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2-{[(1-{[(2S)-3-methyl-2-sulfanylbutanoyl]amino}cyclopentyl)carbonyl]amino}-3-(naphthalen-1-yl)propanoic acid
-
2-{[(1-{[(2S)-3-methyl-2-sulfanylbutanoyl]amino}cyclopentyl)carbonyl]amino}-3-(naphthalen-2-yl)propanoic acid
-
2-{[(1-{[(2S)-3-methyl-2-sulfanylbutanoyl]amino}cyclopentyl)carbonyl]amino}-3-[3'-(trifluoromethyl)biphenyl-4-yl]propanoic acid
-
3-(2'-methoxybiphenyl-4-yl)-2-{[(1-{[(2S)-3-methyl-2-sulfanylbutanoyl]amino}cyclopentyl)carbonyl]amino}propanoic acid
-
3-(2,3'-bipyridin-5'-yl)-N-[(1-{[(2S)-3-methyl-2-sulfanylbutanoyl]amino}cyclopentyl)carbonyl]alanine
-
3-(3'-chloro-4'-fluorobiphenyl-4-yl)-2-{[(1-{[(2S)-3-methyl-2-sulfanylbutanoyl]amino}cyclopentyl)carbonyl]amino}propanoic acid
-
3-(4'-chlorobiphenyl-4-yl)-2-{[(1-{[(2S)-3-methyl-2-sulfanylbutanoyl]amino}cyclopentyl)carbonyl]amino}propanoic acid
-
3-(4'-fluorobiphenyl-4-yl)-2-{[(1-{[(2S)-3-methyl-2-sulfanylbutanoyl]amino}cyclopentyl)carbonyl]amino}propanoic acid
-
3-(biphenyl-4-yl)-2-[({1-[(2-methyl-2-sulfanylpropanoyl)amino]cyclopentyl}carbonyl)amino]propanoic acid
-
3-(biphenyl-4-yl)-2-{[(1-{[(2R)-2-sulfanylhexanoyl]amino}cyclopentyl)carbonyl]amino}propanoic acid
-
3-(biphenyl-4-yl)-2-{[(1-{[(2R)-3-hydroxy-2-sulfanylpropanoyl]amino}cyclopentyl)carbonyl]amino}propanoic acid
-
3-(biphenyl-4-yl)-2-{[(1-{[(2R)-3-methoxy-2-sulfanylpropanoyl]amino}cyclopentyl)carbonyl]amino}propanoic acid
-
3-(biphenyl-4-yl)-2-{[(1-{[(2R)-3-phenyl-2-sulfanylpropanoyl]amino}cyclopentyl)carbonyl]amino}propanoic acid
-
3-(biphenyl-4-yl)-2-{[(1-{[(2R)-4-(methylsulfanyl)-2-sulfanylbutanoyl]amino}cyclopentyl)carbonyl]amino}propanoic acid
-
3-(biphenyl-4-yl)-2-{[(1-{[(2R)-4-methyl-2-sulfanylpentanoyl]amino}cyclopentyl)carbonyl]amino}propanoic acid
-
3-(biphenyl-4-yl)-2-{[(1-{[(2S)-2-sulfanylhexanoyl]amino}cyclopentyl)carbonyl]amino}propanoic acid
-
3-(biphenyl-4-yl)-2-{[(1-{[(2S)-3-methyl-2-sulfanylpentanoyl]amino}cyclopentyl)carbonyl]amino}propanoic acid
-
3-(biphenyl-4-yl)-2-{[(1-{[(2S)-4-methyl-2-sulfanylpentanoyl]amino}cyclopentyl)carbonyl]amino}propanoic acid
-
3-(biphenyl-4-yl)-2-{[(1-{[(3S)-3-methoxy-2-sulfanylbutanoyl]amino}cyclopentyl)carbonyl]amino}propanoic acid
-
3-(biphenyl-4-yl)-2-{[(1-{[(3S)-3-methyl-2-sulfanylpentanoyl]amino}cyclopentyl)carbonyl]amino}propanoic acid
-
3-[4-(furan-2-yl)pyrimidin-5-yl]-N-[(1-{[(2S)-3-methyl-2-sulfanylbutanoyl]amino}cyclopentyl)carbonyl]alanine
-
3-[4-(furan-3-yl)pyrimidin-5-yl]-N-[(1-{[(2S)-3-methyl-2-sulfanylbutanoyl]amino}cyclopentyl)carbonyl]alanine
-
3-[5-(2-methoxyphenyl)pyridin-3-yl]-N-[(1-{[(2S)-3-methyl-2-sulfanylbutanoyl]amino}cyclopentyl)carbonyl]alanine
-
3-[6-(3-aminophenyl)pyridin-3-yl]-N-[(1-{[(2S)-3-methyl-2-sulfanylbutanoyl]amino}cyclopentyl)carbonyl]alanine
-
3-{6-[3-(acetylamino)phenyl]pyridin-3-yl}-N-[(1-{[(2S)-3-methyl-2-sulfanylbutanoyl]amino}cyclopentyl)carbonyl]alanine
-
4-cyclohexyl-N-[(1-{[(2S)-3-methyl-2-sulfanylbutanoyl]amino}cyclopentyl)carbonyl]phenylalanine
-
4-furan-2-yl-N-[(1-{[(2S)-3-methyl-2-sulfanylbutanoyl]amino}cyclopentyl)carbonyl]phenylalanine
-
N-(alpha-L-rhamnopyranosyl-oxyhydroxy-phosphinyl)-L-Leu-L-Trp
mechanism of inhibitor binding analysed (cocrystallization)
N-[(1-{[(2R)-2-sulfanylhexanoyl]amino}cyclopentyl)carbonyl]-3-[4-(thiophen-3-yl)pyrimidin-5-yl]alanine
-
N-[(1-{[(2R)-2-sulfanylpentanoyl]amino}cyclopentyl)carbonyl]-3-[4-(thiophen-3-yl)pyrimidin-5-yl]alanine
-
N-[(1-{[(2S)-2-sulfanylhexanoyl]amino}cyclopentyl)carbonyl]-3-[4-(thiophen-3-yl)pyrimidin-5-yl]alanine
-
N-[(1-{[(2S)-2-sulfanylpentanoyl]amino}cyclopentyl)carbonyl]-3-[4-(thiophen-3-yl)pyrimidin-5-yl]alanine
-
N-[(1-{[(2S)-3-cyclohexyl-2-sulfanylpropanoyl]amino}cyclopentyl)carbonyl]-3-[4-(thiophen-3-yl)pyrimidin-5-yl]alanine
-
N-[(1-{[(2S)-3-methyl-2-sulfanylbutanoyl]amino}cyclopentyl)carbonyl]-3-(4-phenylpyrimidin-5-yl)alanine
-
N-[(1-{[(2S)-3-methyl-2-sulfanylbutanoyl]amino}cyclopentyl)carbonyl]-3-[4-(thiophen-3-yl)pyrimidin-5-yl]alanine
-
N-[(1-{[(2S)-3-methyl-2-sulfanylbutanoyl]amino}cyclopentyl)carbonyl]-3-[6-(3-nitrophenyl)pyridin-3-yl]alanine
-
N-[(1-{[(2S)-3-methyl-2-sulfanylbutanoyl]amino}cyclopentyl)carbonyl]-4-thiophen-3-ylphenylalanine
-
N-[(1-{[(2S)-4-(methylsulfanyl)-2-sulfanylbutanoyl]amino}cyclopentyl)carbonyl]-3-[4-(thiophen-3-yl)pyrimidin-5-yl]alanine
-
N-[(1-{[(2S)-4-methyl-2-sulfanylpentanoyl]amino}cyclopentyl)carbonyl]-3-[4-(thiophen-3-yl)pyrimidin-5-yl]alanine
-
SM19712
selective inhibitor, 0.01 mM used in inhibition assay conditions
(2R,3R,4R,5R)-(2S)-(4-[2-(1,3-dioxo-1H,3H-benzo[de]isoquinolin-2-yl)ethyl]-3-isobutyl-5-phosphonopyrrolidine-2-carbonyl-amino)-3-(1H-indol-3-yl)propionic acid
-
0.01 mM, 91% inhibition of enzyme activity
(2R,4S,5R,6R)-(2S)-(5-[2-(1,3-dioxo-1H,3H-benzo[de]isoquinolin-2-yl)ethyl]-4-isobutyl-6-phosphonopiperidine-2-carbonyl-amino)-3-(1H-indol-3-yl)propionic acid
-
0.01 mM, 98% inhibition of enzyme activity
(2S)-2-((3-[hydroxyl(2-phenyl-(1R)-1-([(benzyloxy)carbonyl]-amino)ethyl)phosphinyl]-(2R)-2-[(3-phenylisoxazol-5-yl)methyl]-1-oxopropyl)amino) 1H-Indole-3-propanoic acid
-
-
(2S)-2-((3-[hydroxyl(2-phenyl-(1R)-1-([(benzyloxy)carbonyl]-amino)ethyl)phosphinyl]-(2R)-2-[(3-phenylisoxazol-5-yl)methyl]-1-oxopropyl)amino)-3-(4-hydroxy-phenyl) propanoic acid
-
-
(2S)-2-((3-[hydroxyl(2-phenyl-(1R)-1-([(benzyloxy)carbonyl]-amino)ethyl)phosphinyl]-(2S)-2-[(3-phenylisoxazol-5-yl)methyl]-1-oxopropyl)amino) 1H-indole-3-propanoic acid
-
-
(2S)-2-((3-[hydroxyl(2-phenyl-(1R)-1-([(benzyloxy)carbonyl]-amino)ethyl)phosphinyl]-(2S)-2-[(3-phenylisoxazol-5-yl)methyl]-1-oxopropyl)amino)-3-(4-hydroxy-phenyl) propanoic acid
-
-
(2S)-2-((3-[hydroxyl(2-phenyl-(1R)-1-([(benzyloxy)carbonyl]amino)ethyl)phosphinyl]-(2R)-2-[(3-phenylisoxazol-5-yl)methyl]-1-oxopropyl)amino)-3-phenyl propanoic acid
-
-
(2S)-2-((3-[hydroxyl(2-phenyl-(1R)-1-([(benzyloxy)carbonyl]amino)ethyl)phosphinyl]-(2S)-2-[(3-phenylisoxazol-5-yl)methyl]-1-oxopropyl)amino)-3-phenyl propanoic acid
-
-
(2S)-2-([3-(1,1'-biphenyl)-2-([hydroxyl(2-phenyl-(1R)-1-([(benzyloxy)carbonyl]amino)ethyl)phosphinyl]methyl)-1-oxopropyl]-amino) 1H-indole-3-propanoic acid
-
-
(2S)-2-([3-(3'-[1,1'-biphenyl]-4''-yl-4',5'-dihydro-5'-isoxazolyl)-2-([hydroxyl(2-phenyl-(1R)-1-([(benzyloxy)carbonyl]amino)ethyl)-phosphinyl]methyl)-1-oxopropyl]amino) 1H-indole-3-propanoic acid
-
-
(2S,4R)-2-[(2,5-difluorobenzylamino)methyl]-4-mercaptopyrrolidine-1-carboxylic acid isopropyl ester
-
IC50: 0.00109 mM
(2S,4R)-2-[2-[[4-mercapto-1-(naphthalene-2-sulfonyl)-pyrrolidine-2-carbonyl]methylamino]acetylamino]-benzoic acid methyl ester
-
IC50: 0.01089 mM
(2S,4R)-4-acetylsulfanyl-2-(2,4,5-trifluorobenzyloxymethyl)pyrrolidine-1-carboxylic acid 2,3-dihydrobenzo-[1,4]dioxin-5-yl ester
-
IC50: 0.0000765 mM
(2S,4R)-4-acetylsulfanyl-2-(2,4,5-trifluorobenzyloxymethyl)pyrrolidine-1-carboxylic acid 2-methoxycarbonylphenylester
-
IC50: 0.0000215 mM
(2S,4R)-4-mercapto-1-(naphthalene-2-sulfonyl)pyrrolidine-2-carboxylic acid N-methyl-N-(4-methylphenylsulfonyl)hydrazide
-
IC50: 0.00253 mM
(2S,4R)-4-mercapto-2-(2,4,5-trifluorobenzyloxymethyl)-pyrrolidine-1-carboxylic acid 2,3-dihydrobenzo[1,4]-dioxin-5-yl ester
-
IC50: 0.000137 mM
(2S,4R)-4-mercapto-2-(2,4,5-trifluorobenzyloxymethyl)-pyrrolidine-1-carboxylic acid 2-ethoxycarbonylphenylester
-
IC50: 0.000067 mM
(2S,4R)-5-[(2,5-difluorobenzylamino)methyl]-1-(5-propylpyrimidin-2-yl)pyrrolidine-3-thiol
-
IC50: 0.0000729 mM
(3R,5S)-1-(5-propylpyrimidin-2-yl)-5-(2,4,5-trifluorobenzyloxymethyl)pyrrolidine-3-thiol trifluoroacetate
-
IC50: 0.0000198 mM
(R,R)-5-[(2,4-difluorophenyl)-2-(3,3,3-trifluoro-2-methoxy-2-phenylpropionyl)amino]pent-4-ynoic acid methyl ester
-
-
(R,S)-5-[(2,4-difluorophenyl)-2-(3,3,3-trifluoro-2-methoxy-2-phenylpropionyl)amino]pent-4-ynoic acid methyl ester
-
-
(S)-2-amino-5-(2,4-difluorophenyl)pent-4-ynoic acid methyl ester
-
-
(S)-2-[(tert-butoxycarbonyl)amino]-5-(2,4-difluorophenyl)pent-4-ynoic acid
-
-
(S)-2-[(tert-butoxycarbonyl)amino]-5-(2,4-difluorophenyl)pent-4-ynoic acid methyl ester
-
-
(S)-2-[(tert-butoxycarbonyl)amino]pent-4-ynoic acid
-
-
(S)-3-[5-[1-amino-4-(2-methoxyphenyl)but-3-ynyl]tetrazol-1-yl]propionitrile
-
-
(S)-5-(2,4-difluorophenyl)-2-[[(dimethoxyphosphoryl)methyl]amino]pent-4-ynoic acid
-
-
(S)-5-(2,4-difluorophenyl)-2-[[(dimethoxyphosphoryl)methyl]amino]pent-4-ynoic acid methyl ester
-
-
(S)-[1-[(2-cyanoethyl)-1-H-tetrazol-5-yl]-4-(2-methoxyphenyl)but-3-ynyl]carbamic acid tert-butyl ester
-
-
(S)-[1-[(2-cyanoethyl)carbamoyl]-4-(2-methoxyphenyl)but-3-ynyl]carbamic acid tert-butyl ester
-
-
(S)-[1-[(2-cyanoethyl)carbamoyl]but-3-ynyl]carbamic acid tert-butyl ester
-
-
(S)-[[1-[[(2-biphenyl-4-ylethyl)-carbamoyl]-4-(2-fluorophenyl)but-3-ynyl]amino]methyl]phosphonic acid
-
-
(S)-[[[1-[1-(2-cyanoethyl)-1-H-tetrazol-5-yl]-4-(2-methoxyphenyl)but-3-ynyl]amino]methyl] phosphonic acid diphenyl ester
-
-
