1.17.4.4: vitamin-K-epoxide reductase (warfarin-sensitive)
This is an abbreviated version!
For detailed information about vitamin-K-epoxide reductase (warfarin-sensitive), go to the full flat file.
Word Map on EC 1.17.4.4
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1.17.4.4
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cyp2c9
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anticoagulant
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dosing
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pharmacogenetic
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bleeding
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cyp4f2
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thromboembolic
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k-dependent
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coagulation
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acenocoumarol
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interindividual
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pharmacogenomics
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fibrillation
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gg
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caucasian
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prothrombin
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atrial
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demographic
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pharmacodynamics
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clot
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valve
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ethnic
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thrombosis
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genotype-guided
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s-warfarin
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rodenticides
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gamma-glutamyl
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non-genetic
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phenprocoumon
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warfarin-treated
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4-hydroxycoumarins
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gamma-carboxylase
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coumadin
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pharmacogenes
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medicine
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pivka-ii
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slco1b1
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calumenin
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amiodarone
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genotype-based
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interpatient
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cyp3a5
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hypoprothrombinemia
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undercarboxylated
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clopidogrel
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antivitamin
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gamma-carboxylation
- 1.17.4.4
- cyp2c9
-
anticoagulant
-
dosing
-
pharmacogenetic
-
bleeding
- cyp4f2
-
thromboembolic
-
k-dependent
-
coagulation
-
acenocoumarol
-
interindividual
-
pharmacogenomics
- fibrillation
- gg
-
caucasian
- prothrombin
- atrial
-
demographic
-
pharmacodynamics
- clot
- valve
-
ethnic
- thrombosis
-
genotype-guided
-
s-warfarin
-
rodenticides
-
gamma-glutamyl
-
non-genetic
- phenprocoumon
-
warfarin-treated
- 4-hydroxycoumarins
- gamma-carboxylase
-
coumadin
-
pharmacogenes
- medicine
-
pivka-ii
-
slco1b1
- calumenin
- amiodarone
-
genotype-based
-
interpatient
- cyp3a5
- hypoprothrombinemia
-
undercarboxylated
- clopidogrel
-
antivitamin
-
gamma-carboxylation
Reaction
Synonyms
EC 1.1.4.1, phylloquinone epoxide reductase, reductase, phylloquinone epoxide, vitamin K 2,3-epoxide reductase, vitamin K 2,3-epoxide reductase complex subunit 1, vitamin K 2,3-epoxide reductase complex subunit-1, vitamin K epoxid reductase, vitamin K epoxide reductase, vitamin K epoxide reductase complex subunit 1, vitamin K oxidoreductase, Vitamin K reductase, vitamin K-2,3-epoxide reductase, vitamin K-2,3-epoxide reductase subunit 1, vitamin K-epoxide reductase, vitamin K1 epoxide reductase, vitaminK epoxide reductase, VKOR, VKOR complex, VKORC1, VKORC1 variant 2, VKORC1-like 1, VKORC1L1, VKORC1v2, warfarin sensitive vitamin K 2,3-epoxide reductase, warfarin-sensitive vitamin K1 2,3-epoxide reductase
ECTree
1.17.4.4 vitamin-K-epoxide reductase (warfarin-sensitive)Advanced search results
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results (Inhibitors
Inhibitors on EC 1.17.4.4 - vitamin-K-epoxide reductase (warfarin-sensitive)
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INHIBITOR 
ORGANISM
UNIPROT
COMMENTARY 
LITERATURE
IMAGE
2,3,5,6-Tetrachloro-4-pyridinol
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2.0 mM, 45% inhibition, warfarin-resistant rats
2-hydroxy-3-(3-methyl-2-butenyl)-1,4-naphthoquinone
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trivial name lapachol, 0.002 mM, 50% inhibition, liver microsomes from normal-strain, inhibition is fully reversible; trivial name lapachol, 50% inhibition of KO reductase activity in whole liver microsomes of warfarin-resistant rats, inhibition is fully reversible
miR-133a
micro-RNA, miR-133a interacts with the 3'-UTR of VKORC1. Transfection of miRNA precursors of miR-133a in HepG2 cells reduces VKORC1 mRNA expression in a dose-dependent manner, quantitative RT-PCR expression analysis, overview. miR-133a levels correlate inversely with VKORC1 mRNA levels in 23 liver samples from healthy subjects. In silico identification of VKORC1 miRNA binding sites, overview
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potassium cholate
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0.5% (w/v) potassium cholate releases nearly 60% of the VKOR activity originally present in intact microsomes
