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Literature summary for 1.17.4.5 extracted from

  • Hodroge, A.; Longin-Sauvageon, C.; Fourel, I.; Benoit, E.; Lattard, V.
    Biochemical characterization of spontaneous mutants of rat VKORC1 involved in the resistance to antivitamin K anticoagulants (2011), Arch. Biochem. Biophys., 515, 14-20.
    View publication on PubMed

Cloned(Commentary)

Cloned (Comment) Organism
expression of thec-myc-tagged enzyme mutant Y137F in Pichia pastoris membranes Rattus norvegicus

Inhibitors

Inhibitors Comment Organism Structure
brodifacoum
-
Rattus norvegicus
bromadiolone
-
Rattus norvegicus
chlorophacinone
-
Rattus norvegicus
Difenacoum
-
Rattus norvegicus
difethialone
-
Rattus norvegicus
additional information VKORC1 mutant Y137F is resistant against inhibition by warfarin, but not against inhibition by other antocoagulants, overview Rattus norvegicus

Localization

Localization Comment Organism GeneOntology No. Textmining
membrane
-
Rattus norvegicus 16020
-
microsome
-
Rattus norvegicus
-
-

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
2-methyl-3-phytyl-1,4-naphthoquinone + oxidized dithiothreitol + H2O Rattus norvegicus
-
2,3-epoxy-2,3-dihydro-2-methyl-3-phytyl-1,4-naphthoquinone + 1,4-dithiothreitol
-
?

Organism

Organism UniProt Comment Textmining
Rattus norvegicus
-
gene Vkorc1, VKORC1 mutant Y137F
-

Source Tissue

Source Tissue Comment Organism Textmining
liver
-
Rattus norvegicus
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
2-methyl-3-phytyl-1,4-naphthoquinone + oxidized dithiothreitol + H2O
-
Rattus norvegicus 2,3-epoxy-2,3-dihydro-2-methyl-3-phytyl-1,4-naphthoquinone + 1,4-dithiothreitol
-
?

Temperature Optimum [°C]

Temperature Optimum [°C] Temperature Optimum Maximum [°C] Comment Organism
37
-
assay at Rattus norvegicus

pH Optimum

pH Optimum Minimum pH Optimum Maximum Comment Organism
7.4
-
assay at Rattus norvegicus

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.00005
-
mutant Y137F, pH 7.4, 37°C Rattus norvegicus difethialone
0.00007
-
mutant Y137F, pH 7.4, 37°C Rattus norvegicus brodifacoum
0.0001
-
mutant Y137F, pH 7.4, 37°C Rattus norvegicus Difenacoum
0.00061
-
mutant Y137F, pH 7.4, 37°C Rattus norvegicus bromadiolone
0.0016
-
mutant Y137F, pH 7.4, 37°C Rattus norvegicus chlorophacinone