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(7-methoxy-coumarin-4-yl)acetyl-Arg-Pro-Pro-Gly-Phe-Ser-Ala-Phe-Lys(2,4-dinitrophenyl) + H2O
?
-
fluorogenic substrate
-
-
?
(7-methoxycoumarin-4-yl)acetyl-Arg-Pro-Pro-Gly-Phe-Ser-Ala-Phe-Lys(2,4-dinitrophenyl)-OH + H2O
?
-
-
-
?
(7-methoxycoumarin-4-yl)acetyl-Arg-Pro-Pro-Gly-Phe-Ser-Ala-Phe-Lys-2,4-dinitrophenyl-OH + H2O
?
-
-
-
-
?
amyloid beta 40 + H2O
?
-
-
-
?
amyloid beta peptide + H2O
?
amyloid-beta peptide + H2O
?
amyloid-beta peptide + H2O
amyloid-beta peptide + ?
-
protein kinase C epsilon, PKCepsilon, stimulates the amyloid-beta peptide degradation by ECE-1 in mice leading to a decrease in plaque-associated astrocytosis and dystrophic neurites, overview
-
-
?
angiotensin I + H2O
?
-
-
-
?
angiotensin-I + H2O
?
-
degradation, no activity with angiotensin-II
-
-
?
big endothelin (18-34) + H2O
?
-
-
-
?
big endothelin + H2O
endothelin + ?
big endothelin + H2O
endothelin 1 + ?
big endothelin + H2O
endothelin-1 + ?
Big endothelin 1 + H2O
?
-
key enzyme in endothelin production, generates potent vasoconstrictor endothelin from its inactive precursor
-
-
?
big endothelin-1 + H2O
big endothelin fragment 22-38 + ?
-
-
-
?
big endothelin-1 + H2O
endothelin + ?
big endothelin-1 + H2O
endothelin-1 + ?
big endothelin-2 + H2O
?
-
-
-
-
?
big endothelin-3 + H2O
endothelin-3 + ?
big endothelin-I + H2O
endothelin + ?
calcitonin gene-related peptide + H2O
?
corticotropin-releasing factor + H2O
?
-
ECE-1 cleaves urocortin-1 (Ucn1) at three different sites but cleaves corticotropin-releasing factor (CRF) at only one site. ECE-1 degrades Ucn1 at both extracellular (pH 7.4) and endosomal (pH 5.5), whereas CRF is degraded at acidic pH alone. At a low or basal level, ECE-1 can disrupt association of Ucn1 or CRF with CRF1 in endosomes and free the receptor to promote recycling and resensitization
-
-
?
Human big endothelin 1 + H2O
Endothelin 1 + big endothelin 1(21-38)
Human big endothelin 2 + H2O
?
Human big endothelin 3 + H2O
?
insulin B chain + H2O
?
-
-
-
-
?
M7-methoxycoumarin-4-ylacetyl-Arg-Pro-Pro-Gly-Phe-Ser-Ala-Phe-Lys(2,4-dinitrophenyl)-OH + H2O
?
-
-
-
-
?
preendothelin + H2O
endothelin + ?
-
-
-
?
preproendothelin-1 + H2O
endothelin-1 + ?
-
-
-
-
?
proendothelin + H2O
endothelin-1 + ?
-
-
-
?
proendothelin-1 + H2O
endothelin + ?
activation
-
-
?
somatostatin + H2O
?
-
-
-
?
Somatostatin-14 + H2O
?
-
i.e. SST-14, degradation of rat substrate internalized via recombinantly expressed somatostatin receptor subtype sst2A into HEK-293 cells
-
-
?
urocortin-1 + H2O
?
-
ECE-1 cleaves urocortin-1 (Ucn1) at three different sites but cleaves corticotropin-releasing factor (CRF) at only one site. ECE-1 cleaves Ucn1 at Arg-34, which allows this ligands to bind and activate CRF1. ECE-1 degrades Ucn1 at both extracellular (pH 7.4) and endosomal (pH 5.5), whereas CRF is degraded at acidic pH alone. At a low or basal level, ECE-1 can disrupt association of Ucn1 or CRF with CRF1 in endosomes and free the receptor to promote recycling and resensitization
-
-
?
additional information
?
