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Literature summary for 1.17.4.4 extracted from

  • Lasseur, R.; Grandemange, A.; Longin-Sauvageon, C.; Berny, P.; Benoit, E.
    Comparison of the inhibition effect of different anticoagulants on vitamin K epoxide reductase activity from warfarin-susceptible and resistant rat (2007), Pestic. Biochem. Physiol., 88, 203-208.
No PubMed abstract available

Protein Variants

Protein Variants Comment Organism
Y139F highly resistant to warfarin and increased resistance to further anticoagulants Rattus norvegicus

Inhibitors

Inhibitors Comment Organism Structure
brodifacoum
-
Rattus norvegicus
bromadiolone
-
Rattus norvegicus
chlorophacinone
-
Rattus norvegicus
coumachlor
-
Rattus norvegicus
coumatetralyl
-
Rattus norvegicus
Difenacoum
-
Rattus norvegicus
diphacinone
-
Rattus norvegicus
warfarin
-
Rattus norvegicus

Localization

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

Organism

Organism UniProt Comment Textmining
Rattus norvegicus
-
-
-

Source Tissue

Source Tissue Comment Organism Textmining
liver
-
Rattus norvegicus
-

Ki Value [mM]

Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
0.00004
-
brodifacoum wild-type, pH 7.4, 30°C Rattus norvegicus
0.00007
-
Difenacoum wild-type, pH 7.4, 30°C Rattus norvegicus
0.00007
-
diphacinone wild-type, pH 7.4, 30°C Rattus norvegicus
0.00008
-
chlorophacinone wild-type, pH 7.4, 30°C Rattus norvegicus
0.00009
-
brodifacoum mutant Y139F, pH 7.4, 30°C Rattus norvegicus
0.00012
-
coumachlor wild-type, pH 7.4, 30°C Rattus norvegicus
0.00013
-
bromadiolone wild-type, pH 7.4, 30°C Rattus norvegicus
0.00013
-
coumatetralyl wild-type, pH 7.4, 30°C Rattus norvegicus
0.00026
-
Difenacoum mutant Y139F, pH 7.4, 30°C Rattus norvegicus
0.00072
-
warfarin wild-type, pH 7.4, 30°C Rattus norvegicus
0.00091
-
bromadiolone mutant Y139F, pH 7.4, 30°C Rattus norvegicus
0.0016
-
chlorophacinone mutant Y139F, pH 7.4, 30°C Rattus norvegicus
0.0019
-
coumachlor mutant Y139F, pH 7.4, 30°C Rattus norvegicus
0.0031
-
coumatetralyl mutant Y139F, pH 7.4, 30°C Rattus norvegicus
0.005
-
diphacinone mutant Y139F, pH 7.4, 30°C Rattus norvegicus
0.029
-
warfarin mutant Y139F, pH 7.4, 30°C Rattus norvegicus