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vitamin K epoxide reductase complex subunit 1

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Target id: 2645

Nomenclature: vitamin K epoxide reductase complex subunit 1

Family: 1.-.-.- Oxidoreductases

Contents:

Gene and Protein Information Click here for help
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human 4 163 16p11.2 VKORC1 vitamin K epoxide reductase complex subunit 1
Mouse 4 161 7 69.81 cM Vkorc1 vitamin K epoxide reductase complex, subunit 1
Rat 4 161 1q37 Vkorc1 vitamin K epoxide reductase complex, subunit 1
Previous and Unofficial Names Click here for help
vitamin K epoxide reductase complex, subunit 1 | vitamin K epoxide reductase complex
Database Links Click here for help
Alphafold Q9BQB6 (Hs), Q9CRC0 (Mm), Q6TEK4 (Rn)
BRENDA 1.1.4.1
ChEMBL Target CHEMBL1930 (Hs), CHEMBL4105870 (Rn)
DrugBank Target Q9BQB6 (Hs)
Ensembl Gene ENSG00000167397 (Hs), ENSMUSG00000096145 (Mm), ENSRNOG00000050828 (Rn)
Entrez Gene 79001 (Hs), 27973 (Mm), 309004 (Rn)
Human Protein Atlas ENSG00000167397 (Hs)
KEGG Enzyme 1.1.4.1
KEGG Gene hsa:79001 (Hs), mmu:27973 (Mm), rno:309004 (Rn)
OMIM 608547 (Hs)
Orphanet ORPHA159472 (Hs)
Pharos Q9BQB6 (Hs)
RefSeq Nucleotide NM_024006 (Hs), NM_178600 (Mm), NM_203335 (Rn)
RefSeq Protein NP_076869 (Hs), NP_848715 (Mm), NP_976080 (Rn)
UniProtKB Q9BQB6 (Hs), Q9CRC0 (Mm), Q6TEK4 (Rn)
Wikipedia VKORC1 (Hs)
Enzyme Reaction Click here for help
EC Number: 1.1.4.1

Download all structure-activity data for this target as a CSV file go icon to follow link

Inhibitors
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Value Parameter Reference
warfarin Small molecule or natural product Approved drug Primary target of this compound Hs Inhibition 5.6 pKi 1
⤷ pKi 5.6 (Ki 2.633x10-6 M) [1]
acenocoumarol Small molecule or natural product Approved drug Rn Inhibition 6.1 pIC50 3
⤷ pIC50 6.1 (IC50 7.7x10-7 M) [3]
alitretinoin Small molecule or natural product Approved drug Primary target of this compound Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition - - 5,8
⤷ [5,8]
dicumarol Small molecule or natural product Approved drug Primary target of this compound Hs Inhibition - - 4
⤷ [4]
phenindione Small molecule or natural product Approved drug Primary target of this compound Ligand has a PDB structure Hs Inhibition - - 2,7
⤷ [2,7]
phenprocoumon Small molecule or natural product Approved drug Primary target of this compound Hs Inhibition - - 2
⤷ [2]
View species-specific inhibitor tables
Clinically-Relevant Mutations and Pathophysiology Click here for help
Disease:  Vitamin K-dependent clotting factors, combined deficiency of, 2; VKCFD2
Synonyms: Hereditary combined deficiency of vitamin K-dependent clotting factors [Orphanet: ORPHA98434]
OMIM: 607473
Orphanet: ORPHA98434
References:  6
Click column headers to sort
Type Species Amino acid change Nucleotide change Description Reference
Missense Human R98W 292C>T 6
Disease:  Warfarin resistance
Synonyms: Coumarin resistance [OMIM: 122700]
OMIM: 122700

References

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1. Bevans CG, Krettler C, Reinhart C, Tran H, Koßmann K, Watzka M, Oldenburg J. (2013) Determination of the warfarin inhibition constant Ki for vitamin K 2,3-epoxide reductase complex subunit-1 (VKORC1) using an in vitro DTT-driven assay. Biochim Biophys Acta, 1830 (8): 4202-10. [PMID:23618698]

2. FIELD JB, GOLDFARB MS, WARE AG, GRIFFITH GC. (1952) Effect in man of a new indandione anticoagulant. Proc Soc Exp Biol Med, 81 (3): 678-81. [PMID:13037763]

3. Gebauer M. (2007) Synthesis and structure-activity relationships of novel warfarin derivatives. Bioorg Med Chem, 15 (6): 2414-20. [PMID:17275317]

4. Hollman A. (1991) Dicoumarol and warfarin. Br Heart J, 66 (2): 181. [PMID:18610395]

5. Keller C, Matzdorff AC, Kemkes-Matthes B. (1999) Pharmacology of warfarin and clinical implications. Semin Thromb Hemost, 25 (1): 13-6. [PMID:10327215]

6. Rost S, Fregin A, Ivaskevicius V, Conzelmann E, Hörtnagel K, Pelz HJ, Lappegard K, Seifried E, Scharrer I, Tuddenham EG et al.. (2004) Mutations in VKORC1 cause warfarin resistance and multiple coagulation factor deficiency type 2. Nature, 427 (6974): 537-41. [PMID:14765194]

7. TOOHEY M. (1952) Antagonism of anticoagulants dicoumarol, tromexan, and phenylindandione by vitamin K. Br Med J, 2 (4786): 687-90. [PMID:12978288]

8. Wallin R, Wajih N, Hutson SM. (2008) VKORC1: a warfarin-sensitive enzyme in vitamin K metabolism and biosynthesis of vitamin K-dependent blood coagulation factors. Vitam Horm, 78: 227-46. [PMID:18374197]

How to cite this page

1.-.-.- Oxidoreductases: vitamin K epoxide reductase complex subunit 1. Last modified on 05/02/2016. Accessed on 16/04/2024. IUPHAR/BPS Guide to PHARMACOLOGY, https://www.guidetomalariapharmacology.org/GRAC/ObjectDisplayForward?objectId=2645.