-
amyloid beta peptide + H2O
?
-
-
-
-
?
amyloid beta peptide + H2O
?
-
-
-
?
amyloid-beta peptide + H2O
?
-
-
-
-
?
amyloid-beta peptide + H2O
?
-
degradation
-
-
?
amyloid-beta peptide + H2O
?
-
degradation
-
-
?
amyloid-beta peptide + H2O
?
-
degradation
-
-
?
big endothelin + H2O
endothelin + ?
-
-
-
-
?
big endothelin + H2O
endothelin + ?
-
-
-
?
big endothelin + H2O
endothelin + ?
-
-
-
-
?
big endothelin + H2O
endothelin + ?
-
activation
-
-
?
big endothelin + H2O
endothelin + ?
-
ECE-1 is a membrane-bound metalloprotease responsible for production of vasoactive endothelin-1 from inactive big ET-1
-
-
?
big endothelin + H2O
endothelin + ?
-
-
-
-
?
big endothelin + H2O
endothelin + ?
-
PKCepsilon regulates the expression of ECE-1 in the brain
-
-
?
big endothelin + H2O
endothelin 1 + ?
-
-
-
-
?
big endothelin + H2O
endothelin 1 + ?
-
ECE-1a, 1b, 1c and 1d are all equally active on endothelin
-
-
?
big endothelin + H2O
endothelin-1 + ?
-
-
-
-
?
big endothelin + H2O
endothelin-1 + ?
-
-
-
?
big endothelin + H2O
endothelin-1 + ?
-
-
-
-
?
big endothelin + H2O
endothelin-1 + ?
-
-
-
-
?
big endothelin + H2O
endothelin-1 + ?
-
-
-
-
?
big endothelin + H2O
endothelin-1 + ?
-
-
-
?
big endothelin-1 + H2O
endothelin + ?
-
-
-
?
big endothelin-1 + H2O
endothelin + ?
-
key enzyme in the biosynthesis of the endothelins
-
?
big endothelin-1 + H2O
endothelin + ?
-
activation
-
-
?
big endothelin-1 + H2O
endothelin + ?
-
ECE-1 is a critical enzyme in the production of the potent vasoconstrictor peptide endothelin, ET-1
-
-
?
big endothelin-1 + H2O
endothelin-1 + ?
-
activation
-
-
?
big endothelin-1 + H2O
endothelin-1 + ?
-
-
-
?
big endothelin-1 + H2O
endothelin-1 + ?
-
-
-
?
big endothelin-1 + H2O
endothelin-1 + ?
-
-
-
-
?
big endothelin-1 + H2O
endothelin-1 + ?
-
-
-
?
big endothelin-1 + H2O
endothelin-1 + ?
-
final step of posttranslational processing of this peptide
-
?
big endothelin-1 + H2O
endothelin-1 + ?
-
most potent naturally occurring vasoconstrictor
-
?
big endothelin-1 + H2O
endothelin-1 + ?
-
activation
-
-
?
big endothelin-1 + H2O
endothelin-1 + ?
-
ECE-1 inhibition in MCF-7 breast cancer cells leads to a significantly decreased ET-1 expression and reduced cell invasiveness, overview
-
-
?
big endothelin-1 + H2O
endothelin-1 + ?
-
short-term endothelin-1 release is not involved in the isometric tension in response to different agonists, e.g. 15-E2t-IsoP, of human umbilical vein ring with or without endothelium, overview
-
-
?
big endothelin-1 + H2O
endothelin-1 + ?
big endothelin-1 is hydrolyzed at Asp18-Ile19
-
-
?
big endothelin-1 + H2O
endothelin-1 + ?
big endothelin-1 is hydrolyzed at Asp18-Ile19
-
-
?
big endothelin-1 + H2O
endothelin-1 + ?
