title: Resveratrol as an inhibitor of pregnane X receptor (PXR): another lesson in PXR antagonism.
abstract: The pregnane X receptor (PXR) plays a central role in the regulation of metabolism. Only few PXR antagonists have been described and the mechanism of PXR inhibition is mostly hypothetical or believed to be allosteric. Resveratrol is now being discussed as a novel agent that is capable of attenuating the PXR-inducible expression of the CYP3A4 gene, although the mechanistic explanation has not been determined. We discuss herein the effect of resveratrol on PXR in the context of our data from a ligand binding assay and with respect to the effect of resveratrol on various cellular signaling pathways that are known to affect PXR.
authors.affiliation: Centre of Drug-Dietary Supplements Interactions and Nutrigenetics, Faculty of Pharmacy, Charles University in Prague, Czech Republic.
authors.forename: Tomas
authors.initials: T
authors.lastname: Smutny
authors.forename: Petr
authors.initials: P
authors.lastname: Pavek
mesh_terms: D000970:Antineoplastic Agents; D051544:Cytochrome P-450 CYP3A / Q000235:genetics / Q000378:metabolism; D065701:Cytochrome P-450 CYP3A Inducers; D055808:Drug Discovery; D015870:Gene Expression / Q000187:drug effects; D006801:Humans; D058990:Molecular Targeted Therapy; D000077297:Pregnane X Receptor; D011987:Receptors, Steroid / Q000037:antagonists & inhibitors* / Q000502:physiology; D000077185:Resveratrol; D012293:Rifampin / Q000037:antagonists & inhibitors; D015398:Signal Transduction / Q000187:drug effects; D013267:Stilbenes / Q000494:pharmacology*
chemical_list: D000970:Antineoplastic Agents; D065701:Cytochrome P-450 CYP3A Inducers; D000077297:Pregnane X Receptor; D011987:Receptors, Steroid; D013267:Stilbenes; D051544:Cytochrome P-450 CYP3A; D000077185:Resveratrol; D012293:Rifampin