Resveratrol as an inhibitor of pregnane X receptor (PXR): another lesson in PXR antagonism
Language English Country Japan Media print
Document type Journal Article, Research Support, Non-U.S. Gov't
PubMed
25341568
DOI
10.1254/jphs.14001lt
PII: DN/JST.JSTAGE/jphs/14001LT
Knihovny.cz E-resources
- MeSH
- Molecular Targeted Therapy MeSH
- Cytochrome P-450 CYP3A genetics metabolism MeSH
- Gene Expression drug effects MeSH
- Cytochrome P-450 CYP3A Inducers MeSH
- Humans MeSH
- Drug Discovery MeSH
- Pregnane X Receptor MeSH
- Antineoplastic Agents MeSH
- Resveratrol MeSH
- Rifampin antagonists & inhibitors MeSH
- Signal Transduction drug effects MeSH
- Receptors, Steroid antagonists & inhibitors physiology MeSH
- Stilbenes pharmacology MeSH
- Check Tag
- Humans MeSH
- Publication type
- Journal Article MeSH
- Research Support, Non-U.S. Gov't MeSH
- Names of Substances
- Cytochrome P-450 CYP3A MeSH
- Cytochrome P-450 CYP3A Inducers MeSH
- Pregnane X Receptor MeSH
- Antineoplastic Agents MeSH
- Resveratrol MeSH
- Rifampin MeSH
- Receptors, Steroid MeSH
- Stilbenes MeSH
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.
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