Details of the Drug Therapeutic Target (DTT)

General Information of Drug Therapeutic Target (DTT) (ID: TTQ9RYT)

• DTT Name: Endothelin-converting enzyme 1 (ECE1)
• Synonyms: ECE-1
• Gene Name: ECE1
• DTT Type: Literature-reported target; [1]
• BioChemical Class: Peptidase
• UniProt ID: ECE1_HUMAN
• TTD ID: T50970
• EC Number: EC 3.4.24.71
• Sequence:
  MRGVWPPPVSALLSALGMSTYKRATLDEEDLVDSLSEGDAYPNGLQVNFHSPRSGQRCWA
  ARTQVEKRLVVLVVLLAAGLVACLAALGIQYQTRSPSVCLSEACVSVTSSILSSMDPTVD
  PCHDFFSYACGGWIKANPVPDGHSRWGTFSNLWEHNQAIIKHLLENSTASVSEAERKAQV
  YYRACMNETRIEELRAKPLMELIERLGGWNITGPWAKDNFQDTLQVVTAHYRTSPFFSVY
  VSADSKNSNSNVIQVDQSGLGLPSRDYYLNKTENEKVLTGYLNYMVQLGKLLGGGDEEAI
  RPQMQQILDFETALANITIPQEKRRDEELIYHKVTAAELQTLAPAINWLPFLNTIFYPVE
  INESEPIVVYDKEYLEQISTLINTTDRCLLNNYMIWNLVRKTSSFLDQRFQDADEKFMEV
  MYGTKKTCLPRWKFCVSDTENNLGFALGPMFVKATFAEDSKSIATEIILEIKKAFEESLS
  TLKWMDEETRKSAKEKADAIYNMIGYPNFIMDPKELDKVFNDYTAVPDLYFENAMRFFNF
  SWRVTADQLRKAPNRDQWSMTPPMVNAYYSPTKNEIVFPAGILQAPFYTRSSPKALNFGG
  IGVVVGHELTHAFDDQGREYDKDGNLRPWWKNSSVEAFKRQTECMVEQYSNYSVNGEPVN
  GRHTLGENIADNGGLKAAYRAYQNWVKKNGAEHSLPTLGLTNNQLFFLGFAQVWCSVRTP
  ESSHEGLITDPHSPSRFRVIGSLSNSKEFSEHFRCPPGSPMNPPHKCEVW
• Function: Converts big endothelin-1 to endothelin-1.
• Reactome Pathway: Peptide ligand-binding receptors (R-HSA-375276)

Molecular Interaction Atlas (MIA) of This DTT

1 Discontinued Drug(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
SCH-54470	DMEWLZ7	N. A.	N. A.	Terminated	[1]

9 Investigative Drug(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
5-(2-hydroxyethyl)nonane-1,9-diol	DMHBD1T	Discovery agent	N.A.	Investigative	[2]
CGS 35066	DMCHT27	Discovery agent	N.A.	Investigative	[3]
LY-292223	DML36ZE	Discovery agent	N.A.	Investigative	[4]
PD159790	DM6RVTO	Discovery agent	N.A.	Investigative	[5]
PMID19899765C22	DMBTV20	Discovery agent	N.A.	Investigative	[1]
PO3 2-Ile-Trp-O-3K	DMQMDSG	Discovery agent	N.A.	Investigative	[6]
PO3 2-Leu-Nal-O-3K	DMY43FU	Discovery agent	N.A.	Investigative	[6]
PO3 2-Leu-Trp-O-3K	DM3O78D	Discovery agent	N.A.	Investigative	[6]
PO3 2-Nle-Trp-O-3K	DMW1XY4	Discovery agent	N.A.	Investigative	[6]

References

• [1] Phosphinic tripeptides as dual angiotensin-converting enzyme C-domain and endothelin-converting enzyme-1 inhibitors. J Med Chem. 2010 Jan 14;53(1):208-20.
• [2] The Protein Data Bank. Nucleic Acids Res. 2000 Jan 1;28(1):235-42.
• [3] The 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.
• [4] Endothelin-converting enzyme-1 inhibition and growth of human glioblastoma cells. J Med Chem. 2005 Jan 27;48(2):483-98.
• [5] URL: 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).
• [6] Aminophosphonate endothelin converting enzyme inhibitors: potency-enhancing and selectivity-improving modifications of phosphoramidon, Bioorg. Med. Chem. Lett. 4(10):1257-1262 (1994).