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Literature summary extracted from

  • Fregin, A.; Czogalla, K.J.; Gansler, J.; Rost, S.; Taverna, M.; Watzka, M.; Bevans, C.G.; Mueller, C.R.; Oldenburg, J.
    A new cell culture-based assay quantifies vitamin K 2,3-epoxide reductase complex subunit 1 function and reveals warfarin resistance phenotypes not shown by the dithiothreitol-driven VKOR assay (2013), J. Thromb. Haemost., 11, 872-880.
    View publication on PubMed

Cloned(Commentary)

EC Number Cloned (Comment) Organism
1.17.4.4 coexpression of human coagulation factor (F)IX and c-myc-tagged VKORC1 mutant variants in HEK-293T cells in presence of varying warfarin concentrations Homo sapiens
1.17.4.4 coexpression of human coagulation factor (F)IX andc-myc-tagged VKORC1 wild-type and mutants in HEK-293T cells in presence of varying warfarin concentrations Homo sapiens

Protein Variants

EC Number Protein Variants Comment Organism
1.17.4.4 L128R site-directed mutagenesis, the mutant is resistant to warfarin and oral anti-coagulants Homo sapiens
1.17.4.4 additional information construction of warfarin-resistant VKORC1 variants following naturally occuring mutations in patients Homo sapiens
1.17.4.4 V29L site-directed mutagenesis, the mutant is resistant to warfarin and oral anti-coagulants Homo sapiens
1.17.4.4 V45A site-directed mutagenesis, the mutant is resistant to warfarin and oral anti-coagulants Homo sapiens

Inhibitors

EC Number Inhibitors Comment Organism Structure
1.17.4.4 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 DTT–VKOR assay. However, VKORC1 variants with warfarin resistance-associated missense mutations often show low VKOR activities and warfarin sensitivity instead of resistance Homo sapiens

Natural Substrates/ Products (Substrates)

EC Number Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
1.17.4.4 2,3-epoxy-2,3-dihydro-2-methyl-3-phytyl-1,4-naphthoquinone + 1,4-dithiothreitol + H2O Homo sapiens
-
 2-methyl-3-phytyl-1,4-naphthoquinone + oxidized dithiothreitol
-
 ?
1.17.4.4 2,3-epoxy-2,3-dihydro-2-methyl-3-phytyl-1,4-naphthoquinone + 1,4-dithiothreitol + H2O Homo sapiens
-
 2-methyl-3-phytyl-1,4-naphthoquinone + oxidized dithiothreitol
-
 r
1.17.4.4 2-methyl-3-phytyl-1,4-naphthoquinone + oxidized dithiothreitol + H2O Homo sapiens
-
 2,3-epoxy-2,3-dihydro-2-methyl-3-phytyl-1,4-naphthoquinone + 1,4-dithiothreitol
-
 ?
1.17.4.4 2-methyl-3-phytyl-1,4-naphthoquinone + oxidized dithiothreitol + H2O Homo sapiens
-
 2,3-epoxy-2,3-dihydro-2-methyl-3-phytyl-1,4-naphthoquinone + 1,4-dithiothreitol
-
 r

Organism

EC Number Organism UniProt Comment Textmining
1.17.4.4 Homo sapiens Q9BQB6
-
-
1.17.4.4 Homo sapiens Q9BQB6 mutants V29L, V45A, and L128R, oveview
-

Source Tissue

EC Number Source Tissue Comment Organism Textmining
1.17.4.4 HEK-293T cell
-
 Homo sapiens
-

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
1.17.4.4 2,3-epoxy-2,3-dihydro-2-methyl-3-phytyl-1,4-naphthoquinone + 1,4-dithiothreitol + H2O
-
 Homo sapiens 2-methyl-3-phytyl-1,4-naphthoquinone + oxidized dithiothreitol
-
 ?
1.17.4.4 2,3-epoxy-2,3-dihydro-2-methyl-3-phytyl-1,4-naphthoquinone + 1,4-dithiothreitol + H2O
-
 Homo sapiens 2-methyl-3-phytyl-1,4-naphthoquinone + oxidized dithiothreitol
-
 r
1.17.4.4 2-methyl-3-phytyl-1,4-naphthoquinone + oxidized dithiothreitol + H2O
-
 Homo sapiens 2,3-epoxy-2,3-dihydro-2-methyl-3-phytyl-1,4-naphthoquinone + 1,4-dithiothreitol
-
 ?
1.17.4.4 2-methyl-3-phytyl-1,4-naphthoquinone + oxidized dithiothreitol + H2O
-
 Homo sapiens 2,3-epoxy-2,3-dihydro-2-methyl-3-phytyl-1,4-naphthoquinone + 1,4-dithiothreitol
-
 r

Synonyms

EC Number Synonyms Comment Organism
1.17.4.4 vitamin K 2,3-epoxide reductase complex subunit 1
-
 Homo sapiens
1.17.4.4 VKORC1
-
 Homo sapiens

pH Optimum

EC Number pH Optimum Minimum pH Optimum Maximum Comment Organism
1.17.4.4 7.4
-
 assay at Homo sapiens

IC50 Value

EC Number IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
1.17.4.4 additional information
-
 IC50 values for warfarin determined by different assay methods, overview Homo sapiens additional information
1.17.4.4 0.0000247
-
 pH and temperature not specified in the publication Homo sapiens warfarin
1.17.4.4 0.000136
-
 mutant V129L, pH and temperature not specified in the publication Homo sapiens warfarin
1.17.4.4 0.000152
-
 mutant V145A, pH and temperature not specified in the publication Homo sapiens warfarin
1.17.4.4 0.001226
-
 mutant L128R, pH and temperature not specified in the publication Homo sapiens warfarin

General Information

EC Number General Information Comment Organism
1.17.4.4 additional information 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 DTT-VKOR assay. However, VKORC1 variants with warfarin resistance-associated missense mutations often show low VKOR activities and warfarin sensitivity instead of resistance. Development and evaluation of a cell culture-based, indirect VKOR assay accurately reports warfarin sensitivity or resistance for wild-type and variant VKORC1 proteins Homo sapiens
1.17.4.4 additional information 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 DTT–VKOR assay. However, VKORC1 variants with warfarin resistance-associated missense mutations often show low VKOR activities and warfarin sensitivity instead of resistance. Development and evaluation of a cell culture-based, indirect VKOR assay accurately reports warfarin sensitivity or resistance for wild-type and variant VKORC1 proteins Homo sapiens