Target Information
| Target General Infomation | |||||
|---|---|---|---|---|---|
| Target ID |
T50970
|
||||
| Former ID |
TTDR00135
|
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| Target Name |
Endothelin-converting enzyme 1
|
||||
| Gene Name |
ECE1
|
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| Synonyms |
ECE-1; ECE1
|
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| Target Type |
Discontinued
|
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| Function |
Converts big endothelin-1 to endothelin-1.
|
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| BioChemical Class |
Peptidase
|
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| Target Validation |
T50970
|
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| UniProt ID | |||||
| EC Number |
EC 3.4.24.71
|
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| Sequence |
MRGVWPPPVSALLSALGMSTYKRATLDEEDLVDSLSEGDAYPNGLQVNFHSPRSGQRCWA
ARTQVEKRLVVLVVLLAAGLVACLAALGIQYQTRSPSVCLSEACVSVTSSILSSMDPTVD PCHDFFSYACGGWIKANPVPDGHSRWGTFSNLWEHNQAIIKHLLENSTASVSEAERKAQV YYRACMNETRIEELRAKPLMELIERLGGWNITGPWAKDNFQDTLQVVTAHYRTSPFFSVY VSADSKNSNSNVIQVDQSGLGLPSRDYYLNKTENEKVLTGYLNYMVQLGKLLGGGDEEAI RPQMQQILDFETALANITIPQEKRRDEELIYHKVTAAELQTLAPAINWLPFLNTIFYPVE INESEPIVVYDKEYLEQISTLINTTDRCLLNNYMIWNLVRKTSSFLDQRFQDADEKFMEV MYGTKKTCLPRWKFCVSDTENNLGFALGPMFVKATFAEDSKSIATEIILEIKKAFEESLS TLKWMDEETRKSAKEKADAIYNMIGYPNFIMDPKELDKVFNDYTAVPDLYFENAMRFFNF SWRVTADQLRKAPNRDQWSMTPPMVNAYYSPTKNEIVFPAGILQAPFYTRSSPKALNFGG IGVVVGHELTHAFDDQGREYDKDGNLRPWWKNSSVEAFKRQTECMVEQYSNYSVNGEPVN GRHTLGENIADNGGLKAAYRAYQNWVKKNGAEHSLPTLGLTNNQLFFLGFAQVWCSVRTP ESSHEGLITDPHSPSRFRVIGSLSNSKEFSEHFRCPPGSPMNPPHKCEVW |
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| Drugs and Mode of Action | |||||
| Drug(s) | SCH-54470 | Drug Info | Terminated | Discovery agent | [1] |
| Inhibitor | 5-(2-hydroxyethyl)nonane-1,9-diol | Drug Info | [2] | ||
| CGS 35066 | Drug Info | [3] | |||
| compound 22 | Drug Info | [4] | |||
| LY-292223 | Drug Info | [5] | |||
| PD159790 | Drug Info | [6] | |||
| PO3 2-Ile-Trp-O-3K | Drug Info | [7] | |||
| PO3 2-Leu-Nal-O-3K | Drug Info | [7] | |||
| PO3 2-Leu-Trp-O-3K | Drug Info | [7] | |||
| PO3 2-Nle-Trp-O-3K | Drug Info | [7] | |||
| SCH-54470 | Drug Info | [4] | |||
| Pathways | |||||
| PANTHER Pathway | Endothelin signaling pathway | ||||
| WikiPathways | SIDS Susceptibility Pathways | ||||
| Corticotropin-releasing hormone | |||||
| Endothelin Pathways | |||||
| References | |||||
| REF 1 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800007872) | ||||
| REF 2 | The Protein Data Bank. Nucleic Acids Res. 2000 Jan 1;28(1):235-42. | ||||
| REF 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. | ||||
| REF 4 | J 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 5 | J Med Chem. 2005 Jan 27;48(2):483-98.Endothelin-converting enzyme-1 inhibition and growth of human glioblastoma cells. | ||||
| REF 6 | (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 7 | Aminophosphonate endothelin converting enzyme inhibitors: potency-enhancing and selectivity-improving modifications of phosphoramidon, Bioorg. Med. Chem. Lett. 4(10):1257-1262 (1994). | ||||
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