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Information on EC 3.4.24.71 - endothelin-converting enzyme 1 and Organism(s) Rattus norvegicus and UniProt Accession P42893

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EC Tree
     3 Hydrolases
         3.4 Acting on peptide bonds (peptidases)
             3.4.24 Metalloendopeptidases
                3.4.24.71 endothelin-converting enzyme 1
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This record set is specific for:
Rattus norvegicus
UNIPROT: P42893 not found.
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Word Map
The taxonomic range for the selected organisms is: Rattus norvegicus
The expected taxonomic range for this enzyme is: Eukaryota, Bacteria, Archaea
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
SYNONYM
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
endothelin-converting enzyme-1
-
ECE-1
Endothelin-converting enzyme
-
-
-
-
endothelin-converting enzyme 1 (ECE-1)
-
-
endothelin-converting enzyme-1
-
-
REACTION TYPE
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
hydrolysis of peptide bond
-
-
-
-
CAS REGISTRY NUMBER
COMMENTARY hide
138238-81-0
-
SUBSTRATE
PRODUCT                       
REACTION DIAGRAM
ORGANISM
UNIPROT
COMMENTARY
(Substrate) hide
LITERATURE
(Substrate)
COMMENTARY
(Product) hide
LITERATURE
(Product)
Reversibility
r=reversible
ir=irreversible
?=not specified
big endothelin + H2O
endothelin-1 + ?
show the reaction diagram
-
-
-
?
big endothelin-1 + H2O
endothelin-1 + ?
show the reaction diagram
-
-
-
?
amyloid-beta peptide + H2O
?
show the reaction diagram
-
degradation
-
-
?
big endothelin + H2O
endothelin-1 + ?
show the reaction diagram
-
-
-
-
?
Big endothelin 1 + H2O
?
show the reaction diagram
-
key enzyme in endothelin production, generates potent vasoconstrictor endothelin from its inactive precursor
-
-
?
big endothelin-1 + H2O
endothelin-1 + ?
show the reaction diagram
-
-
-
-
?
big endothelin-2 + H2O
?
show the reaction diagram
-
-
-
-
?
big endothelin-3 + H2O
endothelin-3 + ?
show the reaction diagram
-
-
-
-
?
Human big endothelin 1 + H2O
Endothelin 1 + big endothelin 1(21-38)
show the reaction diagram
-
best substrate
-
-
?
Human big endothelin 2 + H2O
?
show the reaction diagram
-
hydrolysis at 25% the rate of big endothelin1
-
-
?
Human big endothelin 3 + H2O
?
show the reaction diagram
-
hydrolysis at 50% the rate of big endothelin1
-
-
?
preproendothelin-1 + H2O
endothelin-1 + ?
show the reaction diagram
-
-
-
-
?
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
-
-
?
NATURAL SUBSTRATE
NATURAL PRODUCT
REACTION DIAGRAM
ORGANISM
UNIPROT
COMMENTARY
(Substrate) hide
LITERATURE
(Substrate)
COMMENTARY
(Product) hide
LITERATURE
(Product)
REVERSIBILITY
r=reversible
ir=irreversible
?=not specified
big endothelin + H2O
endothelin-1 + ?
show the reaction diagram
-
-
-
?
big endothelin-1 + H2O
endothelin-1 + ?
show the reaction diagram
-
-
-
?
amyloid-beta peptide + H2O
?
show the reaction diagram
-
degradation
-
-
?
big endothelin + H2O
endothelin-1 + ?
show the reaction diagram
-
-
-
-
?
Big endothelin 1 + H2O
?
show the reaction diagram
-
key enzyme in endothelin production, generates potent vasoconstrictor endothelin from its inactive precursor
-
-
?
big endothelin-1 + H2O
endothelin-1 + ?
show the reaction diagram
-
-
-
-
?
preproendothelin-1 + H2O
endothelin-1 + ?
show the reaction diagram
-
-
-
-
?
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
-
-
?
