General Information of Drug Therapeutic Target (DTT) (ID: TTEUC8H)

DTT Name Vitamin K epoxide reductase complex 1 (VKORC1)
Synonyms Vitamin K1 2,3-epoxide reductase subunit 1; VKORC1; VKOR; UNQ308/PRO351; MSTP576; MSTP134
Gene Name VKORC1
DTT Type
Successful target
[1]
BioChemical Class
Short-chain dehydrogenases reductase
UniProt ID
VKOR1_HUMAN
TTD ID
T11843
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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EC Number
EC 1.17.4.4
Sequence
MGSTWGSPGWVRLALCLTGLVLSLYALHVKAARARDRDYRALCDVGTAISCSRVFSSRWG
RGFGLVEHVLGQDSILNQSNSIFGCIFYTLQLLLGCLRTRWASVLMLLSSLVSLAGSVYL
AWILFFVLYDFCIVCITTYAINVSLMWLSFRKVQEPQGKAKRH
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.
KEGG Pathway
Ubiquinone and other terpenoid-quinone biosynthesis (hsa00130 )
Reactome Pathway
Metabolism of vitamin K (R-HSA-6806664 )
BioCyc Pathway
MetaCyc:HS15548-MON

Molecular Interaction Atlas (MIA) of This DTT

Molecular Interaction Atlas (MIA) Jump to Detail Molecular Interaction Atlas of This DTT
5 Approved Drug(s) Targeting This DTT
Drug Name Drug ID Indication ICD 11 Highest Status REF
Acenocoumarol DMH75KV Thrombosis DB61-GB90 Approved [2]
Dicumarol DMFQCB1 Bleeding disorder GA20-GA21 Approved [1]
Phenindione DM2PYNR Coagulation defect 3B10.0 Approved [3]
Phenprocoumon DMDO279 Myocardial infarction BA41-BA43 Approved [3]
Warfarin DMJYCVW Atrial fibrillation BC81.3 Approved [3]
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1 Clinical Trial Drug(s) Targeting This DTT
Drug Name Drug ID Indication ICD 11 Highest Status REF
Tecarfarin DMTCR2O Cerebrovascular ischaemia 8B1Z Phase 3 [4]
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The Drug-Metabolizing Enzyme (DME) Role of This DTT

DTT DME Name Vitamin K1 2,3-epoxide reductase 1 (VKOR) DME Info
Gene Name VKORC1
1 Approved Drug(s) Metabolized by This DTT
Drug Name Drug ID Indication ICD 11 Highest Status REF
Menadiol sodium diphosphate DMP9N85 Coagulation defect 3B10.0 Approved [5]
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1 Investigative Drug(s) Metabolized by This DTT
Drug Name Drug ID Indication ICD 11 Highest Status REF
Vitamin K DMN6EZY Discovery agent N.A. Investigative [6]
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References

1 Vitamin K antagonism of coumarin intoxication in the rat. Thromb Haemost. 1986 Apr 30;55(2):235-9.
2 Evaluation of a reverse-hybridization StripAssay for the detection of genetic polymorphisms leading to acenocoumarol sensitivity. Mol Biol Rep. 2010 Apr;37(4):1693-7.
3 [Oral anticoagulation and pharmacogenetics: importance in the clinical setting]. Rev Med Suisse. 2007 Sep 12;3(124):2030, 2033-4, 2036.
4 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.
5 SMPDB database: Vitamin K Metabolism
6 VKORC1L1, an enzyme mediating the effect of vitamin K in liver and extrahepatic tissues. Nutrients. 2018 Jul 26;10(8). pii: E970.