(S)-[[[[4-(2-methoxyphenyl)-1-H-tetrazol-5-yl]but-3-ynyl]amino]methyl] phosphonic acid
-
-
(S)-[[[[4-(2-methoxyphenyl)-1-H-tetrazol-5-yl]but-3-ynyl]amino]methyl] phosphonic acid diphenyl ester
-
-
(S,S)-2-[5-(2,4-difluorophenyl)-2-[[(dimethoxyphosphoryl)methyl]amino]pent-4-ynoyl]-4-methylpentanoic acid methyl ester
-
-
(S,S)-2-[[2-amino-5-(2-chlorophenyl)pent-4-ynoyl]amino]-4-methylpentanoic acid methyl ester
-
-
(S,S)-2-[[2-[(tert-butoxycarbonyl)amino]-5-(2-chlorophenyl)pent-4-ynoyl]-amino]-4-methylpentanoic acid methyl ester
-
-
(S,S)-2-[[2-[(tert-butoxycarbonyl)amino]pent-4-ynoyl]-amino]-4-methylpentanoic acid methyl ester
-
-
(S,S)-2-[[5-(2,4-difluorophenyl)-2-[(phosphonomethyl)amino]pent-4-ynoyl]amino]-4-methylpentanoic acid
-
-
(S,S)-2-[[5-(2-chlorophenyl)-2-[(phosphonomethyl)amino]pent-4-ynoyl]amino]-4-methylpentanoic acid
-
-
(S,S)-2-[[5-(2-chlorophenyl)-2-[[(dimethoxyphosphoryl)-methyl]amino]pent-4-ynoyl]amino]-4-methylpentanoic acid methyl ester
-
-
(S,S)-2-[[5-(2-fluorophenyl)-2-[(phosphonomethyl)-amino]pent-4-ynoyl]amino]-4-methyl pentanoic acid
-
-
(S,S)-2-[[5-(3-fluorophenyl)-2-[(phosphonomethyl)-amino]pent-4-ynoyl]amino]-4-methyl pentanoic acid
-
-
(S,S)-5-phenyl-2-[(3,3,3-trifluoro-2-methoxy-2-phenylpropionyl)amino]pent-4-ynoic acid (2-cyanoethyl)amide
-
-
1-(2,6-difluorobenzyl)-5-[(3,3-dimethylbutanoyl)amino]-N-phenyl-1H-indole-2-carboxamide
-
IC50: 0.00065 mM
1-(2-fluorobenzyl)-5-[[(1-methylcyclopentyl)acetyl]amino]-N-phenyl-1H-indole-2-carboxamide
-
IC50: 0.00012 mM
1-(cyclohexylmethyl)-5-[(3,3-dimethylbutanoyl)amino]-N-phenyl-1H-indole-2-carboxamide
-
IC50: 0.00086 mM
2-[(tert-butoxycarbonyl)amino]-5-(2,4-difluorophenyl)pent-4-ynoic acid methyl ester
-
-
4-chloro-N-(((4-cyano-3-methyl-1-phenyl-1H-pyrazol-5-yl)amino)carbonyl)benzenesulfonamide
-
-
4-chloro-N-[(4-cyano-3-methyl-1-phenyl-1H-pyrazol-5-yl)amino]carbonyl benzenesulfonamide
-
-
4-[([5-[(2,2-dimethylpropyl)carbamoyl]-1-(2-fluorobenzyl)-1H-indol-2-yl]carbonyl)amino]benzoic acid
-
IC50: 0.00039 mM
5-[(3,3-dimethylbutanethioyl)amino]-1-(2-fluorobenzyl)-N-phenyl-1H-indole-2-carboxamide
-
IC50: 0.00066 mM
5-[(3,3-dimethylbutanoyl)amino]-1-(2-fluorobenzyl)-N-phenyl-1H-indole-2-carboxamide
-
IC50: 0.00022 mM
5-[(3,3-dimethylbutanoyl)amino]-1-(2-methylbenzyl)-N-phenyl-1H-indole-2-carboxamide
-
IC50: 0.003 mM
5-[(3,3-dimethylbutanoyl)amino]-1-[(2-methyl-1,3-thiazol-4-yl)methyl]-N-phenyl-1H-indole-2-carboxamide
-
IC50: 0.0022 mM
5-[(3,3-dimethylbutanoyl)amino]-N,1-diphenyl-1H-indole-2-carboxamide
-
IC50: 0.0059 mM
5-[(3,3-dimethylbutanoyl)amino]-N-phenyl-1-(2-phenylethyl)-1H-indole-2-carboxamide
-
IC50: 0.0051 mM
5-[(3,3-dimethylbutanoyl)amino]-N-phenyl-1-[2-(trifluoromethyl)benzyl]-1H-indole-2-carboxamide
-
IC50: 0.00017 mM
5-[(4,4-dimethylpentanoyl)amino]-1-(2-fluorobenzyl)-N-phenyl-1H-indole-2-carboxamide
-
IC50: 0.00074 mM
5-[(bicyclo[2.2.1]hept-2-ylacetyl)amino]-1-(2-fluorobenzyl)-N-phenyl-1H-indole-2-carboxamide
-
IC50: 0.0003 mM
5-[(cyclopentylacetyl)amino]-1-(2-fluorobenzyl)-N-phenyl-1H-indole-2-carboxamide
-
IC50: 0.0064 mM
5-[([5-[(2,2-dimethylpropyl)carbamoyl]-1-(2-fluorobenzyl)-1H-indol-2-yl]carbonyl)amino]pyridine-3-carboxylic acid
-
IC50: 0.074 mM
5-[[(2,2-dimethylpropyl)sulfonyl]amino]-1-(2-fluorobenzyl)-N-phenyl-1H-indole-2-carboxamide
-
IC50: 0.0067 mM
benzoylsulfanyl-2-(2,4,5-trifluorobenzyloxymethyl)-pyrrolidine-1-carboxylic acid 2,3-dihydrobenzo[1,4]-dioxin-5-yl ester
-
IC50: 0.0004805 mM
CGS 26303
-
synthetic inhibitor, ECE-1/NEP inhibitor
CGS 34043
-
synthetic inhibitor, ECE-1/NEP inhibitor
CGS 34226
-
synthetic inhibitor, ECE-1/NEP inhibitor
CGS 35601
-
synthetic inhibitor, ECE/NEP/ACE inhibitor
cyclohexyl-2-[[5-(2,4-difluorophenyl)-2-[(phosphonomethyl)-amino]pent-4-ynoyl]amino]propionic acid
-
-
ECEi
-
addition of an ECE-1 specific inhibitor (ECEi) to PC-3 cells reduces phosphorylation of focal adhesion kinase
-
L-tryptophan, N-[[1-[[(2S)-2-(acetylthio)-4-methyl-1 oxopentyl]amino]cyclopentyl]-carbonyl]-methyl ester
-
CGS 37808, at an oral dose of 10 mgEq per kg, CGS 37808 produced 71% and 67% inhibition of the big ET-1 pressor response at 30 and 120 min, respectively
L-tryptophan, N-[[1-[[(2S)-2-mercapto-4-methyl-1-oxopentyl]amino]-cyclopentyl]carbonyl]
-
CGS 35601, IC50: 55 nM
N-(2,2-dimethylpropyl)-1-(2-fluorobenzyl)-2-(3-phenyl-1,2,4-oxadiazol-5-yl)-1H-indole-5-carboxamide
-
IC50: 0.01 mM
N-(2,2-dimethylpropyl)-1-(2-fluorobenzyl)-2-[(phenylamino)methyl]-1H-indole-5-carboxamide
-
IC50: 0.01 mM
N-(2-benzyl-3-[[(1R)-1-[[(benzyloxy)carbonyl]amino]-2-phenylethyl](hydroxy)phosphoryl]propanoyl)-L-tryptophan
-
-
N-(3-{[(1R)-1-{[(benzyloxy)carbonyl]amino}-2-phenylethyl](hydroxy)phosphoryl}-2-{[3-(biphenyl-4-yl)-4,5-dihydro-1,2-oxazol-5-yl]methyl}propanoyl)-L-tryptophan
-
-
N-[3-{[(1R)-1-{[(benzyloxy)carbonyl]amino}-2-phenylethyl](hydroxy)phosphoryl}-2-(biphenyl-4-ylmethyl)propanoyl]-L-tryptophan
-
-
N-{(2S)-3-{[(1R)-1-{[(benzyloxy)carbonyl]amino}-2-phenylethyl](hydroxy)phosphoryl}-2-[(3-phenyl-1,2-oxazol-5-yl)methyl]propanoyl}-L-tryptophan
-
-
N2-(4-carbamoylphenyl)-N5-(2,2-dimethylpropyl)-1-(2-fluorobenzyl)-1H-indole-2,5-dicarboxamide
-
IC50: 0.00022 mM
N2-(5-aminopyridin-2-yl)-N5-(2,2-dimethylpropyl)-1-(2-fluorobenzyl)-1H-indole-2,5-dicarboxamide
-
IC50: 0.0012 mM
N2-(6-aminopyridin-3-yl)-N5-(2,2-dimethylpropyl)-1-(2-fluorobenzyl)-1H-indole-2,5-dicarboxamide
-
IC50: 0.00017 mM
N2-(6-chloropyridin-3-yl)-N5-(2,2-dimethylpropyl)-1-(2-fluorobenzyl)-1H-indole-2,5-dicarboxamide
-
IC50: 0.00044 mM
N2-[4-(dimethylcarbamoyl)phenyl]-N5-(2,2-dimethylpropyl)-1-(2-fluorobenzyl)-1H-indole-2,5-dicarboxamide
-
IC50: 0.00021 mM
N2-[4-[(butylsulfonyl)amino]phenyl]-N5-(2,2-dimethylpropyl)-1-(2-fluorobenzyl)-1H-indole-2,5-dicarboxamide
-
IC50: 0.0002 mM
N2-[6-(acetylamino)pyridin-3-yl]-N5-(2,2-dimethylpropyl)-1-(2-fluorobenzyl)-1H-indole-2,5-dicarboxamide
-
IC50: 0.00013 mM
N5-(2,2-dimethylpropyl)-1-(2-fluorobenzyl)-N2-(3-[[4-(methylsulfamoyl)phenyl]carbamoyl]phenyl)-1H-indole-2,5-dicarboxamide
-
IC50: 0.00015 mM
N5-(2,2-dimethylpropyl)-1-(2-fluorobenzyl)-N2-1,3,4-thiadiazol-2-yl-1H-indole-2,5-dicarboxamide
-
IC50: 0.0023 mM
N5-(2,2-dimethylpropyl)-1-(2-fluorobenzyl)-N2-1H-pyrazol-3-yl-1H-indole-2,5-dicarboxamide
-
IC50: 0.01 mM
N5-(2,2-dimethylpropyl)-1-(2-fluorobenzyl)-N2-phenyl-1H-indole-2,5-dicarboxamide
N5-(2,2-dimethylpropyl)-1-(2-fluorobenzyl)-N2-pyridin-3-yl-1H-indole-2,5-dicarboxamide
-
IC50: 0.00085 mM
N5-(2,2-dimethylpropyl)-1-(2-fluorobenzyl)-N2-[3-[(4-sulfamoylphenyl)carbamoyl]phenyl]-1H-indole-2,5-dicarboxamide
-
IC50: 0.000039 mM
N5-(2,2-dimethylpropyl)-1-(2-fluorobenzyl)-N2-[5-[(4-methylpiperazin-1-yl)carbonyl]pyridin-3-yl]-1H-indole-2,5-dicarboxamide
-
IC50: 0.09 mM
PD069185
-
a more selective ECE inhibitor
RO 67-7447
-
i.e. (2S,4R)-4-mercapto-2-(2,4,5-trifluoro-benzyloxymethyl)-pyrrolidine-1-carboxylic acid 2-methoxycarbonyl-phenyl ester, a selective ECE-1 inhibitor
SLV-306
-
KC-12792, synthetic inhibitor, ECE-1/NEP inhibitor, clinical trial for treatment of arterial hypertension and heart failure in human
specific ECE-1 inhibitor
-
in the presence of 0.001 M ECE-1 inhibitor, cell number was effectively reduced to ~70% of control
-
[Lys-Gly-His-Lys-Co(NH3)2]2+
-
metallopeptide
[Lys-Gly-His-Lys-Cu]+
-
metallopeptide, IC50: 0.0049 mM under hydrolytic condtions
CGS-35066
-
CGS-35066
complete inhibition at 5 nM
SM-19712
-
SM-19712
0.01 mM used in assay conditions
1,10-phenanthroline
-
-
1,10-phenanthroline
-
1 mM, inhibition of ECE-1 activity
CGS 35066
-
-
CGS 35066
-
synthetic inhibitor, selective ECE-1 inhibitor
N5-(2,2-dimethylpropyl)-1-(2-fluorobenzyl)-N2-phenyl-1H-indole-2,5-dicarboxamide
-
IC50: 0.007 mM
N5-(2,2-dimethylpropyl)-1-(2-fluorobenzyl)-N2-phenyl-1H-indole-2,5-dicarboxamide
-
IC50: 0.01 mM
phosphoramidon
-
-
phosphoramidon
-
0.1 M, 35% inhibition of ECE-1 activity
phosphoramidon
-
a metalloproteinase inhibitor
SM-19712
-
a specific ECE-1 inhibitor
SM-19712
-
a specific ECE-1 inhibitor. SM-191712 causes sustained ERK2 activation in cytosolic and nuclear fractions after substance P removal
thiorphan
-
-
thiorphan
-
50% inhibition of native ECE-1, 70% inhibition of solECE-1
thiorphan
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1 mM, inhibition of ECE-1 activity
additional information
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little or no inhibition with captopril
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additional information
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not inhibited by thiorphan and captopril
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additional information
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acidification to pH 6.4 inhibits plasma membrane ECE activity
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additional information
