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Literature summary for 1.17.4.4 extracted from

  • Lasseur, R.; Longin-Sauvageon, C.; Videmann, B.; Billeret, M.; Berny, P.; Benoit, E.
    Warfarin resistance in a french strain of rats (2005), J. Biochem. Mol. Toxicol., 19, 379-385.
    View publication on PubMed

Cloned(Commentary)

Cloned (Comment) Organism
gene VKORC1 Y139F, DNA and amino acid sequence determination, genotyping, semiquantitative expression analysis Rattus norvegicus
gene VKORC1, DNA and amino acid sequence determination, genotyping, semiquantitative expression analysis Rattus norvegicus

Protein Variants

Protein Variants Comment Organism
Y139F the natural occuring mutation confers resistance to enzyme inhibitor warfarin, the mutant rats do not show vitamin K deficiency Rattus norvegicus

Inhibitors

Inhibitors Comment Organism Structure
warfarin the mutant Y139F strain is resistant to warfarin; wild-type rats Rattus norvegicus

KM Value [mM]

KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
additional information
-
additional information kinetics Rattus norvegicus
0.0195
-
2,3-epoxy-2,3-dihydro-2-methyl-3-phytyl-1,4-naphthoquinone pH 7.4, 25°C Rattus norvegicus
0.0577
-
2,3-epoxy-2,3-dihydro-2-methyl-3-phytyl-1,4-naphthoquinone pH 7.4, 25°C Rattus norvegicus

Localization

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

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
2,3-epoxy-2,3-dihydro-2-methyl-3-phytyl-1,4-naphthoquinone + 1,4-dithiothreitol Rattus norvegicus i.e. vitamin K 2,3-epoxide 2-hydroxy-2-methyl-3-phytyl-2,3-dihydronaphthoquinone + oxidized dithiothreitol i.e. vitamin K ?

Organism

Organism UniProt Comment Textmining
Rattus norvegicus
-
gene VKORC1, mutant Y139F
-
Rattus norvegicus Q6TEK4 warfarin-susceptible rats; gene VKORC1
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
2,3-epoxy-2,3-dihydro-2-methyl-3-phytyl-1,4-naphthoquinone + 1,4-dithiothreitol i.e. vitamin K 2,3-epoxide Rattus norvegicus 2-hydroxy-2-methyl-3-phytyl-2,3-dihydronaphthoquinone + oxidized dithiothreitol i.e. vitamin K ?

Synonyms

Synonyms Comment Organism
VKOR
-
Rattus norvegicus
VKORC1
-
Rattus norvegicus

Temperature Optimum [°C]

Temperature Optimum [°C] Temperature Optimum Maximum [°C] Comment Organism
25
-
assay at Rattus norvegicus

pH Optimum

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

Ki Value [mM]

Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
additional information
-
additional information inhibition kinetics Rattus norvegicus
0.00072
-
warfarin pH 7.4, 25°C Rattus norvegicus
0.029
-
warfarin pH 7.4, 25°C Rattus norvegicus