Target Information

Target General Infomation
Target ID
T11843
Former ID
TTDS00398
Target Name
Vitamin K epoxide reductase complex subunit 1
Gene Name
VKORC1
Synonyms
MSTP134; MSTP576; UNQ308/PRO351; VKOR; Vitamin K1 2,3-epoxide reductase subunit 1; VKORC1
Target Type
Successful
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.
BioChemical Class
Short-chain dehydrogenases reductases
Target Validation
T11843
UniProt ID
Q9BQB6
EC Number
EC 1.1.4.1
Sequence
MGSTWGSPGWVRLALCLTGLVLSLYALHVKAARARDRDYRALCDVGTAISCSRVFSSRWG
RGFGLVEHVLGQDSILNQSNSIFGCIFYTLQLLLGCLRTRWASVLMLLSSLVSLAGSVYL
AWILFFVLYDFCIVCITTYAINVSLMWLSFRKVQEPQGKAKRH
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]
Inhibitor Acenocoumarol Drug Info [536520], [537085], [537545]
Dicumarol Drug Info [537681]
Phenindione Drug Info [536520]
Phenprocoumon Drug Info [536520]
Tecarfarin Drug Info [531029]
Warfarin Drug Info [536520]
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 525289ClinicalTrials.gov (NCT02522221) Tecarfarin Anti-Coagulation Trial (TACT).
Ref 536186Emerging drugs in peripheral arterial disease. Expert Opin Emerg Drugs. 2006 Mar;11(1):75-90.
Ref 538444FDA 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 541933(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: 6853).
Ref 550685Drug information of Dicumarol, 2008. eduDrugs.
Ref 550721Drug information of Phenindione, 2008. eduDrugs.
Ref 550766Drug information of Acenocoumarol, 2008. eduDrugs.
Ref 551871Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015
Ref 531029Tecarfarin, 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 536520Oral anticoagulation and pharmacogenetics: importance in the clinical setting. Rev Med Suisse. 2007 Sep 12;3(124):2030, 2033-4, 2036.
Ref 537085Genotypes 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.
Ref 537545Evaluation of a reverse-hybridization StripAssay for the detection of genetic polymorphisms leading to acenocoumarol sensitivity. Mol Biol Rep. 2009 Jun 28.
Ref 537681Vitamin K antagonism of coumarin intoxication in the rat. Thromb Haemost. 1986 Apr 30;55(2):235-9.

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