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carbachol and phorbol 12-myristate 13-acetate reduce enzyme expression in neuroblastoma NB7 cells, only isozyme ECE-1c remains detectable, overview
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additional information
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prevention of acidification of endosomes using bafilomycin A1 inhibits the degradation of internalized somatostatin-14
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additional information
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RNAi-induced knockdown of ECE-1 reduces ECE-1 mRNA and protein levels leading to 80% to 90% inhibition of endothelin-1 secretion by the ovarian carcinoma cells, analysation of cell's behaviour and effect on the cancer
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additional information
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ECE-1 inhibition causes endosomal retention of the substance P neurokinin 1 receptor, beta-arrestins, and Src, resulting in markedly sustained ERK2 activation in the cytosol and nucleus. ECE-1 inhibition also enhances substance P-induced expression and phosphorylation of the nuclear death receptor Nur77, resulting in cell death
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additional information
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no inhibition by thiorphan and captopril
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additional information
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phosphinic tripeptides as dual angiotensin-converting enzyme C-domain and endothelin-converting enzyme-1, while sparing neprilysin, inhibitors, overview
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Acute Coronary Syndrome
Effects of ECE-1b rs213045 and rs2038089 polymorphisms on the development of contrast-induced acute kidney injury in patients with acute coronary syndrome.
Acute Kidney Injury
Effects of ECE-1b rs213045 and rs2038089 polymorphisms on the development of contrast-induced acute kidney injury in patients with acute coronary syndrome.
Acute Kidney Injury
Intranephron distribution and regulation of endothelin-converting enzyme-1 in cyclosporin A-induced acute renal failure in rats.
Acute Kidney Injury
Protective effect of SM-19712, a novel and potent endothelin converting enzyme inhibitor, on ischemic acute renal failure in rats.
Acute Lung Injury
Phosphoramidon, an endothelin-converting enzyme inhibitor, attenuates lipopolysaccharide-induced acute lung injury.
Adenocarcinoma
Endothelin converting enzyme-1 expression in endometrial adenocarcinomas.
Adenocarcinoma
Modulation of human colon tumor-stromal interactions by the endothelin system.
Adenoma
Modulation of human colon tumor-stromal interactions by the endothelin system.
Adenoma, Islet Cell
Immunohistochemical localization of endothelin-converting enzyme-1 in neuroendocrine tumors and normal human tissue.
Albuminuria
Effect on blood pressure of combined inhibition of endothelin-converting enzyme and neutral endopeptidase with daglutril in patients with type 2 diabetes who have albuminuria: a randomised, crossover, double-blind, placebo-controlled trial.
Alzheimer Disease
Alzheimer's disease beta-amyloid peptide is increased in mice deficient in endothelin-converting enzyme.
Alzheimer Disease
C-338A polymorphism of the endothelin-converting enzyme (ECE-1) gene and the susceptibility to sporadic late-onset Alzheimer's disease and coronary artery disease.
Alzheimer Disease
Dynamic alteration of neprilysin and endothelin-converting enzyme in age-dependent APPswe/PS1dE9 mouse model of Alzheimer's disease.
Alzheimer Disease
Endothelin-converting enzyme-1 activity, endothelin-1 production, and free radical-dependent vasoconstriction in Alzheimer's disease.
Alzheimer Disease
Endothelin-converting enzyme-1 in Alzheimer's disease and vascular dementia.
Alzheimer Disease
Endothelin-converting enzyme-1 is expressed in human cerebral cortex and protects against Alzheimer's disease.
Alzheimer Disease
Endothelin-converting enzyme-1 promoter polymorphisms and susceptibility to sporadic late-onset Alzheimer's disease in a Chinese population.
Alzheimer Disease
Major amyloid-?-degrading enzymes, endothelin-converting enzyme-2 and neprilysin, are expressed by distinct populations of GABAergic interneurons in hippocampus and neocortex.
Alzheimer Disease
Regulation of endothelin-converting enzyme-1 expression in human neuroblastoma cells.
Alzheimer Disease
Structural analysis of membrane-bound hECE-1 dimer using molecular modeling techniques: insights into conformational changes and A?1-42 peptide binding.
Aneurysm
Plasma endothelin and big endothelin concentrations and serum endothelin-converting enzyme activity following aneurysmal subarachnoid hemorrhage.
Arteriosclerosis
Up-regulation of endothelin-converting enzyme during the development of transplant renal arteriosclerosis in human renal allografts.
Asthma
Interleukin-1beta attenuates endothelin B receptor-mediated airway contractions in a murine in vitro model of asthma: roles of endothelin converting enzyme and mitogen-activated protein kinase pathways.
Asthma
[Effect of inhaled-corticosteroids on the mRNA expressions of endothelin-1 and endothelin converting enzyme in bronchial asthma]
Asthma
[Effects of butylphthalide on bronchial asthma in guinea pigs and involvement of endothelin].
Asthma
[The effect of GM-CSF on endothelin-1 and endothelin converting enzyme gene expression in human airway smooth muscle cells with or without theophylline incubation]
Astrocytoma
Localization of the endothelin system in human diffuse astrocytomas.
Atherosclerosis
C-338A polymorphism of the endothelin-converting enzyme-1 gene and the susceptibility to carotid atherosclerosis.
Atherosclerosis
Characterization of PgPepO, a bacterial homologue of endothelin-converting enzyme-1.
Atherosclerosis
Coexpression of endothelin-converting enzyme-1 and endothelin-1 in different stages of human atherosclerosis.
Atherosclerosis
Endothelin-1 and endothelin converting enzyme-1 in human atherosclerosis - novel targets for pharmacotherapy in atherosclerosis.
Atherosclerosis
Endothelin-converting enzyme expression in the rat vascular injury model and human coronary atherosclerosis.
Atherosclerosis
Endothelin-converting enzyme-1 increases in atherosclerotic mice: potential role of oxidized low density lipoproteins.
Atherosclerosis
Enhanced endothelin-converting enzyme immunoreactivity in early atherosclerosis.
Atherosclerosis
Expression and localization of human endothelin-converting enzyme-1 isoforms in symptomatic atherosclerotic disease and saphenous vein.
Atherosclerosis
Mammalian membrane metallopeptidases: NEP, ECE, KELL, and PEX.
Atherosclerosis
Modulation of functionally active endothelin-converting enzyme by chronic neutral endopeptidase inhibition in experimental atherosclerosis.
Atherosclerosis
Stimulated release of endothelin-converting enzyme is simultaneous with tissue-type plasminogen activator and decrease in coronary heart disease.
Atherosclerosis
Vascular endothelial growth factor increases endothelin-converting enzyme expression in vascular endothelial cells.
Bacterial Infections
Up-regulation in endothelin-1 by Helicobacter pylori lipopolysaccharide interferes with gastric mucin synthesis via epidermal growth factor receptor transactivation.
Brain Ischemia
Prophylactic use of melatonin protects against focal cerebral ischemia in mice: role of endothelin converting enzyme-1.
Breast Neoplasms
Human breast cancer cells contain a phosphoramidon-sensitive metalloproteinase which can process exogenous big endothelin-1 to endothelin-1: a proposed mitogen for human breast fibroblasts.
Breast Neoplasms
On the role of endothelin-converting enzyme-1 (ECE-1) and neprilysin in human breast cancer.
Carcinogenesis
Endothelin-converting enzyme-1 in cancer aggressiveness.
Carcinogenesis
The endothelin axis: a novel target for pharmacotherapy of female malignancies.
Carcinoid Tumor
Immunohistochemical localization of endothelin-converting enzyme-1 in neuroendocrine tumors and normal human tissue.
Carcinoma
ECE-1 overexpression in head and neck cancer is associated with poor tumor differentiation and patient outcome.
Carcinoma
Endothelin converting enzyme-1 expression in endometrial adenocarcinomas.
Carcinoma
Expression of endothelin-1 is related to poor prognosis in non-small cell lung carcinoma.
Carcinoma
High endothelin-converting enzyme-1 expression independently predicts poor survival of patients with esophageal squamous cell carcinoma.
Carcinoma
Modulation of human colon tumor-stromal interactions by the endothelin system.
Carcinoma
Small interfering RNA molecules targeting endothelin-converting enzyme-1 inhibit endothelin-1 synthesis and the invasive phenotype of ovarian carcinoma cells.
