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Literature summary for 3.4.24.71 extracted from

  • Hasdemir, B.; Mahajan, S.; Bunnett, N.W.; Liao, M.; Bhargava, A.
    Endothelin-Converting Enzyme-1 Actions Determine Differential Trafficking and Signaling of Corticotropin-Releasing Factor Receptor 1 at High Agonist Concentrations (2012), Mol. Endocrinol., 26, 681-695.
    View publication on PubMedView publication on EuropePMC
Search for more literature for 3.4.24.71

Inhibitors

Inhibitors Comment Organism Structure
4-chloro-N-[(4-cyano-3-methyl-1-phenyl-1H-pyrazol-5-yl)amino]carbonyl benzenesulfonamide
-
 Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
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 Homo sapiens ?
-
 ?
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 Homo sapiens ?
-
 ?

Synonyms

Synonyms Comment Organism
ECE-1
-
 Homo sapiens

Temperature Optimum [°C]

Temperature Optimum [°C] Temperature Optimum Maximum [°C] Comment Organism
37
-
 assay at Homo sapiens

pH Optimum

pH Optimum Minimum pH Optimum Maximum Comment Organism
5.5
-
 ECE-1 degrades Ucn1 and CRF at endosomal (pH 5.5) Homo sapiens
7.4
-
 ECE-1 degrades Ucn1 at both extracellular (pH 7.4) Homo sapiens

General Information

General Information Comment Organism
physiological function differential degradation by ECE-1 is a novel mechanism by which corticotropin-releasing factor receptor 1 is protected from overactivation by physiologically relevant high concentrations of higher affinity ligand to mediate distinct resensitization and downstream signaling Homo sapiens