Target Information
Target General Infomation | |||||
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Target ID |
T11843
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Former ID |
TTDS00398
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Target Name |
Vitamin K epoxide reductase complex subunit 1
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Gene Name |
VKORC1
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Synonyms |
MSTP134; MSTP576; UNQ308/PRO351; VKOR; Vitamin K1 2,3-epoxide reductase subunit 1; VKORC1
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Target Type |
Successful
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Disease | Atrial fibrillation [ICD9: 272, 427.31; ICD10: E78, I48] | ||||
Bleeding; Thromboembolism [ICD9:444, 453, 437.6, 671.5, 671.9; ICD10: I74, I80-I82] | |||||
Cerebrovascular ischaemia [ICD9: 434.91; ICD10: I61-I63] | |||||
Pulmonary embolism; Blood clotting disorder [ICD9:415.1, 286; ICD10: I26, D65-D69] | |||||
Thrombosis [ICD9: 437.6, 453, 671.5, 671.9; ICD10: I80-I82] | |||||
Function |
Involved invitamin K metabolism. Catalytic subunit of the vitamin K epoxide reductase (VKOR) complex which reduces inactive vitamin K 2,3-epoxide to active vitamin K. Vitamin K is required for the gamma-carboxylation of various proteins, including clotting factors, and is required for normal blood coagulation, but also for normal bone development.
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BioChemical Class |
Short-chain dehydrogenases reductases
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Target Validation |
T11843
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UniProt ID | |||||
EC Number |
EC 1.1.4.1
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Sequence |
MGSTWGSPGWVRLALCLTGLVLSLYALHVKAARARDRDYRALCDVGTAISCSRVFSSRWG
RGFGLVEHVLGQDSILNQSNSIFGCIFYTLQLLLGCLRTRWASVLMLLSSLVSLAGSVYL AWILFFVLYDFCIVCITTYAINVSLMWLSFRKVQEPQGKAKRH |
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Drugs and Mode of Action | |||||
Drug(s) | Acenocoumarol | Drug Info | Approved | Thrombosis | [550766] |
Dicumarol | Drug Info | Approved | Bleeding; Thromboembolism | [541890], [550685], [551871] | |
Phenindione | Drug Info | Approved | Pulmonary embolism; Blood clotting disorder | [541918], [550721], [551871] | |
Phenprocoumon | Drug Info | Approved | Thrombosis | [538444], [541919], [551871] | |
Warfarin | Drug Info | Approved | Atrial fibrillation | [536186], [541933] | |
Tecarfarin | Drug Info | Phase 3 | Cerebrovascular ischaemia | [525289] | |
Target Expression Profile (TEP) and Drug Resistance Mutation (DRM) | |||||
DRM | DRM Info | ||||
Pathways | |||||
KEGG Pathway | Ubiquinone and other terpenoid-quinone biosynthesis | ||||
PathWhiz Pathway | Vitamin K Metabolism | ||||
Coagulation | |||||
WikiPathways | gamma carboxylation, hypusine formation and arylsulfatase activation | ||||
References | |||||
Ref 536186 | Emerging drugs in peripheral arterial disease. Expert Opin Emerg Drugs. 2006 Mar;11(1):75-90. | ||||
Ref 538444 | FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (NDA) 011228. | ||||
Ref 541890 | (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: 6808). | ||||
Ref 541918 | (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: 6838). | ||||
Ref 541919 | (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: 6839). | ||||
Ref 531029 | Tecarfarin, a novel vitamin K reductase antagonist, is not affected by CYP2C9 and CYP3A4 inhibition following concomitant administration of fluconazole in healthy participants. J Clin Pharmacol. 2011Apr;51(4):561-74. | ||||
Ref 536520 | Oral anticoagulation and pharmacogenetics: importance in the clinical setting. Rev Med Suisse. 2007 Sep 12;3(124):2030, 2033-4, 2036. | ||||
Ref 537085 | Genotypes associated with reduced activity of VKORC1 and CYP2C9 and their modification of acenocoumarol anticoagulation during the initial treatment period. Clin Pharmacol Ther. 2009 Apr;85(4):379-86. Epub 2009 Feb 18. |
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