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phosphoramidon

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Description

phosphoramidon: a membrane metallo-endopeptidase & endothelin-converting enzyme inhibitor; thermolysin inhibitor from culture filtrate of Streptomyces tanashiensis; structure [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

phosphoramidon : A dipeptide isolated from the cultures of Streptomyces tanashiensis. [Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Cross-References

ID SourceID
PubMed CID445114
CHEMBL ID479579
CHEBI ID45353
SCHEMBL ID40933
MeSH IDM0053135

Synonyms (48)

Synonym
RDF ,
n-alpha-l-rhamnopyranosyloxy(hydroxyphosphinyl)-l-leucyl-l-tryptophan
C00563
36357-77-4
phosphoramidon
DB02557
1TLP
l-tryptophan, n-(n-(((6-deoxy-alpha-l-mannopyranosyl)oxy)hydroxyphosphinyl)-l-leucyl)-
n-(n-(((6-deoxy-alpha-l-mannopyranosyl)oxy)hydroxyphosphinyl)-l-leucyl)-l-tryptophan
einecs 252-996-3
phosphoramidon disodium salt
2-{2-[hydroxy-(3,4,6-trihydroxy-5-methyl-tetrahydro-pyran-2-yloxy)-phosphorylamino]-4-methyl-pentanoylamino}-3-(1h-indol-3-yl)-propionic acid( phosphoramidon)
(s)-2-{(s)-2-[hydroxy-((2s,3r,4r,5r,6s)-3,4,5-trihydroxy-6-methyl-tetrahydro-pyran-2-yloxy)-phosphorylamino]-4-methyl-pentanoylamino}-3-(1h-indol-3-yl)-propionic acid
(3r,4r,5r,6s)-3,4,5-trihydroxy-6-methyl-tetrahydro-2h-pyran-2-yl hydrogen (s)-1-((s)-1-(1h-indol-3-yl)-3-oxobutan-2-ylamino)-4-methyl-1-oxopentan-2-ylphosphoramidate
(s)-2-{(s)-2-[hydroxy-(3,4,5-trihydroxy-6-methyl-tetrahydro-pyran-2-yloxy)-phosphorylamino]-4-methyl-1-oxo-pentylamino}-3-(1h-indol-3-yl)-propionic acid
(s)-3-(1-hydroxy-1h-indol-3-yl)-2-{(s)-2-[hydroxy-(3,4,5-trihydroxy-6-methyl-tetrahydro-pyran-2-yloxy)-phosphorylamino]-4-methyl-pentanoylamino}-propionic acid
(s)-2-{(s)-2-[hydroxy-(3,4,5-trihydroxy-6-methyl-tetrahydro-pyran-2-yloxy)-phosphorylamino]-4-methyl-pentanoylamino}-3-(1h-indol-3-yl)-propionic acid
(s)-2-{(s)-2-[hydroxy-((3r,4r,5r,6s)-3,4,5-trihydroxy-6-methyl-tetrahydro-pyran-2-yloxy)-phosphorylamino]-4-methyl-pentanoylamino}-3-(1h-indol-3-yl)-propionic acid
bdbm50251742
(2s)-2-[[(2s)-2-[[hydroxy-[(2s,3r,4r,5r,6s)-3,4,5-trihydroxy-6-methyloxan-2-yl]oxyphosphoryl]amino]-4-methylpentanoyl]amino]-3-(1h-indol-3-yl)propanoic acid
phosphramidon
chebi:45353 ,
phosporamidon
CHEMBL479579 ,
(s)-2-{(r)-2-[hydroxy-((2r,3r,4r,5r,6s)-3,4,5-trihydroxy-6-methyl-tetrahydro-pyran-2-yloxy)-phosphorylamino]-4-methyl-pentanoylamino}-3-(1h-indol-3-yl)-propionic acid
(phosphoramidon) 2-{2-[hydroxy-(3,4,5-trihydroxy-6-methyl-tetrahydro-pyran-2-yloxy)-phosphorylamino]-4-methyl-pentanoylamino}-3-(1h-indol-3-yl)-propionic acid
2-{2-[hydroxy-(3,4,5-trihydroxy-6-methyl-tetrahydro-pyran-2-yloxy)-phosphorylamino]-4-methyl-pentanoylamino}-3-(1h-indol-3-yl)-propionic acid
t3g94e2lb1 ,
unii-t3g94e2lb1
SCHEMBL40933
n-(alpha-l-rhamnopyranosyloxyhydroxyphosphinyl)-l-leucyl-l-tryptophan
n-(hydroxy{[(2s,3r,4r,5r,6s)-3,4,5-trihydroxy-6-methyltetrahydro-2h-pyran-2-yl]oxy}phosphoryl)-l-leucyl-l-tryptophan
(2s)-2-{[(2s)-2-{[(s)-hydroxy{[(2s,3r,4r,5r,6s)-3,4,5-trihydroxy-6-methyltetrahydro-2h-pyran-2-yl]oxy}phosphoryl]amino}-4-methylpentanoyl]amino}-3-(1h-indol-3-yl)propanoic acid (non-preferred name)
l-tryptophan, n-(((6-deoxy-.alpha.-l-mannopyranosyl)oxy)hydroxyphosphinyl)-l-leucyl-
l-tryptophan, n-(n-(((6-deoxy-.alpha.-l-mannopyranosyl)oxy)hydroxyphosphinyl)-l-leucyl)-
(2s)-2-[[(2s)-2-[[hydroxy-[(2s,3r,4r,5r,6s)-3,4,5-trihydroxy-6-methyl-tetrahydropyran-2-yl]oxy-phosphoryl]amino]-4-methyl-pentanoyl]amino]-3-(1h-indol-3-yl)propanoic acid
l-tryptophan,n-[[(6-deoxy-a-l-mannopyranosyl)oxy]hydroxyphosphinyl]-l-leucyl-
ZPHBZEQOLSRPAK-XLCYBJAPSA-N
(2s)-2-{[(2s)-2-{[(s)-hydroxy{[(2s,3r,4r,5r,6s)-3,4,5-trihydroxy-6-methyltetrahydro-2h-pyran-2-yl]oxy}phosphoryl]amino}-4-methylpentanoyl]amino}-3-(1h-indol-3-yl)propanoic acid
(hydroxy(((2s,3r,4r,5r,6s)-3,4,5-trihydroxy-6-methyltetrahydro-2h-pyran-2-yl)oxy)phosphoryl)-l-leucyl-l-tryptophan
(2s)-2-((2s)-2-((hydroxy(((2s,3r,4r,5r,6s)-3,4,5-trihydroxy-6-methyltetrahydro-2h-pyran-2-yl)oxy)phosphoryl)amino)-4-methylpentanamido)-3-(1h-indol-3-yl)propanoic acid
Q7187544
gtpl11653
HY-N2021
CS-0018379
DTXSID601317292
(2s)-2-((2s)-2-((hydroxy(((2s,3r,4r,5r,6s)-3,4,5-trihydroxy-6-methyltetrahydro-2h-pyran-2-yl)oxy)phosphoryl)amino)-4-methylpentanamido)-3-(1h-indol-3-yl)propanoicacid
AKOS040744615

Research Excerpts

Overview

Phosphoramidon is an unspecific proteinase inhibitor. It is also known to be an enkephalinase inhibitors.