-
-
-
-
?
big endothelin-1 + H2O
endothelin-1 + ?
-
-
-
?
big endothelin-3 + H2O
endothelin-3 + ?
-
specific for this substrate, big-endothelin-1 is no substrate
-
?
big endothelin-3 + H2O
endothelin-3 + ?
-
-
-
-
?
big endothelin-I + H2O
endothelin + ?
-
-
-
?
big endothelin-I + H2O
endothelin + ?
-
key enzyme in the biosynthesis of the endothelins
-
?
bradykinin + H2O
?
-
-
-
-
?
bradykinin + H2O
?
-
-
-
?
bradykinin + H2O
?
-
-
-
-
?
bradykinin + H2O
?
-
degradation
-
-
?
calcitonin gene-related peptide + H2O
?
-
degradation
-
-
?
calcitonin gene-related peptide + H2O
?
-
degradation, co-internalization with ECE-1 into early endosomes, calcitonin gene-related peptide degradation promotes CLR/RAMP1 recycling and beta-arrestin2 redistribution into the cytosol, ECE-1 inhibition or knockdown traps CLR/RAMP1 and beta-arrestin2 in endosomes and inhibits CLR/RAMP1 recycling and resensitization, whereas ECE-1 overexpression has the opposite effect, mechanism, overview
-
-
?
Human big endothelin 1 + H2O
Endothelin 1 + big endothelin 1(21-38)
-
best substrate
-
?
Human big endothelin 1 + H2O
Endothelin 1 + big endothelin 1(21-38)
-
cleavage site: Trp21-Val22
-
?
Human big endothelin 1 + H2O
Endothelin 1 + big endothelin 1(21-38)
-
best substrate
-
-
?
Human big endothelin 2 + H2O
?
-
hydrolysis at about 40% the rate of big endothelin1
-
-
?
Human big endothelin 2 + H2O
?
-
hydrolysis at 25% the rate of big endothelin1
-
-
?
Human big endothelin 3 + H2O
?
-
hydrolysis at about 30% the rate of big endothelin1
-
-
?
Human big endothelin 3 + H2O
?
-
big endothelin 3(1-41)amide
-
-
?
Human big endothelin 3 + H2O
?
-
hydrolysis at 50% the rate of big endothelin1
-
-
?
neurotensin + H2O
?
-
-
-
-
?
neurotensin + H2O
?
-
-
-
?
Substance P + H2O
?
-
-
-
-
?
Substance P + H2O
?
-
-
-
?
Substance P + H2O
?
-
-
-
-
?
Substance P + H2O
?
-
-
-
?
Substance P + H2O
?
-
-
-
-
?
additional information
?
-
-
no substrate is the big endothelin 1(1-31) fragment
-
-
?
additional information
?
-
-
isoforms of endothelin-converting enzyme-1, ECE-1a-d, are present in early endosomes, where they degrade neuropeptides and regulate post-endocytic sorting of receptors, ECE-1 does not regulate either the resensitization of receptors for peptides that are not ECE-1 substrates, e.g. angiotensin II, or the recycling of the bradykinin B2 receptor, which transiently interacts with beta-arrestins
-
-
?
additional information
?
-
-
the enzyme catalyzes the final step in endothelin processing
-
-
?
additional information
?
-
-
the enzyme is involved in chalizia, a granulomatous lesions of the eyelid
-
-
?
additional information
?
-
-
the enzyme plays a crucial role in the regulation of vascular tone and endothelial function
-
-
?
additional information
?
-
-
activity with octreotide
-
-
?
additional information
?
-
-
ECE-1 and endosomal acidification regulate the duration of substance P-induced ERK2 activation
-
-
?
additional information
?
-
-
ECEs can hydrolyze several other biologically active peptides in vitro by cleavage on the amino side of hydrophobic residues
-
-
?
additional information
?