Carcinoma
[Association of CD133 and endothelin-converting enzyme expressions with prognosis of non-small cell lung carcinoma]
Carcinoma, Medullary
Immunohistochemical localization of endothelin-converting enzyme-1 in neuroendocrine tumors and normal human tissue.
Carcinoma, Non-Small-Cell Lung
Expression of endothelin-1 is related to poor prognosis in non-small cell lung carcinoma.
Carcinoma, Non-Small-Cell Lung
[Association of CD133 and endothelin-converting enzyme expressions with prognosis of non-small cell lung carcinoma]
Carcinoma, Renal Cell
Cloning and sequencing of a human endothelin converting enzyme in renal adenocarcinoma (ACHN) cells producing endothelin-2.
Carcinoma, Squamous Cell
ECE-1 overexpression in head and neck cancer is associated with poor tumor differentiation and patient outcome.
Carcinoma, Squamous Cell
Endothelin system in oral squamous carcinoma cells: Specific siRNA targeting of ECE-1 blocks cell proliferation.
Cardiomyopathies
Attenuation of Doxorubicin-induced cardiomyopathy by endothelin-converting enzyme-1 ablation through prevention of mitochondrial biogenesis impairment.
Cardiomyopathies
Expression of endothelin-1 and endothelin-converting enzyme-1 mRNAs and proteins in failing human hearts.
Cardiovascular Diseases
Alternative pathway to endothelin-converting enzyme for the synthesis of endothelin in human blood vessels.
Cardiovascular Diseases
Cellular expression of isoforms of endothelin-converting enzyme-1 (ECE-1c, ECE-1b and ECE-1a) and endothelin-converting enzyme-2.
Cardiovascular Diseases
Clinical significance of endothelin in cardiovascular disease.
Cardiovascular Diseases
Endothelin converting-enzyme-1 mRNA expression in human cardiovascular disease.
Cardiovascular Diseases
Endothelin-converting enzyme inhibitors: their application in cardiovascular diseases.
Cardiovascular Diseases
Endothelin-converting enzyme-1 mRNA expression in human cardiovascular disease.
Cardiovascular Diseases
Endothelin: role in hypertension.
Cardiovascular Diseases
Metallopeptide-promoted inactivation of angiotensin-converting enzyme and endothelin-converting enzyme 1: toward dual-action therapeutics.
Cardiovascular Diseases
Modulation of functionally active endothelin-converting enzyme by chronic neutral endopeptidase inhibition in experimental atherosclerosis.
Cardiovascular Diseases
Physiological relevance of hydrolysis of atrial natriuretic Peptide by endothelin-converting enzyme-1.
Cardiovascular Diseases
The endothelin-converting enzyme from human umbilical vein is a membrane-bound metalloprotease similar to that from bovine aortic endothelial cells.
Cardiovascular Diseases
The role of endothelins and their receptors in heart failure.
Cardiovascular Diseases
The therapeutic potential of endothelin-1 receptor antagonists and endothelin-converting enzyme inhibitors on the cardiovascular system.
Cardiovascular Diseases
Utility of endothelin-converting enzyme inhibitors for the treatment of cardiovascular diseases.
Carotid Artery Diseases
Association of Endothelin-converting Enzyme-1b C-338A Polymorphism with Increased Risk of Ischemic Stroke in Chinese Han Population.
Carotid Artery Diseases
C-338A polymorphism of the endothelin-converting enzyme-1 gene and the susceptibility to carotid atherosclerosis.
Cerebrovascular Disorders
Therapeutic effects of endothelin receptor antagonists in stroke.
Chalazion
Endothelin-1 and endothelin-converting enzyme-1 in human granulomatous pathology of eyelid: an immunohistochemical and in situ hybridization study in chalazia.
Colitis
Effects of the endothelin-converting enzyme inhibitor SM-19712 in a mouse model of dextran sodium sulfate-induced colitis.
Colonic Neoplasms
Colon cancer cell invasion is promoted by protein kinase CK2 through increase of endothelin-converting enzyme-1c protein stability.
Colorectal Neoplasms
Melatonin reduces endothelin-1 expression and secretion in colon cancer cells through the inactivation of FoxO-1 and NF-??
Congenital Abnormalities
Ectodermal-derived Endothelin1 is required for patterning the distal and intermediate domains of the mouse mandibular arch.
Coronary Artery Disease
Alterations of endothelin-converting enzyme expression in early and advanced stages of human coronary atherosclerosis.
Coronary Artery Disease
C-338A polymorphism of the endothelin-converting enzyme (ECE-1) gene and the susceptibility to sporadic late-onset Alzheimer's disease and coronary artery disease.
Coronary Artery Disease
Endothelin-converting enzyme expression in the rat vascular injury model and human coronary atherosclerosis.
Coronary Artery Disease
Endothelin-converting enzyme-1b C-338A polymorphism is associated with the increased risk of coronary artery disease in Chinese population.
Coronary Artery Disease
Risk of coronary artery disease as influenced by variants of the human endothelin and endothelin-converting enzyme genes.
Coronary Artery Disease
Tissue endothelin-converting enzyme activity correlates with cardiovascular risk factors in coronary artery disease.
Coronary Disease
Selective Indole-Based ECE Inhibitors: Synthesis and Pharmacological Evaluation.
Coronary Disease
Stimulated release of endothelin-converting enzyme is simultaneous with tissue-type plasminogen activator and decrease in coronary heart disease.
Crohn Disease
Enhanced expressions of endothelin-converting enzyme and endothelin receptors in human colonic tissues of Crohn's disease.
Dementia
Endothelin-converting enzymes degrade ?-synuclein and are reduced in dementia with Lewy bodies.
Dementia
Transducible P11-CNTF rescues the learning and memory impairments induced by amyloid-beta peptide in mice.
Dementia, Vascular
Endothelin-converting enzyme-1 in Alzheimer's disease and vascular dementia.
Diabetes Mellitus, Type 1
Downregulation of renal endothelin-converting enzyme 2 expression in early autoimmune diabetes.
Diabetes Mellitus, Type 2
Effect on blood pressure of combined inhibition of endothelin-converting enzyme and neutral endopeptidase with daglutril in patients with type 2 diabetes who have albuminuria: a randomised, crossover, double-blind, placebo-controlled trial.
Diabetic Cardiomyopathies
A novel endothelin receptor antagonist CPU0213 improves diabetic cardiac insufficiency attributed to up-regulation of the expression of FKBP12.6, SERCA2a, and PLB in rats.
Diabetic Nephropathies
Role of protein kinase C in the expression of endothelin converting enzyme-1.
DiGeorge Syndrome
Dual genetic pathways of endothelin-mediated intercellular signaling revealed by targeted disruption of endothelin converting enzyme-1 gene.
Endometrial Neoplasms
Endothelin converting enzyme-1 expression in endometrial adenocarcinomas.
endothelin-converting enzyme 1 deficiency
Impaired ventilatory responses to hypoxia in mice deficient in endothelin-converting-enzyme-1.
Endotoxemia
Regional distribution of endothelin-1 and endothelin converting enzyme-1 in porcine endotoxemia.
Esophageal Squamous Cell Carcinoma
High endothelin-converting enzyme-1 expression independently predicts poor survival of patients with esophageal squamous cell carcinoma.
Gastritis
Omeprazole fails to suppress up-regulation of gastric mucosal endothelin-converting enzyme-1 by Helicobacter pylori lipopolysaccharide.
Gastritis
Up-regulation of endothelin-converting enzyme-1 in gastric mucosal inflammatory responses to Helicobacter pylori lipopolysaccharide.
Glaucoma
An immunohistochemical study of endothelin-1 converting enzyme in the human eye.
Glioblastoma
Endothelin-converting enzyme-1 inhibition and growth of human glioblastoma cells.
Glioblastoma
The endothelin system in human glioblastoma.
Glioma
Expression of endothelin-converting enzyme in both neuroblastoma and glial cell lines and its localization in rat hippocampus.
Glioma
Hypoxic regulation of EDN1, EDNRA, EDNRB, and ECE1 gene expressions in ERN1 knockdown U87 glioma cells.
Head and Neck Neoplasms
ECE-1 overexpression in head and neck cancer is associated with poor tumor differentiation and patient outcome.
Heart Failure
Angiotensin-converting enzyme inhibitor therapy prevents upregulation of endothelin-converting enzyme-1 in failing human myocardium.
Heart Failure
Atrial natriuretic peptide and regulation of vascular function in hypertension and heart failure: implications for novel therapeutic strategies.
Heart Failure
Chronic effects of an endothelin-converting enzyme inhibitor on cardiorenal and hormonal function in heart failure.
Heart Failure
Deloading of the left ventricle by ventricular assist device normalizes increased expression of endothelin ET(A) receptors but not endothelin-converting enzyme-1 in patients with end-stage heart failure.
Heart Failure
Early activation of cardiac and renal endothelin systems in experimental heart failure.
Heart Failure
Effect of single doses of SLV306, an inhibitor of both neutral endopeptidase and endothelin-converting enzyme, on pulmonary pressures in congestive heart failure.
Heart Failure
Effects of a specific endothelin-converting enzyme inhibitor on cardiac, renal, and neurohumoral functions in congestive heart failure: comparison of effects with those of endothelin A receptor antagonism.
Heart Failure
Endothelin-1 promotes vascular structural remodeling during the progression of heart failure prevention of vascular remodeling using a specific endothelin-converting enzyme inhibitor.
Heart Failure
Endothelin-converting enzyme inhibition in the rat model of acute heart failure: heart function and neurohormonal activation.
Heart Failure
Endothelin-converting enzyme-1 mRNA expression in human cardiovascular disease.
Heart Failure
Expression and activity of pulmonary endothelin converting enzyme in heart failure: relation to endothelin biosynthesis and receptor distribution.
Heart Failure
Expression of endothelin-1, endothelin-converting enzyme, and endothelin receptors in chronic heart failure.
Heart Failure
Increased expression of endothelin-converting enzyme-1 in failing human myocardium.
Heart Failure
Renal endothelin-converting enzyme in rats with congestive heart failure.
Heart Failure
Sustained improvement of cardiac function and prevention of cardiac remodeling after long-term dual ECE-NEP inhibition in rats with congestive heart failure.
Heart Failure
Vasodilator effects of endothelin-converting enzyme inhibition and endothelin ETA receptor blockade in chronic heart failure patients treated with ACE inhibitors.
Heart Failure
[Endothelins and chronic cardiac insufficiency]
Herpes Zoster
Cellular distribution of endothelin-converting enzyme-1 in human tissues.
Hirschsprung Disease
A loss-of-function mutation in the endothelin-converting enzyme 1 (ECE-1) associated with Hirschsprung disease, cardiac defects, and autonomic dysfunction.
Hirschsprung Disease
Dual genetic pathways of endothelin-mediated intercellular signaling revealed by targeted disruption of endothelin converting enzyme-1 gene.
Hyperglycemia
Downregulation of renal endothelin-converting enzyme 2 expression in early autoimmune diabetes.
Hyperglycemia
Effect of Anthocyanin-Rich Extract of Sour Cherry for Hyperglycemia-Induced Inflammatory Response and Impaired Endothelium-Dependent Vasodilation.
Hyperglycemia
Role of protein kinase C in the expression of endothelin converting enzyme-1.
Hyperinsulinism
Hyperinsulinemia increases placenta endothelin-converting enzyme-1 expression in trophoblasts.
Hyperphosphatemia
Hyperphosphatemia induces senescence in human endothelial cells by increasing endothelin-1 production.
Hyperpigmentation
Biochemical characterization of endothelin-converting enzyme-1alpha in cultured skin-derived cells and its postulated role in the stimulation of melanogenesis in human epidermis.
Hypertension
A new ATP-sensitive potassium channel opener protects the kidney from hypertensive damage in spontaneously hypertensive rats.
Hypertension
Angiotensin-converting enzyme as a potential target for treatment of Alzheimer's disease: inhibition or activation?
Hypertension
Association of genetic polymorphisms of endothelin-converting enzyme-1 gene with hypertension in a Japanese population and rare missense mutation in preproendothelin-1 in Japanese hypertensives.
Hypertension
Atrial natriuretic peptide and regulation of vascular function in hypertension and heart failure: implications for novel therapeutic strategies.
Hypertension
Chronic vasopeptidase inhibition restores endothelin-converting enzyme activity and normalizes endothelin levels in salt-induced hypertension.
Hypertension
Endothelin as a regulator of cardiovascular function in health and disease.
Hypertension
Endothelin converting enzyme-1 gene expression in the kidney of spontaneously hypertensive rats.
Hypertension
Endothelin-converting enzyme-1 increases in atherosclerotic mice: potential role of oxidized low density lipoproteins.