ExcerptReferenceRelevance
"Phosphoramidon is an unspecific proteinase inhibitor."( A proteinase inhibitor decreases tumor growth in a laparoscopic rat model.
Günther, T; Halangk, W; Krüger, S; Lippert, H; Mantke, R; Marusch, F; Pross, M; Schulz, HU, 2001
)
1.03
"Phosphoramidon is known to be an enkephalinase inhibitor."( [Effect of enkephalinase inhibitor on endothelin-1 induced bronchoconstriction in guinea pigs].
Endoh, T; Hamada, M; Hasegawa, S; Kameyama, M; Ninomiya, H; Nomura, A; Ohse, H; Saotome, M; Uchida, Y; Watanabe, A, 1992
)
1

Effects

ExcerptReferenceRelevance
"Phosphoramidon, which has been shown to block in vivo conversion of exogenous big ET to ET, was unable to prevent endotoxin-induced increases in ir-ET.(ABSTRACT TRUNCATED AT 250 WORDS)"( Stimulation of endogenous endothelin release in the anesthetized rat.
Divish, BJ; Opgenorth, TJ; Pollock, DM, 1993
)
1.01

Actions

ExcerptReferenceRelevance
"Phosphoramidon tended to increase the potency and delayed the termination of post-tetanic twitch inhibition."( Effect of some peptidase inhibitors on exogenous and endogenous opioid actions in guinea-pig ileum.
Kishioka, S; Masuda, Y; Miyamoto, Y; Ozaki, M; Yamamoto, H, 1994
)
1.01

Treatment

Pretreatment with phosphoramidon (10 mg kg-kg) significantly attenuated the proET-1-induced increase in blood flow to the heart, brain, kidneys, portal system, and GIT. The difference in responsiveness to substance P between the intact and denuded tissues was reduced from 148-fold to 18-fold.

ExcerptReferenceRelevance
"Phosphoramidon-treated CD1 mice survived the acute infection."( Cardioprotective effects of phosphoramidon on myocardial structure and function in murine Chagas' disease.
Bouzahzah, B; Chandra, M; Christ, GJ; D'Orleans-Juste, P; Douglas, SA; Factor, SM; Huang, H; Jelicks, LA; Loredo, ML; Mukherjee, S; Petkova, SB; Shirani, J; Shtutin, V; Tang, B; Tanowitz, HB; Teixeira, MM; Weiss, LM; Wittner, M, 2002
)
1.33
"Phosphoramidon pretreatment significantly attenuated the proET-1-induced increase in blood flow to the heart, brain, kidneys, portal system, and GIT."( Role of endothelin-converting enzyme in the systemic hemodynamics and regional circulatory effects of proendothelin-1 (1-38) and diaspirin cross-linked hemoglobin in rats.
Chung, SM; Gulati, A; Sen, AP; Singh, R, 1995
)
1.01
"Phosphoramidon pretreatment had no effect on the acidosis.5."( A role for endothelin in bicuculline-induced neurogenic pulmonary oedema in rats.
Herbst, C; Shams, H; Simmet, T; Tippler, B, 1995
)
1.01
"In phosphoramidon-treated guinea pigs, ET-1 (5 micrograms/ml) exposure for 30 min evoked a slight but non-significant enhancement of the ACh-induced BR."( Endothelin-1 and bronchial hyperresponsiveness in the guinea pig.
Boichot, E; Braquet, P; Carre, C; Lagente, V; Mencia-Huerta, JM; Pons, F, 1991
)
0.8
"With phosphoramidon treatment, therefore, the difference in responsiveness to substance P between the intact and denuded tissues was reduced from 148-fold to 18-fold."( Epithelium removal alters responsiveness of guinea pig trachea to substance P.
Fine, JM; Gordon, T; Sheppard, D, 1989
)
0.73
"Phosphoramidon-treated animals were more reactive to dry gas hyperpnea compared with control (ES200 = 2.6 ml; P less than 0.0001)."( Tachykinins mediate bronchoconstriction elicited by isocapnic hyperpnea in guinea pigs.
Drazen, JM; Hernandez, C; Leff, AR; Ray, DW; Solway, J, 1989
)
1
"Rats treated with phosphoramidon (an enkephalinase-inhibitor 250 micrograms, i.c.v.), morphine (20 micrograms i.c.v.) or subjected to cold-water-swim (CWS, animals forced to swim in water at 5 degrees C for 5 min) showed consistent analgesia. "( REM sleep deprivation decreases the antinociceptive property of enkephalinase-inhibition, morphine and cold-water-swim.
Dzoljic, MR; Rupreht, J; Ukponmwan, OE, 1984
)
0.6
"Pretreatment with phosphoramidon (10 mg/kg + 0.25 mg/kg/min) completely abolished the increase in blood pressure induced by BET, but the diuretic-natriuretic effects were only partially inhibited (FENa increased from 2.0 +/- 0.9 to 3.7 +/- 1.5, 3.9 +/- 1.3, and 4.3 +/- 1.2%, respectively, P < 0.05)."( Diuretic-natriuretic actions and pressor effects of big-endothelin (1-39) in phosphoramidon-treated rats.
Dalal, I; Haramati, A; Hoffman, A; Shuranyi, E; Winaver, J, 1994
)
0.84
"Pretreatment with phosphoramidon (10(-4) M), a metalloproteinase inhibitor, markedly suppressed the pressor action and increment in IR-ET in the tissues."( Conversion of big ET-1 in the rat lung: role of phosphoramidon-sensitive endothelin-1-converting enzyme.
Fujita, K; Hisaki, K; Maekawa, H; Matsumura, Y; Morimoto, S; Takaoka, M, 1994
)
0.87
"Pretreatment with phosphoramidon (10 mg kg-1, i.v.) did not affect the big ET-1-induced change in plasma IR-ET-1, while significant delay of the disappearance of plasma IR-rANP and significant suppression of a sustained increase in tissue IR-ET-1 were observed."( Comparison of haemoconcentration induced by big endothelin-1 and endothelin-1 in mice.
Arai, K; Asakura, R; Ashikawa, N; Ashizawa, N; Kobayashi, F; Matsuura, A; Okumura, H, 1993
)
0.61
"Treatment with phosphoramidon (1 mM) for 45 min decreased the release of ir-ET by 73% and 76% in 6- and 10-h incubation periods, respectively."( Dexamethasone and phosphoramidon inhibit endothelin release by cultured nonciliated bronchiolar epithelial (Clara) cells.
D'Orléans-Juste, P; Laporte, J; Singh, G; Sirois, P, 1995
)
0.96
"3. Treatment with phosphoramidon did not alter the increase in the lateral pressure at the tracheal tube (Pao) caused by OA inhalation or the increase in bronchial response to methacholine following the allergic reaction."( Involvement of NK2 receptors rather than NK1 receptors in bronchial hyperresponsiveness induced by allergic reaction in guinea-pigs.
Amemiya, T; Fujimura, M; Matsuda, T; Mizuguchi, M; Nishi, K; Ohka, T, 1996
)
0.62
"Pretreatment with phosphoramidon (10(-5) M) significantly increased the number of coughs caused by substance P and capsaicin."( Inhalation of phosphoramidon, a neutral endopeptidase inhibitor, induces cough in awake guinea-pigs.
Fuchikami, J; Isohama, Y; Kai, H; Miyata, T; Takahama, K,
)
0.82
"Pre-treatment with phosphoramidon (1 micron) an ECE-inhibitor, followed by TNF-alpha stimulation, decreased ir-ET-1 levels."( Regulation of endothelin-1 in human non-pigmented ciliary epithelial cells by tumor necrosis factor-alpha.
Dibas, A; Prasanna, G; Tao, W; White, K; Yorio, T, 1998
)
0.62
"Pretreatment with phosphoramidon [an inhibitor of neutral endopeptidase (NEP); 2 mg/kg], which suppresses the degradation of tachykinins, induced an increase in airway reactivity that largely mimicked this SIAHR."( Smoke-induced airway hyperresponsiveness to inhaled wood smoke in guinea pigs: tachykininergic and cholinergic mechanisms.
Hsu, TH; Kou, YR; Lai, YL, 1998
)
0.62
"Pretreatment with phosphoramidon, an NEP inhibitor, also enhanced SP- and ET-1-induced bronchoconstriction."( Administration of SIN-1 induces guinea pig airway hyperresponsiveness through inactivation of airway neutral endopeptidase.
Hirata, K; Kanazawa, H; Yoshikawa, J, 1999
)
0.63
"Pretreatment with phosphoramidon produced dose-dependent reduction in the extent of mucosal damage caused by indomethacin, accompanied by a significant recovery in the expression of cNOS, and a marked decline in ECE-1, epithelial cell apoptosis and the mucosal level of ET-1."( Role of endothelin-converting enzyme-1 in the suppression of constitutive nitric oxide synthase in rat gastric mucosal injury by indomethacin.
Slomiany, A; Slomiany, BL, 2000
)
0.63
"Pretreatment with phosphoramidon (PA) blocked the response to big-ET-1 in all tissues examined but this inhibitor failed to alter the response to ET-1."( Phosphoramidon blocks big-endothelin-1 but not endothelin-1 enhancement of vascular permeability in the rat.
D'Orléans-Juste, P; Lehoux, S; Plante, GE; Sirois, MG; Sirois, P, 1992
)
2.05
"Pretreatment with phosphoramidon, a metalloprotease inhibitor (90 nmol), abolished the hemodynamic responses elicited by BigET-1 (MAP = -9 +/- 2%; RBF = -3 +/- 2%) but not those produced by ET-1."( Functional evidence for the presence of a phosphoramidon-sensitive enzyme in rat brain that converts big endothelin-1 to endothelin-1.
Hashim, MA; Tadepalli, AS, 1991
)
0.87

