3.4.24.71: endothelin-converting enzyme 1
This is an abbreviated version!
For detailed information about endothelin-converting enzyme 1, go to the full flat file.
Word Map on EC 3.4.24.71
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3.4.24.71
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endothelins
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phosphoramidon
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artery
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vasoconstrictor
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endopeptidase
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cardiovascular
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hypertension
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cardiac
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pulmonary
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angiotensin
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neprilysin
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tone
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vasoactive
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metalloprotease
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vessel
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coronary
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phosphoramidon-sensitive
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metallopeptidases
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contractile
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preproet-1
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vasospasm
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thiorphan
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atrial
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natriuretic
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pressor
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ventricular
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aortic
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angiotensin-converting
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preproendothelin-1
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endothelium-derived
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et-1-induced
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insulin-degrading
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drug development
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baecs
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hemodynamic
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medicine
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vasopeptidase
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etb-receptors
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3.4.24.11
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metalloendopeptidase
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subarachnoid
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chymase
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conscious
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ednra
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sarafotoxin
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basilar
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ppet-1
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21-amino
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prepro
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enzyme-2
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bosentan
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et-1-mediated
- 3.4.24.71
- endothelins
- phosphoramidon
- artery
-
vasoconstrictor
- endopeptidase
- cardiovascular
- hypertension
- cardiac
- pulmonary
- angiotensin
- neprilysin
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tone
-
vasoactive
- metalloprotease
- vessel
- coronary
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phosphoramidon-sensitive
- metallopeptidases
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contractile
-
preproet-1
- vasospasm
- thiorphan
-
atrial
-
natriuretic
-
pressor
- ventricular
- aortic
-
angiotensin-converting
- preproendothelin-1
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endothelium-derived
-
et-1-induced
-
insulin-degrading
- drug development
-
baecs
-
hemodynamic
- medicine
-
vasopeptidase
-
etb-receptors
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3.4.24.11
- metalloendopeptidase
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subarachnoid
- chymase
-
conscious
-
ednra
- sarafotoxin
-
basilar
-
ppet-1
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21-amino
-
prepro
- enzyme-2
- bosentan
-
et-1-mediated
Reaction
Hydrolysis of the -Trp21-/-Val- bond in big endothelin to form endothelin 1 =
Synonyms
ECE, ECE-1, ECE-1b, ECE-3, ECE1, endothelin converting enzyme, endothelin converting enzyme-1, Endothelin-converting enzyme, endothelin-converting enzyme 1, endothelin-converting enzyme 1 (ECE-1), endothelin-converting enzyme I, endothelin-converting enzyme-1, endothelin-converting-enzyme-1, ET converting enzyme, hECE-1, More, sECE, solECE-1
ECTree
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Substrates Products
Substrates Products on EC 3.4.24.71 - endothelin-converting enzyme 1
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REACTION DIAGRAM
(7-methoxy-coumarin-4-yl)acetyl-Arg-Pro-Pro-Gly-Phe-Ser-Ala-Phe-Lys(2,4-dinitrophenyl) + H2O
?
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fluorogenic substrate
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-
?
(7-methoxycoumarin-4-yl)acetyl-Arg-Pro-Pro-Gly-Phe-Ser-Ala-Phe-Lys(2,4-dinitrophenyl)-OH + H2O
?
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?
(7-methoxycoumarin-4-yl)acetyl-Arg-Pro-Pro-Gly-Phe-Ser-Ala-Phe-Lys-2,4-dinitrophenyl-OH + H2O
?
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-
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?
amyloid-beta peptide + H2O
amyloid-beta peptide + ?
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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
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?
Big endothelin 1 + H2O
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key enzyme in endothelin production, generates potent vasoconstrictor endothelin from its inactive precursor
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-
?
corticotropin-releasing factor + H2O
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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
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-
?
M7-methoxycoumarin-4-ylacetyl-Arg-Pro-Pro-Gly-Phe-Ser-Ala-Phe-Lys(2,4-dinitrophenyl)-OH + H2O
?
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?
Somatostatin-14 + H2O
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i.e. SST-14, degradation of rat substrate internalized via recombinantly expressed somatostatin receptor subtype sst2A into HEK-293 cells
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?
urocortin-1 + H2O
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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
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?
big endothelin + H2O
endothelin + ?
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ECE-1 is a membrane-bound metalloprotease responsible for production of vasoactive endothelin-1 from inactive big ET-1
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-
?
big endothelin + H2O
endothelin + ?
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PKCepsilon regulates the expression of ECE-1 in the brain
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?
big endothelin + H2O
endothelin 1 + ?
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ECE-1a, 1b, 1c and 1d are all equally active on endothelin
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-
?
big endothelin-1 + H2O
endothelin + ?
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key enzyme in the biosynthesis of the endothelins
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?
big endothelin-1 + H2O
endothelin + ?
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ECE-1 is a critical enzyme in the production of the potent vasoconstrictor peptide endothelin, ET-1
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-
?
big endothelin-1 + H2O
endothelin-1 + ?
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final step of posttranslational processing of this peptide
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?
big endothelin-1 + H2O
endothelin-1 + ?
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most potent naturally occurring vasoconstrictor
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?
big endothelin-1 + H2O
endothelin-1 + ?
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activation
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-
?
big endothelin-1 + H2O
endothelin-1 + ?
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ECE-1 inhibition in MCF-7 breast cancer cells leads to a significantly decreased ET-1 expression and reduced cell invasiveness, overview
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-
?
big endothelin-1 + H2O
endothelin-1 + ?
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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
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?
big endothelin-1 + H2O
endothelin-1 + ?
big endothelin-1 is hydrolyzed at Asp18-Ile19
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-
?
big endothelin-1 + H2O
endothelin-1 + ?
big endothelin-1 is hydrolyzed at Asp18-Ile19
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-
?
endothelin-3 + ?
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specific for this substrate, big-endothelin-1 is no substrate
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?
big endothelin-I + H2O
endothelin + ?
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key enzyme in the biosynthesis of the endothelins
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?
calcitonin gene-related peptide + H2O
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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
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?
Endothelin 1 + big endothelin 1(21-38)
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best substrate
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?
Human big endothelin 1 + H2O
Endothelin 1 + big endothelin 1(21-38)
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cleavage site: Trp21-Val22
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?
Human big endothelin 1 + H2O
Endothelin 1 + big endothelin 1(21-38)
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best substrate
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-
?
?
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hydrolysis at about 40% the rate of big endothelin1
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?
Human big endothelin 2 + H2O
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hydrolysis at 25% the rate of big endothelin1
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?
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hydrolysis at about 30% the rate of big endothelin1
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?
Human big endothelin 3 + H2O
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hydrolysis at 50% the rate of big endothelin1
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?
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no substrate is the big endothelin 1(1-31) fragment
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additional information
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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
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?
additional information
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the enzyme catalyzes the final step in endothelin processing
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?
additional information
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the enzyme is involved in chalizia, a granulomatous lesions of the eyelid
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additional information
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the enzyme plays a crucial role in the regulation of vascular tone and endothelial function
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?
additional information
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ECE-1 and endosomal acidification regulate the duration of substance P-induced ERK2 activation
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additional information
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ECEs can hydrolyze several other biologically active peptides in vitro by cleavage on the amino side of hydrophobic residues
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additional information
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endothelin-converting enzyme function as vasopeptidase
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additional information
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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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additional information
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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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?