Chem. Lett.
21
2945-2948
2011
Homo sapiens
Bertini, S.; Asso, V.; Ghilardi, E.; Granchi, C.; Manera, C.; Minutolo, F.; Saccomanni, G.; Bortolato, A.; Mason, J.; Moro, S.; MacChia, M.
Carbazole-containing arylcarboxamides as BACE1 inhibitors
Bioorg. Med. Chem. Lett.
21
6657-6661
2011
Homo sapiens (P56817)
Thompson, L.A.; Shi, J.; Decicco, C.P.; Tebben, A.J.; Olson, R.E.; Boy, K.M.; Guernon, J.M.; Good, A.C.; Liauw, A.; Zheng, C.; Copeland, R.A.; Combs, A.P.; Trainor, G.L.; Camac, D.M.; Muckelbauer, J.K.; Lentz, K.A.; Grace, J.E.; Burton, C.R.; Toyn, J.H.; Barten, D.M.; Marcinkeviciene, J.; Meredith, J.E.; Albright, C.F.
Synthesis and in vivo evaluation of cyclic diaminopropane BACE-1 inhibitors
Bioorg. Med. Chem. Lett.
21
6909-6915
2011
Mus musculus, Homo sapiens (P56817)
Chiriano, G.; De Simone, A.; Mancini, F.; Perez, D.I.; Cavalli, A.; Bolognesi, M.L.; Legname, G.; Martinez, A.; Andrisano, V.; Carloni, P.; Roberti, M.
A small chemical library of 2-aminoimidazole derivatives as BACE-1 inhibitors: Structure-based design, synthesis, and biological evaluation
Eur. J. Med. Chem.
48
206-213
2012
Homo sapiens
Andreoli, F.; Doukara, A.L.; Mehdid, M.A.; Vanthuyne, N.; Roussel, C.; Dessolin, J.; Kraus, J.L.
Novel phenyl(thio)ureas bearing (thio)oxothiazoline group as potential BACE-1 inhibitors: synthesis and biological evaluation
J. Enzyme Inhib. Med. Chem.
28
153-162
2013
Homo sapiens (P56817)
Cheng, Y.; Judd, T.C.; Bartberger, M.D.; Brown, J.; Chen, K.; Fremeau, R.T.; Hickman, D.; Hitchcock, S.A.; Jordan, B.; Li, V.; Lopez, P.; Louie, S.W.; Luo, Y.; Michelsen, K.; Nixey, T.; Powers, T.S.; Rattan, C.; Sickmier, E.A.; St Jean, D.J.; Wahl, R.C.; Wen, P.H.; Wood, S.
From fragment screening to in vivo efficacy: optimization of a series of 2-aminoquinolines as potent inhibitors of beta-site amyloid precursor protein cleaving enzyme 1 (BACE1)
J. Med. Chem.
54
5836-5857
2011
Homo sapiens, Rattus norvegicus
Al-Tel, T.; Semreen, M.; Al-Qawasmeh, R.; Schmidt, M.; El-Awadi, R.; Ardah, M.; Zaarour, R.; Rao, S.; El-Agnaf, O.
Design, synthesis, and qualitative structure-activity evaluations of novel beta-secretase inhibitors as potential Alzheimers drug leads
J. Med. Chem.
54
8373-8385
2011
Homo sapiens (P56817)
Farah, M.H.; Pan, B.H.; Hoffman, P.N.; Ferraris, D.; Tsukamoto, T.; Nguyen, T.; Wong, P.C.; Price, D.L.; Slusher, B.S.; Griffin, J.W.
Reduced BACE1 activity enhances clearance of myelin debris and regeneration of axons in the injured peripheral nervous system
J. Neurosci.
31
5744-5754
2011
Mus musculus
Takasugi, N.; Sasaki, T.; Suzuki, K.; Osawa, S.; Isshiki, H.; Hori, Y.; Shimada, N.; Higo, T.; Yokoshima, S.; Fukuyama, T.; Lee, V.M.; Trojanowski, J.Q.; Tomita, T.; Iwatsubo, T.
