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Stereoselective interactions of warfarin enantiomers with the pregnane X nuclear receptor in gene regulation of major drug-metabolizing cytochrome P450 enzymes

  1. 1.
    SYSNO ASEP0355208
    Document TypeJ - Journal Article
    R&D Document TypeJournal Article
    Subsidiary JČlánek ve WOS
    TitleStereoselective interactions of warfarin enantiomers with the pregnane X nuclear receptor in gene regulation of major drug-metabolizing cytochrome P450 enzymes
    Author(s) Rulcová, A. (CZ)
    Prokopová, I. (CZ)
    Krausová, L. (CZ)
    Bitman, M. (CZ)
    Vrzal, R. (CZ)
    Dvořák, Z. (CZ)
    Blahoš, Jaroslav (UMG-J) RID
    Pávek, P. (CZ)
    Source TitleJournal of Thrombosis and Haemostasis - ISSN 1538-7933
    Roč. 8, č. 12 (2010), s. 2708-2717
    Number of pages10 s.
    Languageeng - English
    CountryGB - United Kingdom
    KeywordsCYP3A4 ; gene regulation ; warfarin
    Subject RIVEB - Genetics ; Molecular Biology
    R&D ProjectsLC06063 GA MŠMT - Ministry of Education, Youth and Sports (MEYS)
    CEZAV0Z50520514 - UMG-J (2005-2011)
    UT WOS000285110700016
    DOI10.1111/j.1538-7836.2010.04036.x
    AnnotationBackground: Warfarin, an antagonist of vitamin K, is an oral coumarin anticoagulant widely used to control and prevent thromboembolic disorders. Warfarin is clinically available as a racemic mixture of R- and S-warfarin. The S-enantiomer has three to five times greater anticoagulation potency than its optical congener. Recently, vitamin K-2 function has been proposed via the pregnane X receptor (PXR) in osteocytes. PXR acts as a xenobiotic sensor that controls expression of many genes involved in drug/xenobiotic metabolic clearance. Objective: The aim was to examine whether enantiomers of warfarin stereoselectively interact with PXR to up-regulate main drug/ xenobiotic-metabolizing enzymes of the cytochrome P450 superfamily. Methods: Interactions of warfarin enantiomers with PXR were tested by gene reporter assays and time-resolved fluorescence resonance energy transfer technology (TR-FRET) ligand binding assay.
    WorkplaceInstitute of Molecular Genetics
    ContactNikol Škňouřilová, nikol.sknourilova@img.cas.cz, Tel.: 241 063 217
    Year of Publishing2011
Number of the records: 1  

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