Hypertension
In vivo role of endothelin-converting enzyme-1 as examined by adenovirus-mediated overexpression in rats.
Hypertension
Mechanisms of FK 506-induced hypertension in the rat.
Hypertension
Mice deficient in telomerase activity develop hypertension because of an excess of endothelin production.
Hypertension
Regulation of vascular contractility and blood pressure by the E2F2 transcription factor.
Hypertension
[Chronic theatment with an endothelin-converting enzyme inhibitor reduces the development of hypoxia-induced pulmonary hypertension in rat]
Hypertension
[Endothelins--physiology, pathophysiology and importance in arterial hypertension]
Hypertension, Pregnancy-Induced
[Genetic variability of endothelin-1 system in gestational hypertension and preeclampsia].
Hypertension, Pulmonary
Blockade of endothelin-converting enzyme reduces pulmonary hypertension after cardiopulmonary bypass and circulatory arrest.
Hypertension, Pulmonary
Effect of small hairpin RNA targeting endothelin-converting enzyme-1 in monocrotaline-induced pulmonary hypertensive rats.
Hypertension, Pulmonary
Endothelin converting enzyme inhibitor protects development of right ventricular overload and medial thickening of pulmonary arteries in rats with monocrotaline-induced pulmonary hypertension.
Hypertension, Pulmonary
Increased lung preproET-1 and decreased ETB-receptor gene expression in fetal pulmonary hypertension.
Hypertension, Pulmonary
Nitric oxide and endothelin-1 in pulmonary hypertension.
Hypertension, Pulmonary
Role of endothelial and smooth muscle cells in the physiopathology and treatment management of pulmonary hypertension.
Hypertension, Pulmonary
The role of endothelin converting enzyme inhibition during group B streptococcus-induced pulmonary hypertension in newborn piglets.
Hypertension, Pulmonary
[Chronic theatment with an endothelin-converting enzyme inhibitor reduces the development of hypoxia-induced pulmonary hypertension in rat]
Idiopathic Pulmonary Fibrosis
Elevated expression of endothelin-1 and endothelin-converting enzyme-1 in idiopathic pulmonary fibrosis: possible involvement of proinflammatory cytokines.
Infarction, Middle Cerebral Artery
Functional neuroprotective effect of CGS 26303, a dual ECE inhibitor, on ischemic-reperfusion spinal cord injury in rats.
Infarction, Middle Cerebral Artery
Neuroprotective Effect of CGS 26303, an Endothelin-converting Enzyme Inhibitor, on Transient Middle Cerebral Artery Occlusion in Rats.
Infections
Endothelin in a murine model of cerebral malaria.
Infections
Up-regulation of endothelin-converting enzyme-1 in gastric mucosal inflammatory responses to Helicobacter pylori lipopolysaccharide.
Ischemic Stroke
Association of Endothelin-converting Enzyme-1b C-338A Polymorphism with Increased Risk of Ischemic Stroke in Chinese Han Population.
Kidney Failure, Chronic
Endothelin-converting enzyme-1 inhibition and renoprotection in end-stage renal disease.
Kidney Failure, Chronic
The influence of the endothelin-converting enzyme-1 gene polymorphism on the progression of autosomal dominant polycystic kidney disease.
Lentigo
The role of the epidermal endothelin cascade in the hyperpigmentation mechanism of lentigo senilis.
Lewy Body Disease
Endothelin-converting enzymes degrade ?-synuclein and are reduced in dementia with Lewy bodies.
Liver Cirrhosis
Activation of the hepatic endothelin-system in rats with biliary liver fibrosis.
Liver Cirrhosis
Increased immunoreactivities against endothelin-converting enzyme-1 and monocyte chemotactic protein-1 in hepatic stellate cells of rat fibrous liver induced by thioacetamide.
Low Tension Glaucoma
An immunohistochemical study of endothelin-1 converting enzyme in the human eye.
Lung Neoplasms
Studies on the expression of endothelin, its receptor subtypes, and converting enzymes in lung cancer and in human bronchial epithelium.
Lymphatic Metastasis
High endothelin-converting enzyme-1 expression independently predicts poor survival of patients with esophageal squamous cell carcinoma.
Melanoma
Chemokine- and cytokine-induced expression of endothelin 1 and endothelin-converting enzyme 1 in endothelial cells.
Muscle Spasticity
Vasospasm following subarachnoid hemorrhage: evidence against functional upregulation of protein kinase C constrictor pathway.
Muscle Spasticity
Vasospasm following subarachnoid hemorrhage: evidence against functional upregulation of Rho kinase constrictor pathway.
Myocardial Infarction
Effect of a highly selective endothelin-converting enzyme inhibitor on cardiac remodeling in rats after myocardial infarction.
Myocardial Infarction
Endothelin converting-enzyme-1 mRNA expression in human cardiovascular disease.
Myocardial Infarction
Endothelin-converting enzyme and angiotensin-converting enzyme in failing hearts of rats with myocardial infarction.
Myocardial Infarction
Endothelin-converting enzyme-1 mRNA expression in human cardiovascular disease.
Myocardial Ischemia
Endothelin-converting enzyme inhibition in the rat model of acute heart failure: heart function and neurohormonal activation.
Myocardial Ischemia
[Correction of cardiac functions in rats with experimental myocardial ischemia by chronic administration of endothelin-converting enzyme inhibitor]
Neoplasm Metastasis
High endothelin-converting enzyme-1 expression independently predicts poor survival of patients with esophageal squamous cell carcinoma.
Neoplasm Metastasis
On the role of endothelin-converting enzyme-1 (ECE-1) and neprilysin in human breast cancer.
Neoplasm Metastasis
TIMAP, the versatile protein phosphatase 1 regulator in endothelial cells.
Neoplasms
CPU0213, a novel endothelin receptor antagonist, ameliorates septic renal lesion by suppressing ET system and NF-kappaB in rats.
Neoplasms
ECE-1 overexpression in head and neck cancer is associated with poor tumor differentiation and patient outcome.
Neoplasms
Effect of Anthocyanin-Rich Extract of Sour Cherry for Hyperglycemia-Induced Inflammatory Response and Impaired Endothelium-Dependent Vasodilation.
Neoplasms
Endothelin-1 as a Mediator of Heme Oxygenase-1-Induced Stemness in Colorectal Cancer: Influence of p53.
Neoplasms
Endothelin-2 synthesis is stimulated by the type-1 tumour necrosis factor receptor and cAMP: comparison with endothelin-converting enzyme-1 expression.
Neoplasms
Endothelin-converting enzyme-1 (ECE-1) is post-transcriptionally regulated by alternative polyadenylation.
Neoplasms
Endothelin-converting enzyme-1 in cancer aggressiveness.
Neoplasms
Endothelin-converting enzyme-1 inhibition and growth of human glioblastoma cells.
Neoplasms
Expression of endothelin-1 is related to poor prognosis in non-small cell lung carcinoma.
Neoplasms
Herpesvirus saimiri (HVS)-based endothelin converting enzyme-1 (ECE-1) shRNA expression decreases prostate cancer cell invasion and migration.
Neoplasms
High endothelin-converting enzyme-1 expression independently predicts poor survival of patients with esophageal squamous cell carcinoma.
Neoplasms
Immunohistochemical localization of endothelin-converting enzyme-1 in neuroendocrine tumors and normal human tissue.
Neoplasms
Isoforms of endothelin-converting enzyme-1 (ECE-1) have opposing effects on prostate cancer cell invasion.
Neoplasms
Localization of endothelin-converting enzyme-1 in human kidney.
Neoplasms
Localization of the endothelin system in human diffuse astrocytomas.
Neoplasms
Nitrogen Dioxide and Ultrafine Particles Dominate the Biological Effects of Inhaled Diesel Exhaust Treated by a Catalyzed Diesel Particulate Filter.
Neoplasms
On the role of endothelin-converting enzyme-1 (ECE-1) and neprilysin in human breast cancer.
Neoplasms
Phosphorylation of Endothelin-Converting Enzyme-1c at Serines 18 and 20 by CK2 Promotes Aggressiveness Traits in Colorectal Cancer Cells.
Neoplasms
Selective Indole-Based ECE Inhibitors: Synthesis and Pharmacological Evaluation.
Neoplasms
Small interfering RNA molecules targeting endothelin-converting enzyme-1 inhibit endothelin-1 synthesis and the invasive phenotype of ovarian carcinoma cells.
Neoplasms
Stromal-epithelial interactions influence prostate cancer cell invasion by altering the balance of metallopeptidase expression.
Neoplasms
The endothelin axis: a novel target for pharmacotherapy of female malignancies.
Neoplasms
The endothelin system in human glioblastoma.
Neoplasms
The mechanism of hyperpigmentation in seborrhoeic keratosis involves the high expression of endothelin-converting enzyme-1alpha and TNF-alpha, which stimulate secretion of endothelin 1.
Neoplasms
TIMAP, the versatile protein phosphatase 1 regulator in endothelial cells.
Nephrosis
Attenuation of puromycin aminonucleoside-induced glomerular lesions in rats by CGS 26303, a dual neutral endopeptidase/endothelin-converting enzyme inhibitor.
Nephrotic Syndrome
Regulation of endothelin-converting enzyme 1 in nephrotic syndrome in rats.
Neuroblastoma
Effects of 4-Hydroxy-Nonenal and Amyloid-beta on Expression and Activity of Endothelin Converting Enzyme and Insulin Degrading Enzyme in SH-SY5Y Cells.
Neuroblastoma
Endothelin-converting enzymes degrade ?-synuclein and are reduced in dementia with Lewy bodies.
Neuroblastoma
Expression of endothelin-converting enzyme in both neuroblastoma and glial cell lines and its localization in rat hippocampus.
Neuroblastoma
High expression of the novel endothelin-converting enzyme genes, Nbla03145/ECEL1alpha and beta, is associated with favorable prognosis in human neuroblastomas.
Neuroblastoma
Regulation of endothelin-converting enzyme-1 expression in human neuroblastoma cells.
Neuroendocrine Tumors
Immunohistochemical localization of endothelin-converting enzyme-1 in neuroendocrine tumors and normal human tissue.
Neurogenic Inflammation
Endothelin-converting enzyme 1 promotes re-sensitization of neurokinin 1 receptor-dependent neurogenic inflammation.
Neurogenic Inflammation
Re-sensitization of neuropeptide receptors: should we stop the recycling?
Obstetric Labor, Premature
Prevention of Inflammation-Associated Preterm Birth by Knockdown of the Endothelin-1-Matrix Metalloproteinase-1 Pathway.
Paraganglioma
Immunohistochemical localization of endothelin-converting enzyme-1 in neuroendocrine tumors and normal human tissue.
Periodontal Diseases
Periodontal disease and gene-expression levels of metalloendopeptidases in human buccal mucosal epithelium.
Pheochromocytoma
Immunohistochemical localization of endothelin-converting enzyme-1 in neuroendocrine tumors and normal human tissue.
Polycystic Kidney Diseases
The influence of the endothelin-converting enzyme-1 gene polymorphism on the progression of autosomal dominant polycystic kidney disease.
Polycystic Kidney, Autosomal Dominant
The influence of the endothelin-converting enzyme-1 gene polymorphism on the progression of autosomal dominant polycystic kidney disease.
Pre-Eclampsia
Endothelin converting enzyme (ECE) activity in normal pregnancy and preeclampsia.
Pre-Eclampsia
Placental endothelin-converting enzyme-1 is decreased in preeclampsia.
Pre-Eclampsia
Transfer and Vascular Effect of Endothelin Receptor Antagonists in the Human Placenta.
Pre-Eclampsia
[Genetic variability of endothelin-1 system in gestational hypertension and preeclampsia].
Prostatic Neoplasms
Differential expression of neutral endopeptidase-24.11 (neprilysin) and endothelin-converting enzyme in human prostate cancer cell lines.
Prostatic Neoplasms
ECE-1 influences prostate cancer cell invasion via ET-1-mediated FAK phosphorylation and ET-1-independent mechanisms.
Prostatic Neoplasms
Endothelin-converting enzyme-1 (ECE-1) is post-transcriptionally regulated by alternative polyadenylation.
Prostatic Neoplasms
Expression and localization of endothelin-converting enzyme-1 in human prostate cancer.
Prostatic Neoplasms
Herpesvirus saimiri (HVS)-based endothelin converting enzyme-1 (ECE-1) shRNA expression decreases prostate cancer cell invasion and migration.