BACE1 activity is modulated by cell-associated sphingosine-1-phosphate
J. Neurosci.
31
6850-6857
2011
Homo sapiens, Mus musculus
Mouton-Liger, F.; Paquet, C.; Dumurgier, J.; Bouras, C.; Pradier, L.; Gray, F.; Hugon, J.
Oxidative stress increases BACE1 protein levels through activation of the PKR-eIF2? pathway
Biochim. Biophys. Acta
1822
885-896
2012
Homo sapiens
Hamada, Y.; Suzuki, K.; Nakanishi, T.; Sarma, D.; Ohta, H.; Yamaguchi, R.; Yamasaki, M.; Hidaka, K.; Ishiura, S.; Kiso, Y.
Structure-activity relationship study of BACE1 inhibitors possessing a chelidonic or 2,6-pyridinedicarboxylic scaffold at the P(2) position
Bioorg. Med. Chem. Lett.
24
618-623
2014
Homo sapiens (P56817)
Rueeger, H.; Lueoend, R.; Rogel, O.; Rondeau, J.M.; Moebitz, H.; Machauer, R.; Jacobson, L.; Staufenbiel, M.; Desrayaud, S.; Neumann, U.
Discovery of cyclic sulfone hydroxyethylamines as potent and selective beta-site APP-cleaving enzyme 1 (BACE1) inhibitors: structure-based design and in vivo reduction of amyloid beta-peptides
Bioorg. Med. Chem.
23
5300-5306
2013
Homo sapiens (P56817)
Cai, J.; Qi, X.; Kociok, N.; Skosyrski, S.; Emilio, A.; Ruan, Q.; Han, S.; Liu, L.; Chen, Z.; Bowes Rickman, C.; Golde, T.; Grant, M.B.; Saftig, P.; Serneels, L.; de Strooper, B.; Joussen, A.M.; Boulton, M.E.
beta-Secretase (BACE1) inhibition causes retinal pathology by vascular dysregulation and accumulation of age pigment
EMBO Mol. Med.
4
980-991
2012
Mus musculus (P56818)
Zou, Y.; Xu, L.; Chen, W.; Zhu, Y.; Chen, T.; Fu, Y.; Li, L.; Ma, L.; Xiong, B.; Wang, X.; Li, J.; He, J.; Zhang, H.; Xu, Y.; Li, J.; Shen, J.
Discovery of pyrazole as C-terminus of selective BACE1 inhibitors
Eur. J. Med. Chem.
68
270-283
2013
Homo sapiens (P56817)
Stuetzer, I.; Selevsek, N.; Esterhazy, D.; Schmidt, A.; Aebersold, R.; Stoffel, M.
Systematic proteomic analysis identifies beta-site amyloid precursor protein cleaving enzyme 2 and 1 (BACE2 and BACE1) substrates in pancreatic beta-cells
J. Biol. Chem.
288
10536-10547
2013
Mus musculus (P56818)
Ghosh, A.K.; Venkateswara Rao, K.; Yadav, N.D.; Anderson, D.D.; Gavande, N.; Huang, X.; Terzyan, S.; Tang, J.
Structure-based design of highly selective beta-secretase inhibitors: synthesis, biological evaluation, and protein-ligand X-ray crystal structure
J. Med. Chem.
55
9195-9207
2012
Homo sapiens (P56817)
Mandal, M.; Zhu, Z.; Cumming, J.N.; Liu, X.; Strickland, C.; Mazzola, R.D.; Caldwell, J.P.; Leach, P.; Grzelak, M.; Hyde, L.; Zhang, Q.; Terracina, G.; Zhang, L.; Chen, X.; Kuvelkar, R.; Kennedy, M.E.; Favreau, L.; Cox, K.; Orth, P.; Buevich, A.; Voigt, J.; Wang, H.; Kazakevich, I.; McKittrick, B.A.; Greenleew, W.; Parker, E.M.; Stamford, A.W.
