Top ▲

vitamin K epoxide reductase complex subunit 1

Click here for help

Target not currently curated in GtoImmuPdb

Target id: 2645

Nomenclature: vitamin K epoxide reductase complex subunit 1

Family: 1.-.-.- Oxidoreductases

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
BRENDA
ChEMBL Target
DrugBank Target
Ensembl Gene
Entrez Gene
Human Protein Atlas
KEGG Enzyme
KEGG Gene
OMIM
Orphanet
Pharos
RefSeq Nucleotide
RefSeq Protein
UniProtKB
Wikipedia
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

Show »

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 07/12/2021. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=2645.