Pharmacokinetics

ExcerptReferenceRelevance
" These results suggest that clearance receptor is involved in the clearance of the physiological levels of alpha-rANP and that NEP plays a major role in the clearance of a pharmacological dose of alpha-rANP, at which clearance receptors are thought to be saturated, and also indicate a pharmacokinetic difference between alpha-rANP and rBNP."( Clearance mechanisms of atrial and brain natriuretic peptides in rats.
Hama, N; Hashimoto, Y; Hori, R; Imura, H; Mori, S; Nakao, K; Yamaguchi, M; Yasuhara, M, 1994
)
0.29
" The population analysis was useful for analyzing such pharmacodynamic data for which the individual analysis could not be applied easily."( Nonlinear mixed effect modeling of the pharmacodynamics of natriuretic peptides in rats.
Hama, N; Hashimoto, Y; Hori, R; Imura, H; Mori, S; Nakao, K; Yamaguchi, M; Yasuhara, M, 1993
)
0.29
" Acute inhibition of both ETA and ETB receptors with bosentan dramatically prolonged 125I-ET-1 plasma half-life and shifted tissue uptake from lung to liver and kidneys."( Receptor- and non-receptor-mediated clearance of big-endothelin and endothelin-1: differential effects of acute and chronic ETA receptor blockade.
Barton, M; Burkhardt, M; Shaw, SG, 2000
)
0.31

Compound-Compound Interactions

ExcerptReferenceRelevance
"The application of reversed-phase HPLC in combination with micro-electrospray mass spectrometry to study a substance P (SP)-hydrolysing endoprotease in human cerebrospinal fluid (hCSF) is reported."( Reversed-phase high-performance liquid chromatography combined with tandem mass spectrometry in studies of a substance P-converting enzyme from human cerebrospinal fluid.
Andrén, PE; Caprioli, RM; Eriksson, U; Nyberg, F, 1996
)
0.29

Bioavailability

ExcerptReferenceRelevance
" Hence, the bioavailability of h-pro-ET-1, p-pro-ET-1 and pro-ET-2, assessed on the basis of these two parameters, was approximately 50% of that of their corresponding ET, whereas the bioavailability of pro-ET-3 was only 25% that of ET-3."( Differential inhibition of the pressor effects of natural pro-endothelins by phosphoramidon in rats.
Cavero, I; Le Monnier de Gouville, AC; Thiry, C, 1994
)
0.52
" We hypothesized that the in vivo coadministration of specific enzyme inhibitors would improve peptide bioavailability and hence tumor uptake."( "To serve and protect": enzyme inhibitors as radiopeptide escorts promote tumor targeting.
de Jong, M; Krenning, EP; Maina, T; Nock, BA, 2014
)
0.4
" Coinjection of the NEP inhibitor phosphoramidon (PA) with radiolabeled gastrin and other peptide analogs has been recently proposed as a new promising strategy to increase bioavailability and tumor-localization of radiopeptides in tumor sites."( Radiolabeled gastrin/CCK analogs in tumor diagnosis: towards higher stability and improved tumor targeting.
De Jong, M; Kaloudi, A; Krenning, EP; Maina, T; Nock, BA, 2015
)
0.7
" On the other hand, truncated des(Glu)(2-6)-analogs, such as [(111)In-DOTA]MG11 ([(111)In-DOTA-DGlu(10),desGlu(2-6)]minigastrin), despite their low renal uptake, show poor bioavailability and tumor targeting."( Improving the In Vivo Profile of Minigastrin Radiotracers: A Comparative Study Involving the Neutral Endopeptidase Inhibitor Phosphoramidon.
de Jong, M; Kaloudi, A; Krenning, EP; Lymperis, E; Maina, T; Nock, BA, 2016
)
0.64

Dosage Studied

The neutral endopeptidase inhibitor phosphoramidon (10(-5) M) potentiated the effect of VIP, so that the CBF dose-response curve for VIP was shifted to lower concentrations by 0.05%. Addition of the CD10 inhibitor, phosphor amidon, together with IL-1 beta resulted in a left shift in the dose- response curve which corresponded to a 10-fold potentiation of the IL- 1 beta effect.

