Target Information

Target General Infomation
Target ID
T50970
Former ID
TTDR00135
Target Name
Endothelin-converting enzyme 1
Gene Name
ECE1
Synonyms
ECE-1; ECE1
Target Type
Discontinued
Function
Converts big endothelin-1 to endothelin-1.
BioChemical Class
Peptidase
Target Validation
T50970
UniProt ID
P42892
EC Number
EC 3.4.24.71
Sequence
MRGVWPPPVSALLSALGMSTYKRATLDEEDLVDSLSEGDAYPNGLQVNFHSPRSGQRCWA
ARTQVEKRLVVLVVLLAAGLVACLAALGIQYQTRSPSVCLSEACVSVTSSILSSMDPTVD
PCHDFFSYACGGWIKANPVPDGHSRWGTFSNLWEHNQAIIKHLLENSTASVSEAERKAQV
YYRACMNETRIEELRAKPLMELIERLGGWNITGPWAKDNFQDTLQVVTAHYRTSPFFSVY
VSADSKNSNSNVIQVDQSGLGLPSRDYYLNKTENEKVLTGYLNYMVQLGKLLGGGDEEAI
RPQMQQILDFETALANITIPQEKRRDEELIYHKVTAAELQTLAPAINWLPFLNTIFYPVE
INESEPIVVYDKEYLEQISTLINTTDRCLLNNYMIWNLVRKTSSFLDQRFQDADEKFMEV
MYGTKKTCLPRWKFCVSDTENNLGFALGPMFVKATFAEDSKSIATEIILEIKKAFEESLS
TLKWMDEETRKSAKEKADAIYNMIGYPNFIMDPKELDKVFNDYTAVPDLYFENAMRFFNF
SWRVTADQLRKAPNRDQWSMTPPMVNAYYSPTKNEIVFPAGILQAPFYTRSSPKALNFGG
IGVVVGHELTHAFDDQGREYDKDGNLRPWWKNSSVEAFKRQTECMVEQYSNYSVNGEPVN
GRHTLGENIADNGGLKAAYRAYQNWVKKNGAEHSLPTLGLTNNQLFFLGFAQVWCSVRTP
ESSHEGLITDPHSPSRFRVIGSLSNSKEFSEHFRCPPGSPMNPPHKCEVW
Drugs and Mode of Action
Drug(s) SCH-54470 Drug Info Terminated Discovery agent [546391]
Inhibitor 5-(2-hydroxyethyl)nonane-1,9-diol Drug Info [551374]
CGS 35066 Drug Info [535609]
compound 22 Drug Info [530505]
LY-292223 Drug Info [527383]
PD159790 Drug Info [543449]
PO3 2-Ile-Trp-O-3K Drug Info [551263]
PO3 2-Leu-Nal-O-3K Drug Info [551263]
PO3 2-Leu-Trp-O-3K Drug Info [551263]
PO3 2-Nle-Trp-O-3K Drug Info [551263]
SCH-54470 Drug Info [530505]
Pathways
PANTHER Pathway Endothelin signaling pathway
WikiPathways SIDS Susceptibility Pathways
Corticotropin-releasing hormone
Endothelin Pathways
References
Ref 546391Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800007872)
Ref 527383J Med Chem. 2005 Jan 27;48(2):483-98.Endothelin-converting enzyme-1 inhibition and growth of human glioblastoma cells.
Ref 530505J Med Chem. 2010 Jan 14;53(1):208-20.Phosphinic tripeptides as dual angiotensin-converting enzyme C-domain and endothelin-converting enzyme-1 inhibitors.
Ref 535609The therapeutic potential of endothelin-1 receptor antagonists and endothelin-converting enzyme inhibitors on the cardiovascular system. Expert Opin Investig Drugs. 2002 Nov;11(11):1537-52.
Ref 543449(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Target id: 1615).
Ref 551263Aminophosphonate endothelin converting enzyme inhibitors: potency-enhancing and selectivity-improving modifications of phosphoramidon, Bioorg. Med. Chem. Lett. 4(10):1257-1262 (1994).
Ref 551374The Protein Data Bank. Nucleic Acids Res. 2000 Jan 1;28(1):235-42.

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