Design and validation of bicyclic iminopyrimidinones as beta amyloid cleaving enzyme-1 (BACE1) inhibitors: conformational constraint to favor a bioactive conformation
J. Med. Chem.
55
9331-9345
2012
Homo sapiens (P56817)
Thomas, A.A.; Hunt, K.W.; Newhouse, B.; Watts, R.J.; Liu, X.; Vigers, G.; Smith, D.; Rhodes, S.P.; Brown, K.D.; Otten, J.N.; Burkard, M.; Cox, A.A.; Geck Do, M.K.; Dutcher, D.; Rana, S.; DeLisle, R.K.; Regal, K.; Wright, A.D.; Groneberg, R.; Liao, J.; Scearce-Levie, K.; Siu, M.; Purkey, H.E.; Lyssikatos, J.P.
8-Tetrahydropyran-2-yl chromans: highly selective beta-site amyloid precursor protein cleaving enzyme 1 (BACE1) inhibitors
J. Med. Chem.
57
10112-10129
2014
Homo sapiens (P56817)
Dineen, T.A.; Chen, K.; Cheng, A.C.; Derakhchan, K.; Epstein, O.; Esmay, J.; Hickman, D.; Kreiman, C.E.; Marx, I.E.; Wahl, R.C.; Wen, P.H.; Weiss, M.M.; Whittington, D.A.; Wood, S.; Fremeau, R.T.; White, R.D.; Patel, V.F.
Inhibitors of ?-site amyloid precursor protein cleaving enzyme (BACE1): identification of (S)-7-(2-fluoropyridin-3-yl)-3-((3-methyloxetan-3-yl)ethynyl)-5H-spiro[chromeno[2,3-b]pyridine-5,4-oxazol]-2-amine (AMG-8718)
J. Med. Chem.
57
9811-9831
2014
Homo sapiens (P56817)
Butler, C.R.; Brodney, M.A.; Beck, E.M.; Barreiro, G.; Nolan, C.E.; Pan, F.; Vajdos, F.; Parris, K.; Varghese, A.H.; Helal, C.J.; Lira, R.; Doran, S.D.; Riddell, D.R.; Buzon, L.M.; Dutra, J.K.; Martinez-Alsina, L.A.; Ogilvie, K.; Murray, J.C.; Young, J.M.; Atchison, K.; Robshaw, A.; Gonzales, C.; Wang, J.; Zhang, Y.; O'Neill, B.T.
Discovery of a series of efficient, centrally efficacious BACE1 inhibitors through structure-based drug design
J. Med. Chem.
58
2678-2702
2015
Homo sapiens (P56817)
van Bebber, F.; Hruscha, A.; Willem, M.; Schmid, B.; Haass, C.
Loss of Bace2 in zebrafish affects melanocyte migration and is distinct from Bace1 knock out phenotypes
J. Neurochem.
127
471-481
2013
Danio rerio (Q6NZT7), Danio rerio
Georgievska, B.; Gustavsson, S.; Lundkvist, J.; Neelissen, J.; Eketjaell, S.; Ramberg, V.; Bueters, T.; Agerman, K.; Jureus, A.; Svensson, S.; Berg, S.; Faelting, J.; Lendahl, U.
Revisiting the peripheral sink hypothesis: inhibiting BACE1 activity in the periphery does not alter beta-amyloid levels in the CNS
J. Neurochem.
132
477-486
2015
Mus musculus (P56818), Mus musculus
Wu, G.; Sankaranarayanan, S.; Wong, J.; Tugusheva, K.; Michener, M.S.; Shi, X.; Cook, J.J.; Simon, A.J.; Savage, M.J.
Characterization of plasma beta-secretase (BACE1) activity and soluble amyloid precursor proteins as potential biomarkers for Alzheimer's disease
J. Neurosci. Res.
90
2247-2258
2012
Homo sapiens, Macaca mulatta
Gautam, V.; DAvanzo, C.; Hebisch, M.; Kovacs, D.; Kim, D.
BACE1 activity regulates cell surface contactin-2 levels
Mol. Neurodegener.