ExcerptRelevanceReference
" Evaluation of chemotaxis demonstrated that cord blood neutrophils exhibited a shift in the fMLP dose-response relationship showing relatively better chemotaxis to lower concentrations."( Effect of low neutral endopeptidase expression on response to fMLP.
Basford, RE; Kaplan, SS; Park, J; Penchansky, L; Zdziarski, UE, 1992
)
0.28
" The effective dose of substance P (in micrograms) that produced a doubling of baseline specific airway resistance (ED200SP) was determined by interpolation of cumulative substance P dose-response curves."( Aerosolized neutral endopeptidase reverses ozone-induced airway hyperreactivity to substance P.
Chodimella, V; Lang, Z; Murlas, CG; Williams, GJ, 1992
)
0.28
" Dose-response curves to ET-1 with or without phosphoramidon were obtained."( [Effect of enkephalinase inhibitor on endothelin-1 induced bronchoconstriction in guinea pigs].
Endoh, T; Hamada, M; Hasegawa, S; Kameyama, M; Ninomiya, H; Nomura, A; Ohse, H; Saotome, M; Uchida, Y; Watanabe, A, 1992
)
0.54
" Phosphoramidon (10(-7) to 10(-5) M) potentiated the substance P-induced contraction in a dose-dependent fashion, and phosphoramidon shifted the dose-response curve to lower concentrations."( Enkephalinase inhibitor potentiates substance P- and capsaicin-induced bronchial smooth muscle contractions in humans.
Ando, M; Araki, S; Honda, I; Kohrogi, H; Yamaguchi, T, 1991
)
1.19
" However, phosphoramidon caused a significantly greater leftward shift of the substance P dose-response curve in air-exposed animals than it did in TDI-exposed animals, so that after phosphoramidon, mean values of PD200 in animals exposed to air or TDI did not differ."( Toluene diisocyanate increases airway responsiveness to substance P and decreases airway neutral endopeptidase.
Borson, DB; Dusser, D; Nadel, JA; Scypinski, L; Sheppard, D; Thompson, JE, 1988
)
0.68
" The dose-response curve to methacholine was significantly shifted to the right by atropine."( Lateral nasal gland secretion in the anesthetized ferret.
Mizoguchi, H; Widdicombe, JG, 1989
)
0.28
" Methacholine dose-response curves (10(-11) to 10(-7) mol iv) obtained at the conclusion of the experiments were similar among capsaicin, phosphoramidon, and control groups."( Tachykinins mediate bronchoconstriction elicited by isocapnic hyperpnea in guinea pigs.
Drazen, JM; Hernandez, C; Leff, AR; Ray, DW; Solway, J, 1989
)
0.48
" Neither phosphoramidon nor the synthetic substrates altered the dose-response characteristics of the postsynaptic membrane to bath-applied carbachol."( Protease inhibitors implicate metalloendoprotease in synaptic transmission at the mammalian neuromuscular junction.
Baxter, DA; Johnston, D; Strittmatter, WJ, 1983
)
0.68
" Dose-response curves to methacholine were constructed before and 1 h after intratracheal instillation of poly-L-lysine in anaesthetized spontaneously breathing rats, and the concentration of methacholine required to induce a doubling in total lung resistance was calculated."( Cationic protein-induced sensory nerve activation: role of substance P in airway hyperresponsiveness and plasma protein extravasation.
Coyle, AJ; Irvin, CG; Manzini, S; Perretti, F, 1994
)
0.29
" The sodium salt of WS79089B (FR901533) inhibited big endothelin-1 (big ET-1) induced pressor effect in a dose dependent manner when administered to male Sprague-Dawley rats intravenously dosed 2 minutes prior to big ET-1 challenge."( Biological and pharmacological properties of highly selective new endothelin converting enzyme inhibitor WS79089B isolated from Streptosporangium roseum No. 79089.
Fujie, K; Kiyoto, S; Nishikawa, M; Okuhara, M; Tsurumi, Y, 1995
)
0.29
" Addition of the CD10 inhibitor, phosphoramidon, together with IL-1 beta resulted in a left shift in the dose-response curve which corresponded to a 10-fold potentiation of the IL-1 beta effect."( A function of CD10 on bone marrow stroma.
Delikat, SE; Galvani, DW; Zuzel, M, 1994
)
0.57
" In this study we determined the dose-response relationship for this action in SHRs and in a high-renin hypertensive model, the renal artery-ligated rat."( Effect of phosphoramidon (endothelin converting enzyme inhibitor) and BQ-123 (endothelin receptor subtype A antagonist) on blood pressure in hypertensive rats.
Bertenshaw, SR; Brown, MA; Carter, JS; McMahon, EG; Palomo, MA, 1993
)
0.69
" The present study was designed to examine the relationship between the dosing (intravenous constant infusion) rates and the diuretic actions of alpha-rat atrial natriuretic peptide (alpha-rANP) and rat brain natriuretic peptide (rBNP) in rats, and population (nonlinear mixed effect model) analysis was applied to these complicated diuretic actions."( Nonlinear mixed effect modeling of the pharmacodynamics of natriuretic peptides in rats.
Hama, N; Hashimoto, Y; Hori, R; Imura, H; Mori, S; Nakao, K; Yamaguchi, M; Yasuhara, M, 1993
)
0.29
" FK224 (10(-6) M and 10(-5) M, respectively) significantly inhibited NKA-induced contraction and 10(-5) M FK224 shifted the dose-response curve to more than one log unit higher concentration."( Tachykinin antagonist FK224 inhibits neurokinin A-, substance P- and capsaicin-induced human bronchial contraction.
Ando, M; Fujii, K; Goto, E; Hamamoto, J; Hirata, N; Honda, I; Iwagoe, H; Kohrogi, H; Yamaguchi, T, 1997
)
0.3
" Twenty-four sheep were actively sensitized to Ascaris suum, then challenged with nebulized Ascaris extract in a dose-response fashion."( Tachykinins contribute to the acute airways response to allergen in sheep actively sensitized to Ascaris suum.
Holmes, MD; Reynolds, AM; Reynolds, PN; Rice, AJ; Scicchitano, R; Thornton, AT, 1997
)
0.3
" Nasal inoculation with Mycoplasma pneumoniae potentiated contractile responses to neurokinin A and bradykinin, causing a leftward shift of the dose-response curves to a lower concentration by 1 log unit for each agonist, whereas there was no response with acetylcholine."( Airway hyper-responsiveness to neurokinin A and bradykinin following Mycoplasma pneumoniae infection associated with reduced epithelial neutral endopeptidase.
Araake, M; Chiyotani, A; Nagai, A; Tagaya, E; Tamaoki, J, 1998
)
0.3
" BQ123 (1 microm) caused a rightward shift in the ET-1 dose-response curve, while indomethacin at a threshold concentration (28 nm) tended to have an opposite effect."( Endothelin-induced constriction of the ductus venosus in fetal sheep: developmental aspects and possible interaction with vasodilatory prostaglandin.
Adeagbo, AS; Coceani, F; Kelsey, L, 2004
)
0.32
" The dose-response curve for ET-1 was shifted to the left in the diabetics, so that at some lower doses of ET-1 the vasoconstriction was greater than in the controls."( Diabetes-associated changes and role of N epsilon-(carboxymethyl)lysine in big ET-1-induced coronary vasoconstriction.
Kamata, K; Kobayashi, T; Matsumoto, T; Ozawa, Y; Taguchi, K, 2010
)
0.36
" Effects of PIs on antinociception were evaluated by dose-response study (ME, 1-20 nmol; PIs, 1-20 nmol each), by comparison of differences among two combinations of PIs (amastatin and captopril; captopril and phosphoramidon; amastatin and phosphoramidon) and three PIs (amastatin, captopril, and phosphoramidon), and by using opioid receptor selective antagonists."( Potentiation of [Met5]enkephalin-induced antinociception by mixture of three peptidase inhibitors in rat.
Kawaguchi, M; Kobayashi, H; Murata, T; Suzuki, T; Takahashi, S; Watanabe, M; Yoshikawa, M, 2014
)
0.59
" The effects of the PIs on antinociception and toxicity were evaluated by a dose-response study and a comparison of differences among various combinations of Dyn A (1-17) or Dyn A (1-13) and the three PIs and p-hydroxymercuribenzoate."( Effect of three peptidase inhibitors on antinociceptive potential and toxicity with intracerebroventricular administration of dynorphin A (1-17) or (1-13) in the rat.
Ajimi, J; Kawaguchi, M; Kobayashi, H; Miura, M; Suzuki, T; Takahashi, S; Tsukamoto, H; Yoshikawa, M, 2015
)
0.42
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Roles (3)

RoleDescription
bacterial metaboliteAny prokaryotic metabolite produced during a metabolic reaction in bacteria.
EC 3.4.24.11 (neprilysin) inhibitorAn EC 3.4.24.* (metalloendopeptidase) inhibitor that interferes with the action of neprilysin (EC 3.4.24.11).
EC 3.4.24.71 (endothelin-converting enzyme 1) inhibitorAn EC 3.4.24.* (metalloendopeptidase) inhibitor that interferes with the action of endothelin-converting enzyme 1 (EC 3.4.24.71).
[role information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Drug Classes (2)

ClassDescription
deoxyaldohexose phosphate
dipeptideAny molecule that contains two amino-acid residues connected by peptide linkages.
[compound class information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Protein Targets (10)