Prostatic Neoplasms
Isoforms of endothelin-converting enzyme-1 (ECE-1) have opposing effects on prostate cancer cell invasion.
Prostatic Neoplasms
Stromal-epithelial interactions influence prostate cancer cell invasion by altering the balance of metallopeptidase expression.
Proteinuria
Inhibition of Both Neutral Endopeptidase and Endothelin-Converting Enzyme by SLV306 Reduces Proteinuria and Urinary Albumin Excretion in Diabetic Rats.
Pruritus
Neural peptidase endothelin-converting enzyme 1 regulates endothelin 1-induced pruritus.
Pulmonary Arterial Hypertension
[Chronic theatment with an endothelin-converting enzyme inhibitor reduces the development of hypoxia-induced pulmonary hypertension in rat]
Pulmonary Fibrosis
Endothelin-Converting Enzyme-1 Gene Ablation Attenuates Pulmonary Fibrosis via CGRP-cAMP/EPAC1 Pathway.
Renal Insufficiency
Endothelin in renal diseases and cardiovascular remodeling in renal failure.
Renal Insufficiency
Selective Indole-Based ECE Inhibitors: Synthesis and Pharmacological Evaluation.
Renal Insufficiency, Chronic
Therapeutic Effect of Endothelin-Converting Enzyme Inhibitor on Chronic Kidney Disease through the Inhibition of Endoplasmic Reticulum Stress and the NLRP3 Inflammasome.
Reperfusion Injury
Combination therapy of N-acetylcysteine, sodium nitroprusside and phosphoramidon attenuates ischemia-reperfusion injury in rat kidney.
Reperfusion Injury
Phosphoramidon, an endothelin converting enzyme inhibitor attenuates local gastric ischemia-reperfusion injury in rats.
Rhinitis
Co-expression of endothelin-1 and endothelin-converting enzyme-1 in patients with chronic rhinitis.
Scleroderma, Systemic
dsRNA activation of endothelin-1 and markers of vascular activation in endothelial cells and fibroblasts.
Scleroderma, Systemic
Serum activity of endothelin-converting enzyme correlates negatively with vital capacity in systemic sclerosis.
Sepsis
Endothelin-converting enzyme-1-mediated signaling in adult rat ventricular myocyte contractility and apoptosis during sepsis.
Squamous Cell Carcinoma of Head and Neck
ECE-1 overexpression in head and neck cancer is associated with poor tumor differentiation and patient outcome.
Stomach Neoplasms
Association of endothelin-converting enzyme-1b C-338A polymorphism with gastric cancer risk: a case-control study.
Stroke
Novel therapy approach in primary stroke prevention: simultaneous inhibition of endothelin converting enzyme and neutral endopeptidase in spontaneously hypertensive, stroke-prone rats improves survival.
Subarachnoid Hemorrhage
Attenuation of experimental subarachnoid hemorrhage-induced cerebral vasospasm by CGS 26303, an endothelin-converting enzyme inhibitor.
Subarachnoid Hemorrhage
Attenuation of SAH-induced cerebral vasospasm by a selective ECE inhibitor.
Subarachnoid Hemorrhage
CGS 26303 Upregulates mRNA Expression of Heme Oxygenase-1 in Brain Tissue of Rats Subjected to Experimental Subarachnoid Hemorrhage.
Subarachnoid Hemorrhage
Continuous intravenous infusion of CGS 26303, an endothelin-converting enzyme inhibitor, prevents and reverses cerebral vasospasm after experimental subarachnoid hemorrhage.
Subarachnoid Hemorrhage
Effect of endothelin-converting enzyme inhibitors on big endothelin-1 induced contraction in isolated rat basilar artery.
Subarachnoid Hemorrhage
Plasma endothelin and big endothelin concentrations and serum endothelin-converting enzyme activity following aneurysmal subarachnoid hemorrhage.
Subarachnoid Hemorrhage
Prevention and reversal of cerebral vasospasm by an endothelin-converting enzyme inhibitor, CGS 26303, in an experimental model of subarachnoid hemorrhage.
Subarachnoid Hemorrhage
Soluble and Catalytically Active Endothelin Converting Enzyme-1 is Present in Cerebrospinal Fluid of Subarachnoid Hemorrhage Patients.
Subarachnoid Hemorrhage
Systemic administration of an inhibitor of endothelin-converting enzyme for attenuation of cerebral vasospasm following experimental subarachnoid hemorrhage.
Subarachnoid Hemorrhage
[D-Val22]big ET-1[16-38] inhibits endothelin-converting enzyme activity: a promising concept in the prevention of cerebral vasospasm.
Tuberculosis
The endothelin system has a significant role in the pathogenesis and progression of Mycobacterium tuberculosis infection.
Ureteral Obstruction
Endothelin converting enzyme-1 (ECE-1) deletion in association with Endothelin-1 downregulation ameliorates kidney fibrosis in mice.
Ureteral Obstruction
Neutral endopeptidase inhibitors blunt kidney fibrosis by reducing myofibroblast formation.
Vascular Diseases
Chemokine- and cytokine-induced expression of endothelin 1 and endothelin-converting enzyme 1 in endothelial cells.
Vascular System Injuries
Endothelin inhibition delays onset of hyperglycemia and associated vascular injury in type I diabetes: evidence for endothelin release by pancreatic islet beta-cells.
Vascular System Injuries
Endothelin-converting enzyme expression in the rat vascular injury model and human coronary atherosclerosis.
Vasospasm, Intracranial
Attenuation of experimental subarachnoid hemorrhage-induced cerebral vasospasm by CGS 26303, an endothelin-converting enzyme inhibitor.
Vasospasm, Intracranial
Attenuation of experimental subarachnoid hemorrhage-induced increases in circulating intercellular adhesion molecule-1 and cerebral vasospasm by the endothelin-converting enzyme inhibitor CGS 26303.
Vasospasm, Intracranial
CGS 26303 Upregulates mRNA Expression of Heme Oxygenase-1 in Brain Tissue of Rats Subjected to Experimental Subarachnoid Hemorrhage.
Vasospasm, Intracranial
Continuous intravenous infusion of CGS 26303, an endothelin-converting enzyme inhibitor, prevents and reverses cerebral vasospasm after experimental subarachnoid hemorrhage.
Vasospasm, Intracranial
Endothelin and subarachnoid hemorrhage-induced cerebral vasospasm: pathogenesis and treatment.
Vasospasm, Intracranial
Oral administration of an inhibitor of endothelin-converting enzyme attenuates cerebral vasospasm following experimental subarachnoid haemorrhage in rabbits.
Vasospasm, Intracranial
Prevention and reversal of cerebral vasospasm by an endothelin-converting enzyme inhibitor, CGS 26303, in an experimental model of subarachnoid hemorrhage.
Vasospasm, Intracranial
Prevention and reversal of vasospasm and ultrastructural changes in basilar artery by continuous infusion of CGS 35066 following subarachnoid hemorrhage.
Vasospasm, Intracranial
Systemic administration of an inhibitor of endothelin-converting enzyme for attenuation of cerebral vasospasm following experimental subarachnoid hemorrhage.
Vasospasm, Intracranial
[D-Val22]big ET-1[16-38] inhibits endothelin-converting enzyme activity: a promising concept in the prevention of cerebral vasospasm.
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0.00109
(2S,4R)-2-[(2,5-difluorobenzylamino)methyl]-4-mercaptopyrrolidine-1-carboxylic acid isopropyl ester
Homo sapiens
-
IC50: 0.00109 mM
0.01089
(2S,4R)-2-[2-[[4-mercapto-1-(naphthalene-2-sulfonyl)-pyrrolidine-2-carbonyl]methylamino]acetylamino]-benzoic acid methyl ester
Homo sapiens
-
IC50: 0.01089 mM
0.0000765
(2S,4R)-4-acetylsulfanyl-2-(2,4,5-trifluorobenzyloxymethyl)pyrrolidine-1-carboxylic acid 2,3-dihydrobenzo-[1,4]dioxin-5-yl ester
Homo sapiens
-
IC50: 0.0000765 mM
0.0000215
(2S,4R)-4-acetylsulfanyl-2-(2,4,5-trifluorobenzyloxymethyl)pyrrolidine-1-carboxylic acid 2-methoxycarbonylphenylester
Homo sapiens
-
IC50: 0.0000215 mM
0.00253
(2S,4R)-4-mercapto-1-(naphthalene-2-sulfonyl)pyrrolidine-2-carboxylic acid N-methyl-N-(4-methylphenylsulfonyl)hydrazide
Homo sapiens
-
IC50: 0.00253 mM
0.000137
(2S,4R)-4-mercapto-2-(2,4,5-trifluorobenzyloxymethyl)-pyrrolidine-1-carboxylic acid 2,3-dihydrobenzo[1,4]-dioxin-5-yl ester
Homo sapiens
-
IC50: 0.000137 mM
0.000067
(2S,4R)-4-mercapto-2-(2,4,5-trifluorobenzyloxymethyl)-pyrrolidine-1-carboxylic acid 2-ethoxycarbonylphenylester
Homo sapiens
-
IC50: 0.000067 mM
0.0000729
(2S,4R)-5-[(2,5-difluorobenzylamino)methyl]-1-(5-propylpyrimidin-2-yl)pyrrolidine-3-thiol
Homo sapiens
-
IC50: 0.0000729 mM
0.0000198
(3R,5S)-1-(5-propylpyrimidin-2-yl)-5-(2,4,5-trifluorobenzyloxymethyl)pyrrolidine-3-thiol trifluoroacetate
Homo sapiens
-
IC50: 0.0000198 mM
0.00065
1-(2,6-difluorobenzyl)-5-[(3,3-dimethylbutanoyl)amino]-N-phenyl-1H-indole-2-carboxamide
Homo sapiens
-
IC50: 0.00065 mM
0.00012
1-(2-fluorobenzyl)-5-[[(1-methylcyclopentyl)acetyl]amino]-N-phenyl-1H-indole-2-carboxamide
Homo sapiens
-
IC50: 0.00012 mM
0.00086
1-(cyclohexylmethyl)-5-[(3,3-dimethylbutanoyl)amino]-N-phenyl-1H-indole-2-carboxamide
Homo sapiens
-
IC50: 0.00086 mM
0.00039
4-[([5-[(2,2-dimethylpropyl)carbamoyl]-1-(2-fluorobenzyl)-1H-indol-2-yl]carbonyl)amino]benzoic acid
Homo sapiens
-
IC50: 0.00039 mM
0.00066
5-[(3,3-dimethylbutanethioyl)amino]-1-(2-fluorobenzyl)-N-phenyl-1H-indole-2-carboxamide
Homo sapiens
-
IC50: 0.00066 mM
0.00022
5-[(3,3-dimethylbutanoyl)amino]-1-(2-fluorobenzyl)-N-phenyl-1H-indole-2-carboxamide
Homo sapiens
-
IC50: 0.00022 mM
0.003
5-[(3,3-dimethylbutanoyl)amino]-1-(2-methylbenzyl)-N-phenyl-1H-indole-2-carboxamide
Homo sapiens
-
IC50: 0.003 mM
0.0022
5-[(3,3-dimethylbutanoyl)amino]-1-[(2-methyl-1,3-thiazol-4-yl)methyl]-N-phenyl-1H-indole-2-carboxamide
Homo sapiens
-
IC50: 0.0022 mM
0.0059