9
004
2014
Cricetulus griseus
Mirsafian, H.; Mat Ripen, A.; Merican, A.F.; Bin Mohamad, S.
Amino acid sequence and structural comparison of BACE1 and BACE2 using evolutionary trace method
ScientificWorldJournal
2014
482463
2014
Homo sapiens (P56817)
Winneroski, L.L.; Schiffler, M.A.; Erickson, J.A.; May, P.C.; Monk, S.A.; Timm, D.E.; Audia, J.E.; Beck, J.P.; Boggs, L.N.; Borders, A.R.; Boyer, R.D.; Brier, R.A.; Hudziak, K.J.; Klimkowski, V.J.; Garcia Losada, P.; Mathes, B.M.; Stout, S.L.; Watson, B.M.; Mergott, D.J.
Preparation and biological evaluation of conformationally constrained BACE1 inhibitors
Bioorg. Med. Chem.
23
3260-3268
2015
Homo sapiens (P56817)
Innocenti, R.; Lenci, E.; Menchi, G.; Pupi, A.; Trabocchi, A.
Design and synthesis of bicyclic acetals as beta secretase (BACE1) inhibitors
Bioorg. Med. Chem.
25
5077-5083
2017
Homo sapiens (P56817)
Ghosh, A.K.; Ghosh, K.; Brindisi, M.; Lendy, E.K.; Yen, Y.C.; Kumaragurubaran, N.; Huang, X.; Tang, J.; Mesecar, A.D.
Design, synthesis, X-ray studies, and biological evaluation of novel BACE1 inhibitors with bicyclic isoxazoline carboxamides as the P3 ligand
Bioorg. Med. Chem. Lett.
28
2605-2610
2018
Homo sapiens (P56817)
Vnencak, M.; Schoelvinck, M.L.; Schwarzacher, S.W.; Deller, T.; Willem, M.; Jedlicka, P.
Lack of beta-amyloid cleaving enzyme-1 (BACE1) impairs long-term synaptic plasticity but enhances granule cell excitability and oscillatory activity in the dentate gyrus in vivo
Brain Struct. Funct.
224
1279-1290
2019
Mus musculus (P56818)
Ghosh, A.K.; Reddy, B.S.; Yen, Y.C.; Cardenas, E.; Rao, K.V.; Downs, D.; Huang, X.; Tang, J.; Mesecar, A.D.
Design of potent and highly selective inhibitors for human beta-secretase 2 (memapsin 1), a target for type 2 diabetes
Chem. Sci.
7
3117-3122
2016
Homo sapiens (P56817)
Ghosh, A.K.; Brindisi, M.; Yen, Y.C.; Lendy, E.K.; Kovela, S.; Cardenas, E.L.; Reddy, B.S.; Rao, K.V.; Downs, D.; Huang, X.; Tang, J.; Mesecar, A.D.
Highly selective and potent human beta-secretase 2 (BACE2) inhibitors against type 2 diabetes design, synthesis, X-ray structure and structure-activity relationship studies
ChemMedChem
14
545-560
2019
Homo sapiens (P56817), Homo sapiens
Yu, T.; Paudel, P.; Seong, S.H.; Kim, J.A.; Jung, H.A.; Choi, J.S.
Computational insights into beta-site amyloid precursor protein enzyme 1 (BACE1) inhibition by tanshinones and salvianolic acids from Salvia miltiorrhiza via molecular docking simulations
Comput. Biol. Chem.
74
273-285
2018
Homo sapiens (P56817)
Yan, G.; Hao, L.; Niu, Y.; Huang, W.; Wang, W.; Xu, F.; Liang, L.; Wang, C.; Jin, H.; Xu, P.
2-Substituted-thio-N-(4-substituted-thiazol/1H-imidazol-2-yl)acetamides as BACE1 inhibitors Synthesis, biological evaluation and docking studies
Eur. J. Med. Chem.