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Chain E, THERMOLYSINBacillus thermoproteolyticusKi0.02800.02800.02800.0280AID977610
Chain E, ThermolysinBacillus thermoproteolyticusKi0.02800.02800.02800.0280AID977610
ThermolysinBacillus thermoproteolyticusIC50 (µMol)0.03300.00301.93259.5000AID213074
ThermolysinBacillus thermoproteolyticusKi0.02800.01151.14192.2909AID213070
NeprilysinRattus norvegicus (Norway rat)IC50 (µMol)0.05780.00100.17022.3000AID143636; AID147352; AID147354; AID147364; AID147365; AID1607328
NeprilysinRattus norvegicus (Norway rat)Ki0.00400.00170.01520.0400AID67359
NeprilysinOryctolagus cuniculus (rabbit)IC50 (µMol)0.00280.00040.66118.2000AID147212; AID147213; AID67345
NeprilysinHomo sapiens (human)IC50 (µMol)0.04050.00020.54226.7000AID147073; AID147365; AID444547; AID620439
EEF1AKMT4-ECE2 readthrough transcript proteinHomo sapiens (human)Ki0.00120.00120.09810.1950AID1799789
Angiotensin-converting enzyme Homo sapiens (human)IC50 (µMol)0.61500.00010.533610.0000AID444547; AID444548
Endothelin-converting enzyme 1Homo sapiens (human)IC50 (µMol)1.06950.01200.56782.0000AID228593; AID241703; AID433787; AID444548; AID67184; AID67199
P2Y purinoceptor 12Homo sapiens (human)IC50 (µMol)0.01700.00041.048910.0000AID433787
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (116)

Processvia Protein(s)Taxonomy
kidney developmentNeprilysinHomo sapiens (human)
placenta developmentNeprilysinHomo sapiens (human)
proteolysisNeprilysinHomo sapiens (human)
peptide metabolic processNeprilysinHomo sapiens (human)
learning or memoryNeprilysinHomo sapiens (human)
substance P catabolic processNeprilysinHomo sapiens (human)
bradykinin catabolic processNeprilysinHomo sapiens (human)
sensory perception of painNeprilysinHomo sapiens (human)
protein catabolic processNeprilysinHomo sapiens (human)
lung developmentNeprilysinHomo sapiens (human)
hormone catabolic processNeprilysinHomo sapiens (human)
response to estrogenNeprilysinHomo sapiens (human)
creatinine metabolic processNeprilysinHomo sapiens (human)
amyloid-beta metabolic processNeprilysinHomo sapiens (human)
positive regulation of neurogenesisNeprilysinHomo sapiens (human)
neuropeptide processingNeprilysinHomo sapiens (human)
cellular response to cytokine stimulusNeprilysinHomo sapiens (human)
cellular response to UV-ANeprilysinHomo sapiens (human)
cellular response to UV-BNeprilysinHomo sapiens (human)
replicative senescenceNeprilysinHomo sapiens (human)
amyloid-beta clearanceNeprilysinHomo sapiens (human)
amyloid-beta clearance by cellular catabolic processNeprilysinHomo sapiens (human)
positive regulation of long-term synaptic potentiationNeprilysinHomo sapiens (human)
protein processingNeprilysinHomo sapiens (human)
brain developmentEEF1AKMT4-ECE2 readthrough transcript proteinHomo sapiens (human)
heart developmentEEF1AKMT4-ECE2 readthrough transcript proteinHomo sapiens (human)
cardioblast differentiationEEF1AKMT4-ECE2 readthrough transcript proteinHomo sapiens (human)
methylationEEF1AKMT4-ECE2 readthrough transcript proteinHomo sapiens (human)
protein processingEEF1AKMT4-ECE2 readthrough transcript proteinHomo sapiens (human)
response to hypoxiaAngiotensin-converting enzyme Homo sapiens (human)
kidney developmentAngiotensin-converting enzyme Homo sapiens (human)
blood vessel remodelingAngiotensin-converting enzyme Homo sapiens (human)
angiotensin maturationAngiotensin-converting enzyme Homo sapiens (human)
regulation of renal output by angiotensinAngiotensin-converting enzyme Homo sapiens (human)
neutrophil mediated immunityAngiotensin-converting enzyme Homo sapiens (human)
antigen processing and presentation of peptide antigen via MHC class IAngiotensin-converting enzyme Homo sapiens (human)
regulation of systemic arterial blood pressure by renin-angiotensinAngiotensin-converting enzyme Homo sapiens (human)
proteolysisAngiotensin-converting enzyme Homo sapiens (human)
spermatogenesisAngiotensin-converting enzyme Homo sapiens (human)
female pregnancyAngiotensin-converting enzyme Homo sapiens (human)
regulation of blood pressureAngiotensin-converting enzyme Homo sapiens (human)
male gonad developmentAngiotensin-converting enzyme Homo sapiens (human)
response to xenobiotic stimulusAngiotensin-converting enzyme Homo sapiens (human)
embryo development ending in birth or egg hatchingAngiotensin-converting enzyme Homo sapiens (human)
post-transcriptional regulation of gene expressionAngiotensin-converting enzyme Homo sapiens (human)
negative regulation of gene expressionAngiotensin-converting enzyme Homo sapiens (human)
substance P catabolic processAngiotensin-converting enzyme Homo sapiens (human)
bradykinin catabolic processAngiotensin-converting enzyme Homo sapiens (human)
regulation of smooth muscle cell migrationAngiotensin-converting enzyme Homo sapiens (human)
regulation of vasoconstrictionAngiotensin-converting enzyme Homo sapiens (human)
animal organ regenerationAngiotensin-converting enzyme Homo sapiens (human)
response to nutrient levelsAngiotensin-converting enzyme Homo sapiens (human)
response to lipopolysaccharideAngiotensin-converting enzyme Homo sapiens (human)
mononuclear cell proliferationAngiotensin-converting enzyme Homo sapiens (human)
response to laminar fluid shear stressAngiotensin-converting enzyme Homo sapiens (human)
angiotensin-activated signaling pathwayAngiotensin-converting enzyme Homo sapiens (human)
vasoconstrictionAngiotensin-converting enzyme Homo sapiens (human)
hormone metabolic processAngiotensin-converting enzyme Homo sapiens (human)
hormone catabolic processAngiotensin-converting enzyme Homo sapiens (human)
eating behaviorAngiotensin-converting enzyme Homo sapiens (human)
positive regulation of apoptotic processAngiotensin-converting enzyme Homo sapiens (human)
peptide catabolic processAngiotensin-converting enzyme Homo sapiens (human)
positive regulation of vasoconstrictionAngiotensin-converting enzyme Homo sapiens (human)
negative regulation of glucose importAngiotensin-converting enzyme Homo sapiens (human)
regulation of synaptic plasticityAngiotensin-converting enzyme Homo sapiens (human)
lung alveolus developmentAngiotensin-converting enzyme Homo sapiens (human)
amyloid-beta metabolic processAngiotensin-converting enzyme Homo sapiens (human)
arachidonic acid secretionAngiotensin-converting enzyme Homo sapiens (human)
positive regulation of neurogenesisAngiotensin-converting enzyme Homo sapiens (human)
heart contractionAngiotensin-converting enzyme Homo sapiens (human)
regulation of angiotensin metabolic processAngiotensin-converting enzyme Homo sapiens (human)
hematopoietic stem cell differentiationAngiotensin-converting enzyme Homo sapiens (human)
angiogenesis involved in coronary vascular morphogenesisAngiotensin-converting enzyme Homo sapiens (human)
cellular response to glucose stimulusAngiotensin-converting enzyme Homo sapiens (human)
response to dexamethasoneAngiotensin-converting enzyme Homo sapiens (human)
cell proliferation in bone marrowAngiotensin-converting enzyme Homo sapiens (human)
regulation of heart rate by cardiac conductionAngiotensin-converting enzyme Homo sapiens (human)
negative regulation of calcium ion importAngiotensin-converting enzyme Homo sapiens (human)
response to thyroid hormoneAngiotensin-converting enzyme Homo sapiens (human)
blood vessel diameter maintenanceAngiotensin-converting enzyme Homo sapiens (human)
regulation of hematopoietic stem cell proliferationAngiotensin-converting enzyme Homo sapiens (human)
negative regulation of gap junction assemblyAngiotensin-converting enzyme Homo sapiens (human)
cellular response to aldosteroneAngiotensin-converting enzyme Homo sapiens (human)
positive regulation of peptidyl-cysteine S-nitrosylationAngiotensin-converting enzyme Homo sapiens (human)
positive regulation of systemic arterial blood pressureAngiotensin-converting enzyme Homo sapiens (human)
positive regulation of receptor recyclingEndothelin-converting enzyme 1Homo sapiens (human)
regulation of systemic arterial blood pressure by endothelinEndothelin-converting enzyme 1Homo sapiens (human)
G protein-coupled receptor signaling pathwayEndothelin-converting enzyme 1Homo sapiens (human)
heart developmentEndothelin-converting enzyme 1Homo sapiens (human)
substance P catabolic processEndothelin-converting enzyme 1Homo sapiens (human)
bradykinin catabolic processEndothelin-converting enzyme 1Homo sapiens (human)
calcitonin catabolic processEndothelin-converting enzyme 1Homo sapiens (human)
protein processingEndothelin-converting enzyme 1Homo sapiens (human)
peptide hormone processingEndothelin-converting enzyme 1Homo sapiens (human)
regulation of vasoconstrictionEndothelin-converting enzyme 1Homo sapiens (human)
endothelin maturationEndothelin-converting enzyme 1Homo sapiens (human)
embryonic heart tube developmentEndothelin-converting enzyme 1Homo sapiens (human)
hormone catabolic processEndothelin-converting enzyme 1Homo sapiens (human)
embryonic digit morphogenesisEndothelin-converting enzyme 1Homo sapiens (human)
ear developmentEndothelin-converting enzyme 1Homo sapiens (human)
pharyngeal system developmentEndothelin-converting enzyme 1Homo sapiens (human)
axonogenesis involved in innervationEndothelin-converting enzyme 1Homo sapiens (human)
sympathetic neuron axon guidanceEndothelin-converting enzyme 1Homo sapiens (human)
semaphorin-plexin signaling pathway involved in axon guidanceEndothelin-converting enzyme 1Homo sapiens (human)
G protein-coupled adenosine receptor signaling pathwayP2Y purinoceptor 12Homo sapiens (human)
monoatomic ion transportP2Y purinoceptor 12Homo sapiens (human)
substrate-dependent cell migration, cell extensionP2Y purinoceptor 12Homo sapiens (human)
G protein-coupled receptor signaling pathwayP2Y purinoceptor 12Homo sapiens (human)
adenylate cyclase-inhibiting G protein-coupled receptor signaling pathwayP2Y purinoceptor 12Homo sapiens (human)
phospholipase C-activating G protein-coupled receptor signaling pathwayP2Y purinoceptor 12Homo sapiens (human)
hemostasisP2Y purinoceptor 12Homo sapiens (human)
calcium-mediated signalingP2Y purinoceptor 12Homo sapiens (human)
cerebral cortex radial glia-guided migrationP2Y purinoceptor 12Homo sapiens (human)
cell projection organizationP2Y purinoceptor 12Homo sapiens (human)
lamellipodium assemblyP2Y purinoceptor 12Homo sapiens (human)
platelet activationP2Y purinoceptor 12Homo sapiens (human)
positive regulation of integrin activation by cell surface receptor linked signal transductionP2Y purinoceptor 12Homo sapiens (human)
positive regulation of cell adhesion mediated by integrinP2Y purinoceptor 12Homo sapiens (human)
G protein-coupled purinergic nucleotide receptor signaling pathwayP2Y purinoceptor 12Homo sapiens (human)
positive regulation of monoatomic ion transportP2Y purinoceptor 12Homo sapiens (human)
response to axon injuryP2Y purinoceptor 12Homo sapiens (human)
regulation of chemotaxisP2Y purinoceptor 12Homo sapiens (human)
positive regulation of chemotaxisP2Y purinoceptor 12Homo sapiens (human)
establishment of localization in cellP2Y purinoceptor 12Homo sapiens (human)
positive regulation of phosphatidylinositol 3-kinase/protein kinase B signal transductionP2Y purinoceptor 12Homo sapiens (human)
platelet aggregationP2Y purinoceptor 12Homo sapiens (human)
cellular response to ATPP2Y purinoceptor 12Homo sapiens (human)
visual system developmentP2Y purinoceptor 12Homo sapiens (human)
positive regulation of ruffle assemblyP2Y purinoceptor 12Homo sapiens (human)
regulation of microglial cell migrationP2Y purinoceptor 12Homo sapiens (human)
positive regulation of microglial cell migrationP2Y purinoceptor 12Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (29)

