Details of the Drug Therapeutic Target (DTT)

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	Download 2D Sequence (FASTA) Download 3D Structure (PDB) Download
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.