-
-
endothelin-converting enzyme function as vasopeptidase
-
-
?
additional information
?
-
-
endothelin-converting enzyme-1 degrades substance P in early endosomes of epithelial cells and neurons to destabilize the endosomal mitogen-activated protein kinase signalosome and terminate signaling
-
-
?
additional information
?
-
-
endothelin-converting enzyme-1 degrades substance P in early endosomes of epithelial cells and neurons to destabilize the endosomal mitogen-activated protein kinase signalosome and terminate signaling
-
-
?
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(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
-
-
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-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-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
-
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 26393
-
slight inhibition
CGS 26582
-
synthetic inhibitor, ECE/NEP/ACE 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
CGS-26303
-
specific, complete inhibition at 0.025 mM
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
-
FR901533
-
specific ECE-1 inhibitor, in vitro not in vivo
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-(alpha-L-rhamnopyranosyl-oxyhydroxy-phosphinyl)-L-Leu-L-Trp
mechanism of inhibitor binding analysed (cocrystallization)
N-(alpha-rhamnopyranosyloxyhydroxyphosphinyl)-Leu-Trp
-
phosphoramidon, synthetic inhibitor, ECE-1/NEP inhibitor
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
-
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
-
IC50: 0.007 mM; IC50: 0.01 mM
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
SCH 54470
-
synthetic inhibitor, ECE/NEP/ACE inhibitor
SLV-306
-
KC-12792, synthetic inhibitor, ECE-1/NEP inhibitor, clinical trial for treatment of arterial hypertension and heart failure in human
SM19712
selective inhibitor, 0.01 mM used in inhibition assay conditions
specific ECE-1 inhibitor
-
in the presence of 0.001 M ECE-1 inhibitor, cell number was effectively reduced to ~70% of control
-
WS-79089B
-
natural inhibitor, selective ECE-1 inhibitor
WS75624A
-
natural inhibitor, selective ECE-1 inhibitor
WS79089A
-
natural inhibitor, selective ECE-1 inhibitor
WS79089C
-
natural inhibitor, selective ECE-1 inhibitor
[Lys-Gly-His-Lys-Co(NH3)2]2+
-
metallopeptide
[Lys-Gly-His-Lys-Cu]+
-
metallopeptide, IC50: 0.0049 mM under hydrolytic condtions
1,10-phenanthroline
-
-
1,10-phenanthroline
-
1 mM, inhibition of ECE-1 activity
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
-
-
CGS 26303
-
synthetic inhibitor, ECE-1/NEP inhibitor
CGS 26303
-
synthetic inhibitor, ECE-1/NEP inhibitor
CGS 35066
-
synthetic inhibitor, selective ECE-1 inhibitor
CGS-35066
-
a selective ECE-1 inhibitor, mimicks the effects of CGS-26303
CGS-35066
complete inhibition at 5 nM
EDTA
-
0.03 mM, Zn2+ restores, Cu2+, Co2+, Mn2+ or Fe2+ partially restores, not Ca2+ or Mg2+
phosphoramidon
-
0.1 mM, in vivo and in vitro
phosphoramidon
-
complete inhibition at 0.1 mM
phosphoramidon
-
0.1 M, 35% inhibition of ECE-1 activity
phosphoramidon
-
a metalloproteinase 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
RO 67-7447
-
synthetic inhibitor, selective ECE-1 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
SM-19712
0.01 mM used in assay conditions
SM-19712
-
a specific ECE-1 inhibitor. SM-191712 causes sustained ERK2 activation in cytosolic and nuclear fractions after substance P removal
SM-19712
-
ECE-1 inhibitor prevents endosomal substance P degardation. Thus, neurokinin 1 receptor (NK1R) recycling is suppressed by more than 50%
SM-19712
0.01 mM used in assay conditions
SM-19712
-
a specific ECE-1 inhibitor. SM-191712 causes sustained ERK2 activation in cytosolic and nuclear fractions after substance P removal
SM-19712
-
synthetic inhibitor, selective ECE-1 inhibitor
thiorphan
-
50% inhibition of native ECE-1, 70% inhibition of solECE-1
