vitamin K epoxide reductase complex subunit 1

Target id: 2645

Nomenclature: vitamin K epoxide reductase complex subunit 1

Family: 1.-.-.- Oxidoreductases

Annotation status:  image of a grey circle Awaiting annotation/under development. Please contact us if you can help with annotation.  » Email us

   GtoImmuPdb view: OFF :     Currently no data for vitamin K epoxide reductase complex subunit 1 in GtoImmuPdb

Gene and Protein Information
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human - 163 16p11.2 VKORC1 vitamin K epoxide reductase complex subunit 1
Mouse - 161 7 F3 Vkorc1 vitamin K epoxide reductase complex
Rat - 161 1q36 Vkorc1 vitamin K epoxide reductase complex
Previous and Unofficial Names
vitamin K epoxide reductase complex, subunit 1 | vitamin K epoxide reductase complex
Database Links
BRENDA
ChEMBL Target
DrugBank Target
Ensembl Gene
Entrez Gene
GenitoUrinary Development Molecular Anatomy Project
Human Protein Atlas
KEGG Enzyme
KEGG Gene
OMIM
Orphanet
RefSeq Nucleotide
RefSeq Protein
UniProtKB
Wikipedia
Enzyme Reaction
EC Number: 1.1.4.1

Download all structure-activity data for this target as a CSV file

Inhibitors
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Affinity Units Reference
warfarin Hs Inhibition 5.6 pKi 1
pKi 5.6 (Ki 2.633x10-6 M) [1]
acenocoumarol Rn Inhibition 6.1 pIC50 3
pIC50 6.1 (IC50 7.7x10-7 M) [3]
alitretinoin Hs Inhibition - - 5,8
[5,8]
dicumarol Hs Inhibition - - 4
[4]
phenindione Hs Inhibition - - 2,7
[2,7]
phenprocoumon Hs Inhibition - - 2
[2]
View species-specific inhibitor tables
Clinically-Relevant Mutations and Pathophysiology
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. Acta1830 (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 J66 (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. Nature427 (6974): 537-41. [PMID:14765194]

7. TOOHEY M. (1952) Antagonism of anticoagulants dicoumarol, tromexan, and phenylindandione by vitamin K. Br Med J2 (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 17/12/2017. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=2645.