Target Information
Target General Infomation | |||||
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Target ID |
T12819
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Former ID |
TTDI01954
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Target Name |
E3 ubiquitin protein ligase COP1
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Gene Name |
RFWD2
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Synonyms |
Constitutive photomorphogenesis protein 1 homolog; E3 ubiquitinprotein ligase RFWD2; RING finger and WD repeat domain protein 2; RING finger protein 200; hCOP1; RFWD2
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Target Type |
Successful
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Disease | Heart arrhythmia [ICD10: I47-I49] | ||||
Malaria [ICD10: B54] | |||||
Tachyarrhythmias [ICD9: 427, 785.0; ICD10: I47-I49, R00.0] | |||||
Ventricular arrhythmias [ICD9: 427.1; ICD10: I47.2] | |||||
Function |
E3 ubiquitin-protein ligase that mediates ubiquitination and subsequent proteasomal degradation of target proteins. E3 ubiquitin ligases accept ubiquitin from an E2 ubiquitin- conjugating enzyme in the form of a thioester and then directly transfers the ubiquitin to targeted substrates. Involved in JUN ubiquitination and degradation. Directly involved in p53 (TP53) ubiquitination and degradation, thereby abolishing p53-dependent transcription and apoptosis. Ubiquitinates p53 independently of MDM2 or RCHY1. Probably mediates E3 ubiquitin ligase activity by functioning as the essential RING domain subunit of larger E3 complexes. In contrast, it does not constitute the catalytic RING subunit in the DCX DET1-COP1 complex that negatively regulates JUN, the ubiquitin ligase activity being mediated by RBX1. Involved in 14-3-3 proteinsigma/SFN ubiquitination and proteasomal degradation, leading to AKT activation and promotion of cell survival. Ubiquitinates MTA1 leading to its proteasomal degradation.
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BioChemical Class |
Carbon-nitrogen ligase
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UniProt ID | |||||
EC Number |
EC 6.3.2.-
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Sequence |
MSGSRQAGSGSAGTSPGSSAASSVTSASSSLSSSPSPPSVAVSAAALVSGGVAQAAGSGG
LGGPVRPVLVAPAVSGSGGGAVSTGLSRHSCAARPSAGVGGSSSSLGSGSRKRPLLAPLC NGLINSYEDKSNDFVCPICFDMIEEAYMTKCGHSFCYKCIHQSLEDNNRCPKCNYVVDNI DHLYPNFLVNELILKQKQRFEEKRFKLDHSVSSTNGHRWQIFQDWLGTDQDNLDLANVNL MLELLVQKKKQLEAESHAAQLQILMEFLKVARRNKREQLEQIQKELSVLEEDIKRVEEMS GLYSPVSEDSTVPQFEAPSPSHSSIIDSTEYSQPPGFSGSSQTKKQPWYNSTLASRRKRL TAHFEDLEQCYFSTRMSRISDDSRTASQLDEFQECLSKFTRYNSVRPLATLSYASDLYNG SSIVSSIEFDRDCDYFAIAGVTKKIKVYEYDTVIQDAVDIHYPENEMTCNSKISCISWSS YHKNLLASSDYEGTVILWDGFTGQRSKVYQEHEKRCWSVDFNLMDPKLLASGSDDAKVKL WSTNLDNSVASIEAKANVCCVKFSPSSRYHLAFGCADHCVHYYDLRNTKQPIMVFKGHRK AVSYAKFVSGEEIVSASTDSQLKLWNVGKPYCLRSFKGHINEKNFVGLASNGDYIACGSE NNSLYLYYKGLSKTLLTFKFDTVKSVLDKDRKEDDTNEFVSAVCWRALPDGESNVLIAAN SQGTIKVLELV |
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Drugs and Mode of Action | |||||
Drug(s) | Flecainide | Drug Info | Approved | Tachyarrhythmias | [538298], [539654] |
Procainamide | Drug Info | Approved | Ventricular arrhythmias | [468043], [538376] | |
Propafenone | Drug Info | Approved | Tachyarrhythmias | [536095], [539655] | |
Quinine | Drug Info | Approved | Malaria | [538576], [539633] | |
Tocainide | Drug Info | Approved | Ventricular arrhythmias | [538501], [542331] | |
Barucainide | Drug Info | Terminated | Heart arrhythmia | [544576] | |
Pathways | |||||
KEGG Pathway | p53 signaling pathway | ||||
Ubiquitin mediated proteolysis | |||||
PANTHER Pathway | P53 pathway feedback loops 1 | ||||
Pathway Interaction Database | ATM pathway | ||||
Direct p53 effectors | |||||
p53 pathway | |||||
References | |||||
Ref 468043 | (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. (Ligand id: 4811). | ||||
Ref 536095 | New antiarrhythmic agents for atrial fibrillation and atrial flutter. Expert Opin Emerg Drugs. 2005 May;10(2):311-22. | ||||
Ref 538298 | FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (ANDA) 075442. | ||||
Ref 538376 | FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (ANDA) 089257. | ||||
Ref 538501 | FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (NDA) 018257. | ||||
Ref 538576 | FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (NDA) 021799. | ||||
Ref 539633 | (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. (Ligand id: 2510). | ||||
Ref 539654 | (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. (Ligand id: 2560). | ||||
Ref 539655 | (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. (Ligand id: 2561). |
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