Vitamin K 2,3-epoxide analogs
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hydroxymethyl-, chloromethyl-, fluoromethyl-, difluoromethyl-, formyl-analogs and analogs with modified phytyl chain, competitive inhibition
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Deriphat 160
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Deriphat 160 is an efficient detergent for the solubilization of VKOR, but the enzyme is inactive in its presence
N-ethylmaleimide
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inhibition increased if the enzyme is prereduced by DTT, 1,4-butanedithiol or 1,2-ethanediol
phenprocoumon
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4-hydroxycoumarin-derived anticoagulation drug, blocks the recycling of vitamin K epoxid inhibiting the two dithiol-dependent steps performed by the enzyme
warfarin
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determination of warfarin metabolic rate in liver microsomes based on P450 content, overview. Conversion to 4-, 6-, 7- and 10-hydroxylated warfarin
warfarin
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determination of warfarin metabolic rate in liver microsomes based on P450 content, overview. Conversion to 4-, 6-, and 8-hydroxylated warfarin
warfarin
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determination of warfarin metabolic rate in liver microsomes based on P450 content, overview. Conversion to 4-, 6-, and 8-hydroxylated warfarin
warfarin
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determination of warfarin metabolic rate in liver microsomes based on P450 content, overview. Conversion to 4-, 6-, 7-, 8- and 10-hydroxylated warfarin
warfarin
mutations in VKORC1 cause warfarin resistance and multiple coagulation factor deficiency type 2
warfarin
the enzyme is the therapeutic target site for warfarin, an anticoagulant that is prescribed widely for the treatment and prevention of thrombosis. Point mutations in VKORC1 may be an important, though rare, cause of warfarin resistance in anticoagulation clinic populations. V66M mutation is responsible for warfarin resistance phenotype
warfarin
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4-hydroxycoumarin-derived anticoagulation drug, blocks the recycling of vitamin K epoxid inhibiting the two dithiol-dependent steps performed by the enzyme
warfarin
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acts by blocking vitamin K at the active site of the enzyme and thereby effectively blocking the initial step
warfarin
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non-competitive inhibitor, displacement of the warfarin binding site away from the vitamin K binding site by at least one turn of the transmembrane helix. The fully extended phenyl group of S-warfarin may interact with the phenyl fragment of Tyr139 of VKOR in a stacking configuration. Binding of S-warfarin to VKOR in the presence of vitamin K could modify, i.e. reduce the rate of flip-flop of lipid membrane, ultimately leading to the decrease of the amount of the vitamin K hydroquinone form
warfarin
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hVKOR is directly and irreversibly inhibited by warfarin, hVKOR is the target of a common anticoagulant, warfarin. Tyr139 in hVKOR is part of the warfarin binding site
warfarin
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the oral anticoagulant impairs the synthesis of functional clotting factors through inhibition of VKOR and is widely used for prevention and treatment of thrombosis
warfarin
mutants V29L, V45A, and L128R are resistant to inhibition by warfarin in vivo, oveview; VKORC1 function is measured in vitro using a dithiothreitol-driven vitamin K 2,3-epoxide reductase assay. Warfarin inhibits wild-type VKORC1 function by the DTTVKOR assay. However, VKORC1 variants with warfarin resistance-associated missense mutations often show low VKOR activities and warfarin sensitivity instead of resistance
warfarin
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overnight treatment with the drug produces similar phenotypes to 7 days of siRNA-mediated VKOR depletion
warfarin
traps human vitamin K epoxide reductase in an intermediate state during electron transfer
warfarin
warfarin inhibits androgen receptor activity (an important driver of prostate cancer development and progression) by inhibiting vitamin K epoxide reductase
warfarin
warfarin inhibits androgen receptor activity (an important driver of prostate cancer development and progression) by inhibiting vitamin K epoxide reductase
warfarin
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i.e. 3-(alpha-acetonylbenzyl)-4-hydroxycoumarin, inhibition decreased by DTT
warfarin
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0.01 mM, 18% inhibition, 0.1 mM, 64% inhibition, warfarin-resistant rats
warfarin
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0.0017 mM, 50% inhibition; mixed non-competitive inhibition vs. vitamin k 2,3-epoxide, competive inhibition vs. DTT
warfarin
the mutant Y139F strain is resistant to warfarin; wild-type rats
warfarin
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i.e. 3-(alpha-acetonylbenzyl)-4-hydroxycoumarin, VKOR is highly sensitive to inhibition by warfarin
warfarin
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determination of warfarin metabolic rate in liver microsomes based on P450 content, overview. Conversion to 4-, 6-, 7-, 8- and 10-hydroxylated warfarin
warfarin
the inhibition effect of warfarin on the enzyme activity is neutralized when it was coadministered with puerarin in rats
warfarin
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determination of warfarin metabolic rate in liver microsomes based on P450 content, overview. Conversion to 4-, 6-, 7-, and 8-hydroxylated warfarin
additional information
pharmacodynamics of resistance to warfarin, overview
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additional information
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mechanism of 4-hydroxycoumarin derivative-resistance, overview
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