5-[(3,3-dimethylbutanoyl)amino]-N,1-diphenyl-1H-indole-2-carboxamide
Homo sapiens
-
IC50: 0.0059 mM
0.0051
5-[(3,3-dimethylbutanoyl)amino]-N-phenyl-1-(2-phenylethyl)-1H-indole-2-carboxamide
Homo sapiens
-
IC50: 0.0051 mM
0.00017
5-[(3,3-dimethylbutanoyl)amino]-N-phenyl-1-[2-(trifluoromethyl)benzyl]-1H-indole-2-carboxamide
Homo sapiens
-
IC50: 0.00017 mM
0.00074
5-[(4,4-dimethylpentanoyl)amino]-1-(2-fluorobenzyl)-N-phenyl-1H-indole-2-carboxamide
Homo sapiens
-
IC50: 0.00074 mM
0.0003
5-[(bicyclo[2.2.1]hept-2-ylacetyl)amino]-1-(2-fluorobenzyl)-N-phenyl-1H-indole-2-carboxamide
Homo sapiens
-
IC50: 0.0003 mM
0.0064
5-[(cyclopentylacetyl)amino]-1-(2-fluorobenzyl)-N-phenyl-1H-indole-2-carboxamide
Homo sapiens
-
IC50: 0.0064 mM
0.074
5-[([5-[(2,2-dimethylpropyl)carbamoyl]-1-(2-fluorobenzyl)-1H-indol-2-yl]carbonyl)amino]pyridine-3-carboxylic acid
Homo sapiens
-
IC50: 0.074 mM
0.0067
5-[[(2,2-dimethylpropyl)sulfonyl]amino]-1-(2-fluorobenzyl)-N-phenyl-1H-indole-2-carboxamide
Homo sapiens
-
IC50: 0.0067 mM
0.0004805
benzoylsulfanyl-2-(2,4,5-trifluorobenzyloxymethyl)-pyrrolidine-1-carboxylic acid 2,3-dihydrobenzo[1,4]-dioxin-5-yl ester
Homo sapiens
-
IC50: 0.0004805 mM
0.000017
CGS 26303
Homo sapiens
-
optimized form of inhibitor, human recombinant ECE-1 overexpressed in CHO cells
0.0000058
CGS 34043
Homo sapiens
-
human recombinant ECE-1 overexpressed in CHO cells
0.000011
CGS 34226
Homo sapiens
-
human recombinant ECE-1 overexpressed in CHO cells
0.000022
CGS 35066
Homo sapiens
-
COS-1 cell membrane with overexpression of human ECE-1
0.000055
CGS 35601
Homo sapiens
-
-
0.000055
L-tryptophan, N-[[1-[[(2S)-2-mercapto-4-methyl-1-oxopentyl]amino]-cyclopentyl]carbonyl]
Homo sapiens
-
CGS 35601, IC50: 55 nM
0.01
N-(2,2-dimethylpropyl)-1-(2-fluorobenzyl)-2-(3-phenyl-1,2,4-oxadiazol-5-yl)-1H-indole-5-carboxamide
Homo sapiens
-
IC50: 0.01 mM
0.01
N-(2,2-dimethylpropyl)-1-(2-fluorobenzyl)-2-[(phenylamino)methyl]-1H-indole-5-carboxamide
Homo sapiens
-
IC50: 0.01 mM
0.00022
N2-(4-carbamoylphenyl)-N5-(2,2-dimethylpropyl)-1-(2-fluorobenzyl)-1H-indole-2,5-dicarboxamide
Homo sapiens
-
IC50: 0.00022 mM
0.0012
N2-(5-aminopyridin-2-yl)-N5-(2,2-dimethylpropyl)-1-(2-fluorobenzyl)-1H-indole-2,5-dicarboxamide
Homo sapiens
-
IC50: 0.0012 mM
0.00017
N2-(6-aminopyridin-3-yl)-N5-(2,2-dimethylpropyl)-1-(2-fluorobenzyl)-1H-indole-2,5-dicarboxamide
Homo sapiens
-
IC50: 0.00017 mM
0.00044
N2-(6-chloropyridin-3-yl)-N5-(2,2-dimethylpropyl)-1-(2-fluorobenzyl)-1H-indole-2,5-dicarboxamide
Homo sapiens
-
IC50: 0.00044 mM
0.00021
N2-[4-(dimethylcarbamoyl)phenyl]-N5-(2,2-dimethylpropyl)-1-(2-fluorobenzyl)-1H-indole-2,5-dicarboxamide
Homo sapiens
-
IC50: 0.00021 mM
0.0002
N2-[4-[(butylsulfonyl)amino]phenyl]-N5-(2,2-dimethylpropyl)-1-(2-fluorobenzyl)-1H-indole-2,5-dicarboxamide
Homo sapiens
-
IC50: 0.0002 mM
0.00013
N2-[6-(acetylamino)pyridin-3-yl]-N5-(2,2-dimethylpropyl)-1-(2-fluorobenzyl)-1H-indole-2,5-dicarboxamide
Homo sapiens
-
IC50: 0.00013 mM
0.00015
N5-(2,2-dimethylpropyl)-1-(2-fluorobenzyl)-N2-(3-[[4-(methylsulfamoyl)phenyl]carbamoyl]phenyl)-1H-indole-2,5-dicarboxamide
Homo sapiens
-
IC50: 0.00015 mM
0.0023
N5-(2,2-dimethylpropyl)-1-(2-fluorobenzyl)-N2-1,3,4-thiadiazol-2-yl-1H-indole-2,5-dicarboxamide
Homo sapiens
-
IC50: 0.0023 mM
0.01
N5-(2,2-dimethylpropyl)-1-(2-fluorobenzyl)-N2-1H-pyrazol-3-yl-1H-indole-2,5-dicarboxamide
Homo sapiens
-
IC50: 0.01 mM
0.007 - 0.01
N5-(2,2-dimethylpropyl)-1-(2-fluorobenzyl)-N2-phenyl-1H-indole-2,5-dicarboxamide
0.00085
N5-(2,2-dimethylpropyl)-1-(2-fluorobenzyl)-N2-pyridin-3-yl-1H-indole-2,5-dicarboxamide
Homo sapiens
-
IC50: 0.00085 mM
0.000039
N5-(2,2-dimethylpropyl)-1-(2-fluorobenzyl)-N2-[3-[(4-sulfamoylphenyl)carbamoyl]phenyl]-1H-indole-2,5-dicarboxamide
Homo sapiens
-
IC50: 0.000039 mM
0.09
N5-(2,2-dimethylpropyl)-1-(2-fluorobenzyl)-N2-[5-[(4-methylpiperazin-1-yl)carbonyl]pyridin-3-yl]-1H-indole-2,5-dicarboxamide
Homo sapiens
-
IC50: 0.09 mM
0.0049
[Lys-Gly-His-Lys-Cu]+
Homo sapiens
-
metallopeptide, IC50: 0.0049 mM under hydrolytic condtions
0.007
N5-(2,2-dimethylpropyl)-1-(2-fluorobenzyl)-N2-phenyl-1H-indole-2,5-dicarboxamide
Homo sapiens
-
IC50: 0.007 mM
0.01
N5-(2,2-dimethylpropyl)-1-(2-fluorobenzyl)-N2-phenyl-1H-indole-2,5-dicarboxamide
Homo sapiens
-
IC50: 0.01 mM
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Ahn, K.; Herman, S.B.; Fahnoe, D.C.
Soluble human endothelin-converting enzyme-1: expression, purification, and demonstration of pronounced pH sensitivity
Arch. Biochem. Biophys.
359
258-268
1998
Homo sapiens
brenda
Cronin, N.B.; Wallace, B.A.
Do the structures of big ET-1 and big ET-3 adopt a similar overall fold? Consequences for endothelin converting enzyme specificity
Biochemistry
38
1721-1726
1999
Homo sapiens
brenda
Korth, P.; Egidy, G.; Parnot, C.; LeMoullec, J.M.; Corvol, P.; Pinet, F.
Construction, expression and characterization of a soluble form of human endothelin-converting-enzyme-1
FEBS Lett.
417
365-370
1997
Homo sapiens
brenda
Wallace, E.M.; Moliterni, J.A.; Moskal, M.A.; Neubert, A.D.; Marcopulos, N.; Stamford, L.B.; Trapani, A.J.; Savage, P.; Chou, M.; Jeng, A.Y.
Design and synthesis of potent, selective inhibitors of endothelin-converting enzyme
J. Med. Chem.
41
1513-1523
1998
Homo sapiens
brenda
Bur, D.; Dale, G.E.; Oefner, C.
A three-dimensional model of endothelin-converting enzyme (ECE) based on the X-ray structure of neutral endopeptidase 24.11 (NEP)
Protein Eng.
14
337-341
2001
Homo sapiens
brenda
Brands, M.; Ergueden, J.K.; Hashimoto, K.; Heimbach, D.; Schroeder, C.; Siegel, S.; Stasch, J.P.; Weigand, S.
Novel, selective indole-based ECE inhibitors: lead optimization via solid-phase and classical synthesis
Bioorg. Med. Chem. Lett.
15
4201-4205
2005
Homo sapiens
brenda
Awano, S.; Dawson, L.A.; Hunter, A.R.; Turner, A.J.; Usmani, B.A.
Endothelin system in oral squamous carcinoma cells: specific siRNA targeting of ECE-1 blocks cell proliferation
Int. J. Cancer
118
1645-1652
2006
Homo sapiens
brenda
Gokhale, N.H.; Cowan, J.A.
Metallopeptide-promoted inactivation of angiotensin-converting enzyme and endothelin-converting enzyme 1: Toward dual-action therapeutics
J. Biol. Inorg. Chem.
11
937-947
2006
Homo sapiens
brenda
Trapani, A.J.; Beil, M.E.; Bruseo, C.W.; Savage, P.; Firooznia, F.; Jeng, A.Y.
CGS 35601 and its orally active prodrug CGS 37808 as triple inhibitors of endothelin-converting enzyme-1, neutral endopeptidase 24.11, and angiotensin-converting enzyme
J. Cardiovasc. Pharmacol.
44
S211-S215
2004
Homo sapiens
-
brenda
Berger, Y.; Dehmlow, H.; Blum-Kaelin, D.; Kitas, E.A.; Loeffler, B.M.; Aebi, J.D.; Juillerat-Jeanneret, L.
Endothelin-converting enzyme-1 inhibition and growth of human glioblastoma cells
J. Med. Chem.
48
483-498
2005
Homo sapiens
brenda
Dibas, A.; Prasanna, G.; Yorio, T.
Characterization of endothelin-converting enzyme activities in ARPE-19 cells, a human retinal pigmented epithelial cell line
J. Ocul. Pharmacol. Ther.
21
196-204
2005
Homo sapiens
brenda
Hanessian, S.; Gauchet, C.; Charron, G.; Marin, J.; Nakache, P.
Design and synthesis of diversely substituted azacyclic inhibitors of endothelin converting enzyme
J. Org. Chem.
71
2760-2778
2006
Homo sapiens
brenda
Klipper, E.; Gilboa, T.; Levy, N.; Kisliouk, T.; Spanel-Borowski, K.; Meidan, R.
Characterization of endothelin-1 and nitric oxide generating systems in corpus luteum-derived endothelial cells
Reproduction
128
463-473
2004
Homo sapiens
brenda
Smollich, M.; Goette, M.; Yip, G.W.; Yong, E.S.; Kersting, C.; Fischgraebe, J.; Radke, I.; Kiesel, L.; Wuelfing, P.
On the role of endothelin-converting enzyme-1 (ECE-1) and neprilysin in human breast cancer
Breast Cancer Res. Treat.
106
361-369
2007
Homo sapiens
brenda
Roosterman, D.; Kempkes, C.; Cottrell, G.S.; Padilla, B.E.; Bunnett, N.W.; Turck, C.W.; Steinhoff, M.
Endothelin-converting enzyme-1 degrades internalized somatostatin-14
Endocrinology
149
2200-2207
2008
Homo sapiens
brenda
Fisk, L.; Nalivaeva, N.N.; Turner, A.J.
Regulation of endothelin-converting enzyme-1 expression in human neuroblastoma cells
Exp. Biol. Med.
231
1048-1053
2006
Homo sapiens, Rattus norvegicus
brenda
Dawson, L.A.; Maitland, N.J.; Berry, P.; Turner, A.J.; Usmani, B.A.
Expression and localization of endothelin-converting enzyme-1 in human prostate cancer
Exp. Biol. Med.
231
1106-1110
2006
Homo sapiens
brenda
Jafri, F.; Ergul, A.
Phosphorylation of endothelin converting enzyme-1 isoforms: relevance to subcellular localization
Exp. Biol. Med.
231
713-717
2006
Homo sapiens
brenda
Hunter, A.R.; Turner, A.J.
Expression and localization of endothelin-converting enzyme-1 isoforms in human endothelial cells
Exp. Biol. Med.
231
718-722
2006
Homo sapiens
brenda
Klipper, E.; Levy, N.; Gilboa, T.; Muller, L.; Meidan, R.
Identification of a novel alternatively spliced variant endothelin converting enzyme-1 lacking a transmembrane domain
Exp. Biol. Med.
231
723-728
2006
Homo sapiens
brenda
Jackson, C.D.; Barnes, K.; Homer-Vanniasinkam, S.; Turner, A.J.
Expression and localization of human endothelin-converting enzyme-1 isoforms in symptomatic atherosclerotic disease and saphenous vein
Exp. Biol. Med.
231
794-801
2006
Homo sapiens
brenda
Kuruppu, S.; Reeve, S.; Ian Smith, A.
Characterisation of endothelin converting enzyme-1 shedding from endothelial cells
FEBS Lett.