137
462-475
2017
Homo sapiens (P56817)
Azimi, S.; Zonouzi, A.; Firuzi, O.; Iraji, A.; Saeedi, M.; Mahdavi, M.; Edraki, N.
Discovery of imidazopyridines containing isoindoline-1,3-dione framework as a new class of BACE1 inhibitors Design, synthesis and SAR analysis
Eur. J. Med. Chem.
138
729-737
2017
Homo sapiens (P56817)
Chlebek, J.; De Simone, A.; Hostalkova, A.; Opletal, L.; Perez, C.; Perez, D.I.; Havlikova, L.; Cahlikova, L.; Andrisano, V.
Application of BACE1 immobilized enzyme reactor for the characterization of multifunctional alkaloids from Corydalis cava (Fumariaceae) as Alzheimers disease targets
Fitoterapia
109
241-247
2016
Homo sapiens (P56817)
Ellis, C.R.; Shen, J.
pH-Dependent population shift regulates BACE1 activity and inhibition
J. Am. Chem. Soc.
137
9543-9546
2015
Homo sapiens (P56817)
Manoharan, P.; Chennoju, K.; Ghoshal, N.
Computational analysis of BACE1-ligand complex crystal structures and linear discriminant analysis for identification of BACE1 inhibitors with anti P-glycoprotein binding property
J. Biomol. Struct. Dyn.
36
262-276
2018
Homo sapiens (P56817)
Gutierrez, L.J.; Parravicini, O.; Sanchez, E.; Rodriguez, R.; Cobo, J.; Enriz, R.D.
New substituted aminopyrimidine derivatives as BACE1 inhibitors in silico design, synthesis and biological assays
J. Biomol. Struct. Dyn.
37
229-246
2019
Homo sapiens (P56817)
Wu, Y.J.; Guernon, J.; Shi, J.; Marcin, L.; Higgins, M.; Rajamani, R.; Muckelbauer, J.; Lewis, H.; Chang, C.; Camac, D.; Toyn, J.H.; Ahlijanian, M.K.; Albright, C.F.; Macor, J.E.; Thompson, L.A.
Discovery of S3-truncated, C-6 heteroaryl substituted aminothiazine beta-site APP cleaving enzyme-1 (BACE1) inhibitors
J. Med. Chem.
59
8593-8600
2016
Mus musculus (P56818)
Fujimoto, K.; Matsuoka, E.; Asada, N.; Tadano, G.; Yamamoto, T.; Nakahara, K.; Fuchino, K.; Ito, H.; Kanegawa, N.; Moechars, D.; Gijsen, H.J.M.; Kusakabe, K.I.
Structure-based design of selective beta-site amyloid precursor protein cleaving enzyme 1 (BACE1) inhibitors targeting the flap to gain selectivity over BACE2
J. Med. Chem.
62
5080-5095
2019
Homo sapiens (P56817)
Kumalo, H.M.; Soliman, M.E.
A comparative molecular dynamics study on BACE1 and BACE2 flap flexibility
J. Recept. Signal Transduct. Res.
36
505-514
2016
Homo sapiens (P56817)
Manoharan, P.; Chennoju, K.; Ghoshal, N.
Target specific proteochemometric model development for BACE1 - protein flexibility and structural water are critical in virtual screening
Mol. Biosyst.
11
1955-1972
2015
Homo sapiens (P56817)
Dislich, B.; Wohlrab, F.; Bachhuber, T.; Mueller, S.A.; Kuhn, P.H.; Hogl, S.; Meyer-Luehmann, M.; Lichtenthaler, S.F.
Label-free quantitative proteomics of mouse cerebrospinal fluid detects beta-site APP cleaving enzyme (BACE1) protease substrates in vivo
Mol. Cell. Proteomics
14
2550-2563
2015
Mus musculus (P56818), Mus musculus
Tallon, C.; Rockenstein, E.; Masliah, E.; Farah, M.H.
Increased BACE1 activity inhibits peripheral nerve regeneration after injury
Neurobiol. Dis.
106
147-157
2017
Mus musculus (P56818), Mus musculus
html completed