Processvia Protein(s)Taxonomy
phosphatidylserine bindingNeprilysinHomo sapiens (human)
endopeptidase activityNeprilysinHomo sapiens (human)
metalloendopeptidase activityNeprilysinHomo sapiens (human)
protein bindingNeprilysinHomo sapiens (human)
exopeptidase activityNeprilysinHomo sapiens (human)
zinc ion bindingNeprilysinHomo sapiens (human)
peptide bindingNeprilysinHomo sapiens (human)
protein homodimerization activityNeprilysinHomo sapiens (human)
oligopeptidase activityNeprilysinHomo sapiens (human)
cardiolipin bindingNeprilysinHomo sapiens (human)
methyltransferase activityEEF1AKMT4-ECE2 readthrough transcript proteinHomo sapiens (human)
metal ion bindingEEF1AKMT4-ECE2 readthrough transcript proteinHomo sapiens (human)
metalloendopeptidase activityEEF1AKMT4-ECE2 readthrough transcript proteinHomo sapiens (human)
endopeptidase activityAngiotensin-converting enzyme Homo sapiens (human)
carboxypeptidase activityAngiotensin-converting enzyme Homo sapiens (human)
metalloendopeptidase activityAngiotensin-converting enzyme Homo sapiens (human)
calmodulin bindingAngiotensin-converting enzyme Homo sapiens (human)
peptidase activityAngiotensin-converting enzyme Homo sapiens (human)
metallopeptidase activityAngiotensin-converting enzyme Homo sapiens (human)
exopeptidase activityAngiotensin-converting enzyme Homo sapiens (human)
tripeptidyl-peptidase activityAngiotensin-converting enzyme Homo sapiens (human)
peptidyl-dipeptidase activityAngiotensin-converting enzyme Homo sapiens (human)
zinc ion bindingAngiotensin-converting enzyme Homo sapiens (human)
chloride ion bindingAngiotensin-converting enzyme Homo sapiens (human)
mitogen-activated protein kinase kinase bindingAngiotensin-converting enzyme Homo sapiens (human)
bradykinin receptor bindingAngiotensin-converting enzyme Homo sapiens (human)
mitogen-activated protein kinase bindingAngiotensin-converting enzyme Homo sapiens (human)
metallodipeptidase activityAngiotensin-converting enzyme Homo sapiens (human)
heterocyclic compound bindingAngiotensin-converting enzyme Homo sapiens (human)
endopeptidase activityEndothelin-converting enzyme 1Homo sapiens (human)
metalloendopeptidase activityEndothelin-converting enzyme 1Homo sapiens (human)
protein bindingEndothelin-converting enzyme 1Homo sapiens (human)
zinc ion bindingEndothelin-converting enzyme 1Homo sapiens (human)
peptide hormone bindingEndothelin-converting enzyme 1Homo sapiens (human)
protein homodimerization activityEndothelin-converting enzyme 1Homo sapiens (human)
G protein-coupled adenosine receptor activityP2Y purinoceptor 12Homo sapiens (human)
G protein-coupled ADP receptor activityP2Y purinoceptor 12Homo sapiens (human)
guanyl-nucleotide exchange factor activityP2Y purinoceptor 12Homo sapiens (human)
G protein-coupled purinergic nucleotide receptor activityP2Y purinoceptor 12Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (36)