thiorphan
-
1 mM, inhibition of ECE-1 activity
additional information
-
leupeptin, chymostatin, pepstatin A, E-64, p-chloromercuriphenylsulfonic acid, N-ethylmaleimide or 4-amidinophenylmethyl sulfonylfluoride; no inhibition by thiorphan, captopril
-
additional information
-
enzyme activity unaffected by thiorphan
-
additional information
-
neither exogenously added ET-1 nor the blockade of the receptors with bosentan modifies ECE-1 protein, overview
-
additional information
-
little or no inhibition with captopril
-
additional information
-
not inhibited by thiorphan and captopril
-
additional information
-
acidification to pH 6.4 inhibits plasma membrane ECE activity
-
additional information
-
prevention of acidification of endosomes using bafilomycin A1 inhibits the degradation of internalized somatostatin-14
-
additional information
-
carbachol and phorbol 12-myristate 13-acetate reduce enzyme expression in neuroblastoma NB7 cells, only isozyme ECE-1c remains detectable, overview
-
additional information
-
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
-
additional information
-
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
-
additional information
-
phosphinic tripeptides as dual angiotensin-converting enzyme C-domain and endothelin-converting enzyme-1, while sparing neprilysin, inhibitors, overview
-
additional information
-
no inhibition by thiorphan and captopril
-
additional information
-
no inhibition by thiorphan, captopril
-
additional information
-
no inhibition by thiorphan, captopril
-
additional information
-
expression of ECE-1 is significantly reduced in the cortex of adult rats after 15 mins of global ischemia, and is also significantly reduced in the striatum of rats subjected to prenatal hypoxia
-
additional information
-
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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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 - 0.0011
CGS 26303
0.00062
CGS 26582
Sus scrofa
-
-
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
0.0035
N-(alpha-rhamnopyranosyloxyhydroxyphosphinyl)-Leu-Trp
Sus scrofa
-
potency varies with pH of medium
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
0.0000012
RO 67-7447
Rattus norvegicus
-
-
0.00008
SCH 54470
Cavia sp.
-
-
0.000042
SM-19712
Sus scrofa
-
in vitro result, in vivo potency is lower than expected compared to in vitro result
0.00014
WS-79089B
Bos taurus
-
-
0.00073
WS79089A
Bos taurus
-
-
0.00342
WS79089C
Bos taurus
-
-
0.0049
[Lys-Gly-His-Lys-Cu]+
Homo sapiens
-
metallopeptide, IC50: 0.0049 mM under hydrolytic condtions
0.000017
CGS 26303
Homo sapiens
-
optimized form of inhibitor, human recombinant ECE-1 overexpressed in CHO cells
0.0011
CGS 26303
Sus scrofa
-
long-active in vivo
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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Takahashi, M.; Matsushita, Y.; Iijima, Y.; Tanzawa, K.
Purification and characterization of endothelin-converting enzyme from rat lung
J. Biol. Chem.
268
21394-21398
1993
Rattus norvegicus
brenda
Shimada, K.; Takahashi, M.; Tanzawa, K.
Cloning and functional expression of endothelin-converting enzyme from rat endothelial cells
J. Biol. Chem.
269
18275-18278
1994
Rattus norvegicus
brenda
Xu, D.; Emoto, N.; Giaid, A.; Slaughter, C.; Kaw, S.; deWit, D.; Yanagisawa, M.
ECE-1: a membrane-bound metalloprotease that catalyzes the proteolytic activation of big endothelin-1
Cell
78
473-485
1994
Bos taurus
brenda
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
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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
Hasegawa, H.; Hiki, K.; Sawamura, T.; Aoyama, T.; Okamoto, Y.; Miwa, S.; Shimohama, S.; Kimura, J.; Masaki, T.
Purification of a novel endothelin-converting enzyme specific for big endothelin-3
FEBS Lett.
