Počet záznamů: 1

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

SYSNO ASEP	0355208
Druh ASEP	J - Článek v odborném periodiku
Zařazení RIV	J - Článek v odborném periodiku
Poddruh J	Článek ve WOS
Název	Stereoselective interactions of warfarin enantiomers with the pregnane X nuclear receptor in gene regulation of major drug-metabolizing cytochrome P450 enzymes
Tvůrce(i)	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)
Zdroj.dok.	Journal of Thrombosis and Haemostasis - ISSN 1538-7933 Roč. 8, č. 12 (2010), s. 2708-2717
Poč.str.	10 s.
Jazyk dok.	eng - angličtina
Země vyd.	GB - Velká Británie
Klíč. slova	CYP3A4 ; gene regulation ; warfarin
Vědní obor RIV	EB - Genetika a molekulární biologie
CEP	LC06063 GA MŠMT - Ministerstvo školství, mládeže a tělovýchovy
CEZ	AV0Z50520514 - UMG-J (2005-2011)
UT WOS	000285110700016
DOI	10.1111/j.1538-7836.2010.04036.x
Anotace	Background: 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.
Pracoviště	Ústav molekulární genetiky
Kontakt	Nikol Škňouřilová, nikol.sknourilova@img.cas.cz, Tel.: 241 063 217
Rok sběru	2011

Počet záznamů: 1