Processvia Protein(s)Taxonomy
cytoplasmNeprilysinHomo sapiens (human)
early endosomeNeprilysinHomo sapiens (human)
trans-Golgi networkNeprilysinHomo sapiens (human)
plasma membraneNeprilysinHomo sapiens (human)
brush borderNeprilysinHomo sapiens (human)
focal adhesionNeprilysinHomo sapiens (human)
synaptic vesicleNeprilysinHomo sapiens (human)
cell surfaceNeprilysinHomo sapiens (human)
membraneNeprilysinHomo sapiens (human)
axonNeprilysinHomo sapiens (human)
dendriteNeprilysinHomo sapiens (human)
secretory granule membraneNeprilysinHomo sapiens (human)
cytoplasmic vesicleNeprilysinHomo sapiens (human)
neuronal cell bodyNeprilysinHomo sapiens (human)
neuron projection terminusNeprilysinHomo sapiens (human)
membrane raftNeprilysinHomo sapiens (human)
synapseNeprilysinHomo sapiens (human)
extracellular exosomeNeprilysinHomo sapiens (human)
presynapseNeprilysinHomo sapiens (human)
plasma membraneNeprilysinHomo sapiens (human)
Golgi membraneEEF1AKMT4-ECE2 readthrough transcript proteinHomo sapiens (human)
transport vesicle membraneEEF1AKMT4-ECE2 readthrough transcript proteinHomo sapiens (human)
plasma membraneEEF1AKMT4-ECE2 readthrough transcript proteinHomo sapiens (human)
extracellular spaceAngiotensin-converting enzyme Homo sapiens (human)
extracellular regionAngiotensin-converting enzyme Homo sapiens (human)
extracellular spaceAngiotensin-converting enzyme Homo sapiens (human)
lysosomeAngiotensin-converting enzyme Homo sapiens (human)
endosomeAngiotensin-converting enzyme Homo sapiens (human)
plasma membraneAngiotensin-converting enzyme Homo sapiens (human)
external side of plasma membraneAngiotensin-converting enzyme Homo sapiens (human)
basal plasma membraneAngiotensin-converting enzyme Homo sapiens (human)
brush border membraneAngiotensin-converting enzyme Homo sapiens (human)
extracellular exosomeAngiotensin-converting enzyme Homo sapiens (human)
sperm midpieceAngiotensin-converting enzyme Homo sapiens (human)
plasma membraneAngiotensin-converting enzyme Homo sapiens (human)
lysosomal membraneEndothelin-converting enzyme 1Homo sapiens (human)
endosomeEndothelin-converting enzyme 1Homo sapiens (human)
plasma membraneEndothelin-converting enzyme 1Homo sapiens (human)
external side of plasma membraneEndothelin-converting enzyme 1Homo sapiens (human)
endosome membraneEndothelin-converting enzyme 1Homo sapiens (human)
membraneEndothelin-converting enzyme 1Homo sapiens (human)
vesicleEndothelin-converting enzyme 1Homo sapiens (human)
Weibel-Palade bodyEndothelin-converting enzyme 1Homo sapiens (human)
perinuclear region of cytoplasmEndothelin-converting enzyme 1Homo sapiens (human)
extracellular exosomeEndothelin-converting enzyme 1Homo sapiens (human)
plasma membraneEndothelin-converting enzyme 1Homo sapiens (human)
plasma membraneP2Y purinoceptor 12Homo sapiens (human)
cell surfaceP2Y purinoceptor 12Homo sapiens (human)
membraneP2Y purinoceptor 12Homo sapiens (human)
cell projection membraneP2Y purinoceptor 12Homo sapiens (human)
cell body membraneP2Y purinoceptor 12Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (37)