581
4501-4506
2007
Homo sapiens
brenda
Massai, L.; Volpi, N.; Carbotti, P.; Fruschelli, M.; Mencarelli, M.; Pecorelli, A.; Muscettola, M.; Agliano, M.; Alessandrini, C.; Grasso, G.
Endothelin-1 and endothelin-converting enzyme-1 in human granulomatous pathology of eyelid: an immunohistochemical and in situ hybridization study in chalazia
Histol. Histopathol.
22
1343-1354
2007
Homo sapiens
brenda
Padilla, B.E.; Cottrell, G.S.; Roosterman, D.; Pikios, S.; Muller, L.; Steinhoff, M.; Bunnett, N.W.
Endothelin-converting enzyme-1 regulates endosomal sorting of calcitonin receptor-like receptor and beta-arrestins
J. Cell Biol.
179
981-997
2007
Homo sapiens
brenda
Suekane, T.; Ikura, Y.; Arimoto, J.; Nakagawa, M.; Kitabayashi, C.; Naruko, T.; Watanabe, T.; Fujiwara, Y.; Oshitani, N.; Maeda, K.; Tanzawa, K.; Hirakawa, K.; Arakawa, T.; Ueda, M.
Enhanced expressions of endothelin-converting enzyme and endothelin receptors in human colonic tissues of Crohns disease
J. Clin. Biochem. Nutr.
42
126-132
2008
Homo sapiens
brenda
Iwase, A.; Ando, H.; Nagasaka, T.; Goto, M.; Harata, T.; Kikkawa, F.
Distribution of endothelin-converting enzyme-1 and neutral endopeptidase in human endometrium
J. Histochem. Cytochem.
55
1229-1235
2007
Homo sapiens
brenda
Shirai, N.; Naruko, T.; Ohsawa, M.; Ikura, Y.; Sugama, Y.; Hirayama, M.; Kitabayashi, C.; Ehara, S.; Inoue, T.; Itoh, A.; Haze, K.; Tanzawa, K.; Yoshiyama, M.; Yoshikawa, J.; Ueda, M.
Expression of endothelin-converting enzyme, endothelin-1 and endothelin receptors at the site of percutaneous coronary intervention in humans
J. Hypertens.
24
711-721
2006
Homo sapiens
brenda
Daray, F.M.; Colombo, J.R.; Kibrik, J.R.; Errasti, A.E.; Pelorosso, F.G.; Nowak, W.; Cracowski, J.L.; Rothlin, R.P.
Involvement of endothelial thromboxane A2 in the vasoconstrictor response induced by 15-E2t-isoprostane in isolated human umbilical vein
Naunyn Schmiedebergs Arch. Pharmacol.
373
367-375
2006
Homo sapiens
brenda
Buehler, K.; Ufer, M.; Mueller-Marbach, A.; Brinkmann, U.; Laule, M.; Stangl, V.; Roots, I.; Stangl, K.; Cascorbi, I.
Risk of coronary artery disease as influenced by variants of the human endothelin and endothelin-converting enzyme genes
Pharmacogenet. Genomics
17
77-83
2007
Homo sapiens
brenda
Choi, D.S.; Wang, D.; Yu, G.Q.; Zhu, G.; Kharazia, V.N.; Paredes, J.P.; Chang, W.S.; Deitchman, J.K.; Mucke, L.; Messing, R.O.
PKCepsilon increases endothelin converting enzyme activity and reduces amyloid plaque pathology in transgenic mice
Proc. Natl. Acad. Sci. USA
103
8215-8220
2006
Homo sapiens, Mus musculus
brenda
Keeble, J.E.
Re-sensitization of neuropeptide receptors: should we stop the recycling?
Br. J. Pharmacol.
156
728-729
2009
Homo sapiens
brenda
Cattaruzza, F.; Cottrell, G.S.; Vaksman, N.; Bunnett, N.W.
Endothelin-converting enzyme 1 promotes re-sensitization of neurokinin 1 receptor-dependent neurogenic inflammation
Br. J. Pharmacol.
156
730-739
2009
Homo sapiens, Rattus norvegicus
brenda
Rayhman, O.; Klipper, E.; Muller, L.; Davidson, B.; Reich, R.; Meidan, R.
Small interfering RNA molecules targeting endothelin-converting enzyme-1 inhibit endothelin-1 synthesis and the invasive phenotype of ovarian carcinoma cells
Cancer Res.
68
9265-9273
2008
Homo sapiens
brenda
Peltonen, T.; Taskinen, P.; Naepaenkangas, J.; Leskinen, H.; Ohtonen, P.; Soini, Y.; Juvonen, T.; Satta, J.; Vuolteenaho, O.; Ruskoaho, H.
Increase in tissue endothelin-1 and ETA receptor levels in human aortic valve stenosis
Eur. Heart J.
30
242-249
2009
Homo sapiens
brenda
Martinez-Miguel, P.; Raoch, V.; Zaragoza, C.; Valdivielso, J.M.; Rodriguez-Puyol, M.; Rodriguez-Puyol, D.; Lopez-Ongil, S.
Endothelin-converting enzyme-1 increases in atherosclerotic mice: potential role of oxidized low density lipoproteins
J. Lipid Res.
50
364-375
2009
Bos taurus, Homo sapiens, Mus musculus, Mus musculus C57/BL6J
brenda
Schulz, H.; Dale, G.E.; Karimi-Nejad, Y.; Oefner, C.
Structure of human endothelin-converting enzyme I complexed with phosphoramidon
J. Mol. Biol.
385
178-187
2009
Homo sapiens (P42892), Homo sapiens
brenda
Cerdeira, A.S.; Bras-Silva, C.; Leite-Moreira, A.F.
Endothelin-converting enzyme inhibitors: their application in cardiovascular diseases
Rev. Port. Cardiol.
27
385-408
2008
Bos taurus, Homo sapiens, Rattus norvegicus, Sus scrofa, Cavia sp.
brenda
Cottrell, G.S.; Padilla, B.E.; Amadesi, S.; Poole, D.P.; Murphy, J.E.; Hardt, M.; Roosterman, D.; Steinhoff, M.; Bunnett, N.W.
Endosomal endothelin-converting enzyme-1: a regulator of beta-arrestin-dependent ERK signaling
J. Biol. Chem.
284
22411-22425
2009
Homo sapiens, Mus musculus, Rattus norvegicus
brenda
Jullien, N.; Makritis, A.; Georgiadis, D.; Beau, F.; Yiotakis, A.; Dive, V.
Phosphinic tripeptides as dual angiotensin-converting enzyme C-domain and endothelin-converting enzyme-1 inhibitors
J. Med. Chem.
53
208-220
2010
Homo sapiens
brenda
Jin, Z.; Luxiang, C.; Huadong, Z.; Zhiqiang, X.; Lihua, H.; Huiyun, L.
C-338A polymorphism of the endothelin-converting enzyme-1 gene and the susceptibility to carotid atherosclerosis
Microvasc. Res.
78
128-131
2009
Homo sapiens
brenda
Palmer, J.C.; Kehoe, P.G.; Love, S.
Endothelin-converting enzyme-1 in Alzheimers disease and vascular dementia
Neuropathol. Appl. Neurobiol.
36
487-497
2010
Homo sapiens
brenda
Whyteside, A.R.; Hinsley, E.E.; Lambert, L.A.; McDermott, P.J.; Turner, A.J.
ECE-1 influences prostate cancer cell invasion via ET-1-mediated FAK phosphorylation and ET-1-independent mechanisms
Can. J. Physiol. Pharmacol.
88
850-854
2010
Homo sapiens
brenda
Wang, S.; Wang, R.; Chen, L.; Bennett, D.A.; Dickson, D.W.; Wang, D.S.
Expression and functional profiling of neprilysin, insulin-degrading enzyme, and endothelin-converting enzyme in prospectively studied elderly and Alzheimers brain
J. Neurochem.
115
47-57
2010
Homo sapiens
brenda
Hasdemir, B.; Mahajan, S.; Bunnett, N.W.; Liao, M.; Bhargava, A.
Endothelin-Converting Enzyme-1 Actions Determine Differential Trafficking and Signaling of Corticotropin-Releasing Factor Receptor 1 at High Agonist Concentrations
Mol. Endocrinol.
26
681-695
2012
Homo sapiens
brenda
Sonawane, K.; Barage, S.
Structural analysis of membrane-bound hECE-1 dimer using molecular modeling techniques: insights into conformational changes and Abeta1-42 peptide binding
Amino Acids
47
543-559
2015
Homo sapiens (P42892), Homo sapiens
brenda
Pacheco-Quinto, J.; Herdt, A.; Eckman, C.; Eckman, E.
Endothelin-converting enzymes and related metalloproteases in Alzheimer's disease
J. Alzheimers Dis.
33
S101
2013
Homo sapiens (P42892)
brenda
Jensen, D.; Halls, M.; Murphy, J.; Canals, M.; Cattaruzza, F.; Poole, D.; Lieu, T.; Koon, H.; Pothoulakis, C.; Bunnett, N.
Endothelin-converting enzyme 1 and beta-arrestins exert spatiotemporal control of substance P-induced inflammatory signals
J. Biol. Chem.
289
20283-20294
2014
Homo sapiens (P42892), Homo sapiens
brenda
Kido-Nakahara, M.; Buddenkotte, J.; Kempkes, C.; Ikoma, A.; Cevikbas, F.; Akiyama, T.; Nunes, F.; Seeliger, S.; Hasdemir, B.; Mess, C.; Buhl, T.; Sulk, M.; Mller, F.; Metze, D.; Bunnett, N.; Bhargava, A.; Carstens, E.; Furue, M.; Steinhoff, M.
Neural peptidase endothelin-converting enzyme 1 regulates endothelin 1-induced pruritus
J. Clin. Invest.
124
2683-2695
2014
Homo sapiens (P42892), Homo sapiens, Mus musculus (Q4PZA2), Mus musculus
brenda
Park, P.; Lee, T.; Cho, E.
Substance P stimulates endothelin 1 secretion via endothelin-converting enzyme 1 and promotes melanogenesis in human melanocytes
J. Invest. Dermatol.
135
551-559
2015
Homo sapiens (P42892), Homo sapiens
brenda
Tanneeru, K.; Sahu, I.; Guruprasad, L.
Ligand-based drug design for human endothelin converting enzyme-1 inhibitors
Med. Chem. Res.
22
4401-4409
2013
Homo sapiens (P42892)
-
brenda
Kuruppu, S.; Chou, S.; Feske, S.; Suh, S.; Hanchapola, I.; Lo, E.; Ning, M.; Smith, A.
Soluble and catalytically active endothelin converting enzyme-1 is present in cerebrospinal fluid of subarachnoid hemorrhage patients
Mol. Cell. Proteomics
13
1091-1094
2014
Homo sapiens (P42892), Homo sapiens
brenda
Whyteside, A.; Turner, A.; Lambert, D.
Endothelin-converting enzyme-1 (ECE-1) is post-transcriptionally regulated by alternative polyadenylation
PLoS ONE
9
e83260
2014
Homo sapiens (P42892)
brenda
Lu, J.; Willars, G.B.
Endothelin-converting enzyme-1 regulates glucagon-like peptide-1 receptor signalling and resensitisation
Biochem. J.
476
513-533
2019
Homo sapiens (P42892), Homo sapiens
brenda
Boratko, A.; Vereb, Z.; Petrovski, G.; Csortos, C.
TIMAP-protein phosphatase 1-complex controls endothelin-1 production via ECE-1 dephosphorylation
Int. J. Biochem. Cell Biol.
73
11-18
2016
Homo sapiens (P42892)
brenda
Smith, A.I.; Rajapakse, N.W.; Kleifeld, O.; Lomonte, B.; Sikanyika, N.L.; Spicer, A.J.; Hodgson, W.C.; Conroy, P.J.; Small, D.H.; Kaye, D.M.; Parkington, H.C.; Whisstock, J.C.; Kuruppu, S.
N-terminal domain of Bothrops asper myotoxin II enhances the activity of endothelin converting enzyme-1 and neprilysin
Sci. Rep.
6
22413
2016
Homo sapiens (P42892)
brenda
Wu, C.F.; Lee, C.T.; Kuo, Y.H.; Chen, T.H.; Chang, C.Y.; Chang, I.W.; Wang, W.L.
High endothelin-converting enzyme-1 expression independently predicts poor survival of patients with esophageal squamous cell carcinoma
Tumor Biol.
39
1010428317725922
2017
Homo sapiens (P42892), Homo sapiens
brenda