428
304-308
1998
Bos taurus
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
Raoch, V.; Martinez-Miguel, P.; Arribas-Gomez, I.; Rodriguez-Puyol, M.; Rodriguez-Puyol, D.; Lopez-Ongil, S.
The peptidase inhibitor CGS-26303 increases endothelin converting enzyme-1 expression in endothelial cells through accumulation of big endothelin-1
Br. J. Pharmacol.
152
313-322
2007
Bos taurus
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
Eckman, E.A.; Adams, S.K.; Troendle, F.J.; Stodola, B.A.; Kahn, M.A.; Fauq, A.H.; Xiao, H.D.; Bernstein, K.E.; Eckman, C.B.
Regulation of steady-state beta-amyloid levels in the brain by neprilysin and endothelin-converting enzyme but not angiotensin-converting enzyme
J. Biol. Chem.
281
30471-30478
2006
Mus musculus
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
Hyndman, K.A.; Evans, D.H.
Endothelin and endothelin converting enzyme-1 in the fish gill: evolutionary and physiological perspectives
J. Exp. Biol.
210
4286-4297
2007
Fundulus heteroclitus (A7LFV6), Fundulus heteroclitus
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
Khamaisi, M.; Raz, I.; Shilo, V.; Shina, A.; Rosenberger, C.; Dahan, R.; Abassi, Z.; Meidan, R.; Lecht, S.; Heyman, S.N.
Diabetes and radiocontrast media increase endothelin converting enzyme-1 in the kidney
Kidney Int.
74
91-100
2008
Rattus norvegicus
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
Khimji, A.K.; Shao, R.; Rockey, D.C.
Divergent transforming growth factor-beta signaling in hepatic stellate cells after liver injury: functional effects on ECE-1 regulation
Am. J. Pathol.
173
716-727
2008
Rattus norvegicus
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
Lee, S.; Carter, P.R.; Watts, M.N.; Bao, J.R.; Harris, N.R.
Effects of the endothelin-converting enzyme inhibitor SM-19712 in a mouse model of dextran sodium sulfate-induced colitis
Inflamm. Bowel Dis.
15
1007-1013
2009
Mus musculus, Mus musculus C57BL/6
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
Raoch, V.; Rodriguez-Pascual, F.; Lopez-Martinez, V.; Medrano-Andres, D.; Rodriguez-Puyol, M.; Lamas, S.; Rodriguez-Puyol, D.; Lopez-Ongil, S.
Nitric oxide decreases the expression of endothelin-converting enzyme-1 through mRNA destabilization
Arterioscler. Thromb. Vasc. Biol.
31
2577-2585
2011
Bos taurus
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
Pelayo, J.C.; Poole, D.P.; Steinhoff, M.; Cottrell, G.S.; Bunnett, N.W.
Endothelin-converting enzyme-1 regulates trafficking and signalling of the neurokinin 1 receptor in endosomes of myenteric neurones
J. Physiol.
589
5213-5230
2011
Mus musculus
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
Khamaisi, M.; Skarzinski, G.; Mekler, J.; Zreik, F.; Damouni, R.; Ariel, I.; Bursztyn, M.
Hyperinsulinemia increases placenta endothelin-converting enzyme-1 expression in trophoblasts
Am. J. Hypertens.
25
109-114
2012
Rattus norvegicus (P42893)
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
Heyman, S.N.; Abassi, Z.; Rosenberger, C.; Yaseen, H.; Skarjinski, G.; Shina, A.; Mathia, S.; Krits, N.; Khamaisi, M.
Cyclosporine A induces endothelin-converting enzyme-1 Studies invivo and invitro
Acta Physiol. (Oxf.)
223
e13033
2018
Rattus norvegicus (P42893)
brenda
Cho, T.J.; Kim, H.J.; Cho, J.
Endothelin-converting enzyme-1 expression in acute and chronic liver injury in fibrogenesis
Anim. Cells Sys.
23
170-175
2019
Rattus norvegicus (P42893)
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