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Information on EC 3.4.24.71 - endothelin-converting enzyme 1
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3.4.24.71 endothelin-converting enzyme 1Specify your search results
Word Map
- 3.4.24.71
- endothelins
- phosphoramidon
- artery
-
vasoconstrictor
- endopeptidase
- cardiovascular
- hypertension
- cardiac
- pulmonary
- angiotensin
- neprilysin
-
tone
-
vasoactive
- metalloprotease
- vessel
- coronary
-
phosphoramidon-sensitive
- metallopeptidases
-
contractile
-
preproet-1
- vasospasm
- thiorphan
-
atrial
-
natriuretic
-
pressor
- ventricular
- aortic
-
angiotensin-converting
- preproendothelin-1
-
endothelium-derived
-
et-1-induced
-
insulin-degrading
- drug development
-
baecs
-
hemodynamic
- medicine
-
vasopeptidase
-
etb-receptors
-
3.4.24.11
- metalloendopeptidase
-
subarachnoid
- chymase
-
conscious
-
ednra
- sarafotoxin
-
basilar
-
ppet-1
-
21-amino
-
prepro
- enzyme-2
- bosentan
-
et-1-mediated
The enzyme appears in viruses and cellular organisms
Reaction Schemes
Hydrolysis of the -Trp21-/-Val- bond in big endothelin to form endothelin 1
Synonyms
ece-1, endothelin-converting enzyme, endothelin converting enzyme, endothelin-converting enzyme-1, ece-1b, endothelin converting enzyme-1, hece-1, et converting enzyme, endothelin-converting enzyme 1, endothelin-converting enzyme 1 (ece-1), 
more
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SYNONYM 
ORGANISM
UNIPROT
COMMENTARY 
LITERATURE
ECE
ECE-1
ECE1
endothelin converting enzyme-1
Endothelin-converting enzyme
endothelin-converting enzyme 1
endothelin-converting enzyme 1 (ECE-1)
endothelin-converting enzyme-1
endothelin-converting-enzyme-1
additional information
ECE-1
-
-
-
-
ECE-1
-
-
649414, 649885, 651235, 652710, 653706, 667961, 668981, 669533, 669569, 669782, 669970, 670866, 683321, 683416, 683434, 683435, 683437, 683438, 683439, 683440, 683474, 683513, 683696, 683702, 683720, 683965, 684002, 697033, 697100, 697686, 699415, 701191, 709039, 709470, 709856, 710094, 719207, 720290, 720472
ECE-1
-
Endothelin-converting enzyme
-
-
-
-
endothelin-converting enzyme-1
-
-
additional information
-
ECE-1 is a type II membrane protease belonging to the neprilysin family of zinc metallopeptidases
additional information
-
endothelin-converting enzymes are a class of type II integral membrane-bound proteases, belonging to the M13 family of zinc metallopeptidases
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REACTION
REACTION DIAGRAM
COMMENTARY
ORGANISM
UNIPROT
LITERATURE
Hydrolysis of the -Trp21-/-Val- bond in big endothelin to form endothelin 1
-
-
-
-
Hydrolysis of the -Trp21-/-Val- bond in big endothelin to form endothelin 1
ECE-1 promotes the recycling and re-sensitization of NK1 receptors, by degrading endocytosed substance P in endothelial cell endosomes. ECE-1 promotes CGRP and somatostatin receptor recycling
-
Hydrolysis of the -Trp21-/-Val- bond in big endothelin to form endothelin 1
ECE-1 regulates re-sensitization of substance P signalling in HMEC-1-NK1 receptor cells
-
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REACTION TYPE
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
hydrolysis of peptide bond
-
-
-
-
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CAS REGISTRY NUMBER
COMMENTARY
138238-81-0
-
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SUBSTRATE
PRODUCT
REACTION DIAGRAM
ORGANISM
UNIPROT
COMMENTARY
(Substrate)
(Substrate)
LITERATURE
(Substrate)
(Substrate)
COMMENTARY
(Product)
(Product)
LITERATURE
(Product)
(Product)
Reversibility
r=reversible
ir=irreversible
?=not specified
r=reversible
ir=irreversible
?=not specified
(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 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
-
-
?
Big endothelin 1 + H2O
?
-
key enzyme in endothelin production, generates potent vasoconstrictor endothelin from its inactive precursor
-
-
?
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
-
-
?
M7-methoxycoumarin-4-ylacetyl-Arg-Pro-Pro-Gly-Phe-Ser-Ala-Phe-Lys(2,4-dinitrophenyl)-OH + 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
-
-
?
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 + ?
-
PKCepsilon regulates the expression of ECE-1 in the brain
-
-
?
big endothelin + H2O
endothelin 1 + ?
-
ECE-1a, 1b, 1c and 1d are all equally active on endothelin
-
-
?
big endothelin-1 + H2O
endothelin + ?
-
key enzyme in the biosynthesis of the endothelins
-
?
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 + ?
-
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-3 + H2O
endothelin-3 + ?
-
specific for this substrate, big-endothelin-1 is no substrate
-
?
big endothelin-I + H2O
endothelin + ?
-
key enzyme in the biosynthesis of the endothelins
-
?
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
?
-
hydrolysis at 50% the rate of big endothelin1
-
-
?
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
?
-
-
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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NATURAL SUBSTRATE
NATURAL PRODUCT
REACTION DIAGRAM
ORGANISM
UNIPROT
COMMENTARY
(Substrate)
(Substrate)
LITERATURE
(Substrate)
(Substrate)
COMMENTARY
(Product)
(Product)
LITERATURE
(Product)
(Product)
REVERSIBILITY
r=reversible
ir=irreversible
?=not specified
r=reversible
ir=irreversible
?=not specified
Big endothelin 1 + H2O
?
-
key enzyme in endothelin production, generates potent vasoconstrictor endothelin from its inactive precursor
-
-
?
big endothelin-3 + H2O
endothelin-3 + ?
-
specific for this substrate, big-endothelin-1 is no substrate
-
?
big endothelin-I + H2O
endothelin + ?
-
key enzyme in the biosynthesis of the endothelins
-
?
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
-
-
?
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 + ?
-
PKCepsilon regulates the expression of ECE-1 in the brain
-
-
?
big endothelin-1 + H2O
endothelin + ?
-
key enzyme in the biosynthesis of the endothelins
-
?
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 + ?
-
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 + ?
-
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
-
-
?