METALS and IONS
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
Zinc
-
zinc metalloproteinase, zinc-binding domain
additional information
-
neutral metalloendopeptidase
INHIBITOR
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
1,10-phenanthroline
-
-
4-chloro-N-(((4-cyano-3-methyl-1-phenyl-1H-pyrazol-5-yl)amino)carbonyl)benzenesulfonamide
-
-
phosphoramidon
-
-
RO 67-7447
-
synthetic inhibitor, selective 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
additional information
-
ACTIVATING COMPOUND
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
additional information
-
diabetes and radiocontrast media increase medullary, but not cortical endothelin converting enzyme-1 content in the kidney, in vivo, the induction of diabetes or the administration of contrast media rises the enzyme activity 4-5fold, but 15fold when diabetic rats are given contrast media, the in vitro activity is increased 3-4fold, overview
-
KM VALUE [mM]
SUBSTRATE
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
0.0002
Big endothelin-1
-
-
0.00046
big endothelin-2
-
-
0.00027
big endothelin-3
-
-
IC50 VALUE [mM]
INHIBITOR
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
0.0000012
RO 67-7447
Rattus norvegicus
-
-
SPECIFIC ACTIVITY [µmol/min/mg]
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
0.00127
-
-
pH OPTIMUM
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
6.6 - 6.8
-
-
pH RANGE
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
6.5 - 7.2
-
active in a narrow range
TEMPERATURE OPTIMUM
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
37
-
assay at
ORGANISM
COMMENTARY hide
LITERATURE
UNIPROT
SEQUENCE DB
SOURCE
SOURCE TISSUE
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
SOURCE
-
analysis of the levels of ECE-1 expression and distribution under normal and pathologic conditions of Alzheimer disease, overview
Manually annotated by BRENDA team
-
ECE-1 promotes re-sensitization of SP-induced inflammation
Manually annotated by BRENDA team
-
vascular
Manually annotated by BRENDA team
-
lung enzyme is similar to that of endothelial cells
Manually annotated by BRENDA team
-
dorsal skin, ECE-1 promotes re-sensitization of SP-induced inflammation
Manually annotated by BRENDA team
-
ECE-1 protein level in stellate cell from bile duct ligation-injured liver is increased twofold compared to those in normal stellate cell, ECE-1 protein is also up-regulated in cell from CCl4-injured liver and culture-activated stellate cell. Exposure of stellate cell from injured livers to TGF-betaincreases ECE-1 expression
Manually annotated by BRENDA team
-
ECE-1 promotes re-sensitization of SP-induced inflammation
Manually annotated by BRENDA team
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
Manually annotated by BRENDA team
LOCALIZATION
ORGANISM
UNIPROT
COMMENTARY hide
GeneOntology No.
LITERATURE
SOURCE
GENERAL INFORMATION
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
malfunction
-
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
metabolism
-
regulation of neuropeptide signaling at the cell surface involving ECE-1, detailed overview
physiological function
-
ECE-1 regulates the duration and subcellular location of substance P-induced, beta-arrestin-dependent ERK activation, overview
UNIPROT
ENTRY NAME
ORGANISM
NO. OF AA
NO. OF TRANSM. HELICES
MOLECULAR WEIGHT[Da]
SOURCE
SEQUENCE
LOCALIZATION PREDICTION?
ECE1_RAT
762
1
86126
Swiss-Prot
Secretory Pathway (Reliability: 5)
MOLECULAR WEIGHT
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
130000
-
1 * 130000, SDS-PAGE
170000 - 190000
-
rat, FPLC gel filtration
85520
-
rat, deduced from nucleotide sequence
86000
-
1 * 86000, deglycosylated enzyme, SDS-PAGE
SUBUNIT
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
monomer
POSTTRANSLATIONAL MODIFICATION
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
glycoprotein
-
highly glycosylated with 10 possible N-linked glycosylated sites
PURIFICATION (Commentary)
ORGANISM
UNIPROT
LITERATURE
CLONED (Commentary)
ORGANISM
UNIPROT
LITERATURE
expressed in COS-cells
-
EXPRESSION
ORGANISM
UNIPROT
LITERATURE
cyclosporine A intensifies renal enzyme expression. The enzyme is upregulated by hypoxia via hypoxia-inducible factor
enzyme expression is significantly increased in the placenta and its implantation site of pregnant hyperinsulinemic rats. In the kidney and heart, protein expression is increased by 230 and 220%, respectively, while its level in the liver is similar in normal and hyperinsulinemic rats
the mRNA expression of isoforms ECE-1a and -b is upregulated in biliary cirrhosis and in CCl4-injured livers, whereas isoform ECE-1c mRNA remains unchanged. Enzyme activity is increased after bile duct occlusion and peaks at 12 h after acute CCl4-intoxication
REF.
AUTHORS
TITLE
JOURNAL
VOL.
PAGES
YEAR
ORGANISM (UNIPROT)
PUBMED ID
SOURCE
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
Manually annotated by BRENDA team
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
Manually annotated by BRENDA team
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
Manually annotated by BRENDA team
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
Manually annotated by BRENDA team
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
Manually annotated by BRENDA team
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
Manually annotated by BRENDA team
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.
Manually annotated by BRENDA team
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
Manually annotated by BRENDA team
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)
Manually annotated by BRENDA team
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)
Manually annotated by BRENDA team
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)
Manually annotated by BRENDA team