Assay IDTitleYearJournalArticle
AID302848Inhibition of thermolysin by enzcheck protease assay2007Bioorganic & medicinal chemistry letters, Dec-01, Volume: 17, Issue:23
Identifying common metalloprotease inhibitors by protein fold types using Fourier transform mass spectrometry.
AID241703Inhibitory concentration against human ECE-1 by RIA2005Journal of medicinal chemistry, Jan-27, Volume: 48, Issue:2
Endothelin-converting enzyme-1 inhibition and growth of human glioblastoma cells.
AID67184Inhibition of endothelin converting enzyme in an RIA assay using ET-1 as substrate (value corresponds to <25% inhibition when assayed at a 100 uM screening concentration)1993Journal of medicinal chemistry, Jan-08, Volume: 36, Issue:1
Phosphorus-containing inhibitors of endothelin converting enzyme: effects of the electronic nature of phosphorus on inhibitor potency.
AID340317Inhibition of human ECE2008Journal of medicinal chemistry, Jul-24, Volume: 51, Issue:14
Identification of a potent, selective, and orally active leukotriene a4 hydrolase inhibitor with anti-inflammatory activity.
AID147354In vitro inhibition of Neutral endopeptidase (NEP) enzyme1994Journal of medicinal chemistry, Feb-18, Volume: 37, Issue:4
N-Phosphonomethyl dipeptides and their phosphonate prodrugs, a new generation of neutral endopeptidase (NEP, EC 3.4.24.11) inhibitors.
AID213087Binding affinity against Thermolysin2002Journal of medicinal chemistry, Jun-20, Volume: 45, Issue:13
SMall Molecule Growth 2001 (SMoG2001): an improved knowledge-based scoring function for protein-ligand interactions.
AID147212Inhibitory activity against Leu-enkeph of Neutral endopeptidase1995Journal of medicinal chemistry, Jun-09, Volume: 38, Issue:12
Hydroxamic acids as potent inhibitors of endothelin-converting enzyme from human bronchiolar smooth muscle.
AID1607329Inhibition of rabbit lung ACE using hippuryl-His-Leu as substrate preincubated with enzyme for 15 mins followed by substrate addition2020Journal of medicinal chemistry, 05-28, Volume: 63, Issue:10
Molecular Basis for Omapatrilat and Sampatrilat Binding to Neprilysin-Implications for Dual Inhibitor Design with Angiotensin-Converting Enzyme.
AID147364Inhibitory activity against neutral endopeptidase (NEP) from rat cortex brain membrane2003Journal of medicinal chemistry, Jul-17, Volume: 46, Issue:15
Computer-aided selection of potential antihypertensive compounds with dual mechanism of action.
AID1578357Inhibition of Mycobacterium tuberculosis Zinc metalloprotease-1 at 40 uM using angiotensin 2 as substrate preincubated for 3 mins and measured after 20 mins by MALDI-TOF MS analysis relative to control2020European journal of medicinal chemistry, Jan-01, Volume: 185Novel thiazolidinedione-hydroxamates as inhibitors of Mycobacterium tuberculosis virulence factor Zmp1.
AID67359Binding affinity towards enkephalinase (metalloendopeptidase, E.C.3.4.24.11) of rat kidney1985Journal of medicinal chemistry, Sep, Volume: 28, Issue:9
Synthesis and biological evaluation of phosphonamidate peptide inhibitors of enkephalinase and angiotensin-converting enzyme.
AID1607328Inhibition of rat kidney NEP using glutaryl-Ala-Ala-beta-naphthylamide as substrate preincubated with enzyme for 15 mins followed by substrate addition2020Journal of medicinal chemistry, 05-28, Volume: 63, Issue:10
Molecular Basis for Omapatrilat and Sampatrilat Binding to Neprilysin-Implications for Dual Inhibitor Design with Angiotensin-Converting Enzyme.
AID213070Inhibitory constant against thermolysin.1992Journal of medicinal chemistry, May-15, Volume: 35, Issue:10
Definition and display of steric, hydrophobic, and hydrogen-bonding properties of ligand binding sites in proteins using Lee and Richards accessible surface: validation of a high-resolution graphical tool for drug design.
AID67206Ratio of inhibitory activities against endothelin converting enzyme-1(ECE-1) and neutral endopeptidase (NEP).1998Journal of medicinal chemistry, Apr-23, Volume: 41, Issue:9
Design and synthesis of potent, selective inhibitors of endothelin-converting enzyme.
AID67199Inhibitory activity was assessed on CHO cells expressing recombinant human Endothelin-converting enzyme 1 (ECE-1).1998Journal of medicinal chemistry, Apr-23, Volume: 41, Issue:9
Design and synthesis of potent, selective inhibitors of endothelin-converting enzyme.
AID67345Inhibition of enkephalinase activity in membranes prepared from rabbit1989Journal of medicinal chemistry, Dec, Volume: 32, Issue:12
Enkephalinase inhibitors. 1. 2,4-Dibenzylglutaric acid derivatives.
AID213074Inhibitory activity against thermolysin with 0.5 uM [Leu5]-enkephalin (NEN)1995Journal of medicinal chemistry, Jun-09, Volume: 38, Issue:12
Hydroxamic acids as potent inhibitors of endothelin-converting enzyme from human bronchiolar smooth muscle.
AID147365Inhibitory activity against neutral endopeptidase (NEP).1998Journal of medicinal chemistry, Apr-23, Volume: 41, Issue:9
Design and synthesis of potent, selective inhibitors of endothelin-converting enzyme.
AID228593In Vitro inhibition of recombinant human endothelin converting enzyme-12000Journal of medicinal chemistry, Feb-10, Volume: 43, Issue:3
Potent and selective non-peptidic inhibitors of endothelin-converting enzyme-1 with sustained duration of action.
AID147213Inhibitory activity against big ET-1 of Neutral endopeptidase1995Journal of medicinal chemistry, Jun-09, Volume: 38, Issue:12
Hydroxamic acids as potent inhibitors of endothelin-converting enzyme from human bronchiolar smooth muscle.
AID67194Inhibitory activity against human bronchiolar smooth muscle Endothelin-converting enzyme 11995Journal of medicinal chemistry, Jun-09, Volume: 38, Issue:12
Hydroxamic acids as potent inhibitors of endothelin-converting enzyme from human bronchiolar smooth muscle.
AID456871Inhibition of collagenase type 4 after 30 mins by fluorescence plate reader2010Bioorganic & medicinal chemistry letters, Feb-01, Volume: 20, Issue:3
Identification of potential and selective collagenase, gelatinase inhibitors from Crataegus pinnatifida.
AID433787Inhibition of human recombinant ECE1 by fluorimetry2009Bioorganic & medicinal chemistry letters, Aug-15, Volume: 19, Issue:16
Synthesis and enzymatic evaluation of novel partially fluorinated thiol dual ACE/NEP inhibitors.
AID67352Inhibition of enkephalinase activity in synaptic membranes prepared from rat striatum1989Journal of medicinal chemistry, Dec, Volume: 32, Issue:12
Enkephalinase inhibitors. 1. 2,4-Dibenzylglutaric acid derivatives.
AID147352Evaluation of in vitro inhibitory activity against Neutral endopeptidase1995Journal of medicinal chemistry, Dec-22, Volume: 38, Issue:26
New alpha-thiol dipeptide dual inhibitors of angiotensin-I converting enzyme and neutral endopeptidase EC 3.4.24.11.
AID147073Inhibitory activity against neutral endopeptidase (NEP) from human blood serum2003Journal of medicinal chemistry, Jul-17, Volume: 46, Issue:15
Computer-aided selection of potential antihypertensive compounds with dual mechanism of action.
AID620439Inhibition of neutral endopeptidase in human fibroblasts homogenates using glutaryl-Ala-Ala-Phe-4-methoxy-2-naphtylamide as substrate after 1 hrs by fluorimetric assay2011Bioorganic & medicinal chemistry, Oct-15, Volume: 19, Issue:20
Structure-based design of dipeptide derivatives for the human neutral endopeptidase.
AID402013Inhibition of collagenase type 52005Journal of natural products, May, Volume: 68, Issue:5
Collagenase inhibitory quinic acid esters from Ipomoea pes-caprae.
AID1578358Inhibition of Mycobacterium tuberculosis Zinc metalloprotease-1 using angiotensin 2 as substrate preincubated for 3 mins and measured after 20 mins by MALDI-TOF MS analysis2020European journal of medicinal chemistry, Jan-01, Volume: 185Novel thiazolidinedione-hydroxamates as inhibitors of Mycobacterium tuberculosis virulence factor Zmp1.
AID444548Inhibition of human somatic ECE12010Journal of medicinal chemistry, Jan-14, Volume: 53, Issue:1
Phosphinic tripeptides as dual angiotensin-converting enzyme C-domain and endothelin-converting enzyme-1 inhibitors.
AID143636In vitro inhibition of rat neutral endopeptidase2000Journal of medicinal chemistry, Feb-10, Volume: 43, Issue:3
Potent and selective non-peptidic inhibitors of endothelin-converting enzyme-1 with sustained duration of action.
AID67338Inhibition of Endothelin-converting enzyme 1 activity at a concentration of 1 uM2000Journal of medicinal chemistry, Feb-10, Volume: 43, Issue:3
Potent and selective non-peptidic inhibitors of endothelin-converting enzyme-1 with sustained duration of action.
AID235174Selectivity ratio of IC50 NEP/IC50 ECE2000Journal of medicinal chemistry, Feb-10, Volume: 43, Issue:3
Potent and selective non-peptidic inhibitors of endothelin-converting enzyme-1 with sustained duration of action.
AID444547Inhibition of human somatic NEP2010Journal of medicinal chemistry, Jan-14, Volume: 53, Issue:1
Phosphinic tripeptides as dual angiotensin-converting enzyme C-domain and endothelin-converting enzyme-1 inhibitors.
AID977610Experimentally measured binding affinity data (Ki) for protein-ligand complexes derived from PDB1986European journal of biochemistry, Jun-02, Volume: 157, Issue:2
Crystallographic structural analysis of phosphoramidates as inhibitors and transition-state analogs of thermolysin.
AID1811Experimentally measured binding affinity data derived from PDB1986European journal of biochemistry, Jun-02, Volume: 157, Issue:2
Crystallographic structural analysis of phosphoramidates as inhibitors and transition-state analogs of thermolysin.
AID1799789Enzymatic Assay from Article 10.1074/jbc.M110.120576: \\Identification of an endothelin-converting enzyme-2-specific fluorigenic substrate and development of an in vitro and ex vivo enzymatic assay.\\2010The Journal of biological chemistry, Nov-05, Volume: 285, Issue:45
Identification of an endothelin-converting enzyme-2-specific fluorigenic substrate and development of an in vitro and ex vivo enzymatic assay.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (760)

TimeframeStudies, This Drug (%)All Drugs %
pre-1990101 (13.29)18.7374
1990's476 (62.63)18.2507
2000's142 (18.68)29.6817
2010's39 (5.13)24.3611
2020's2 (0.26)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 26.49

According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be moderate demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index26.49 (24.57)
Research Supply Index6.68 (2.92)
Research Growth Index4.82 (4.65)
Search Engine Demand Index36.71 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (26.49)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials12 (1.54%)5.53%
Reviews10 (1.28%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other759 (97.18%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]