Novel antagonists reveal the mechanism of PXR inhibition
Language English Country England, Great Britain Media print-electronic
Document type Journal Article
PubMed
39419741
DOI
10.1016/j.tips.2024.10.002
PII: S0165-6147(24)00212-8
Knihovny.cz E-resources
- Keywords
- PXR, antagonist, crystal structures, drug discovery,
- MeSH
- Humans MeSH
- Pregnane X Receptor * antagonists & inhibitors metabolism MeSH
- Animals MeSH
- Check Tag
- Humans MeSH
- Animals MeSH
- Publication type
- Journal Article MeSH
- Names of Substances
- Pregnane X Receptor * MeSH
The pregnane X receptor (PXR) is a key regulator of metabolism, but the mechanisms underlying its antagonism remain unclear. Garcia-Maldonado et al. reported potent new antagonists and their co-crystal structures, revealing molecular determinants of PXR antagonism and paving the way for developing antagonists as therapeutics and preventing undesirable PXR activation.
References provided by Crossref.org
Discovery of PXR Antagonist MI891 and PXR Degrader MI1013 and Their Roles in Hepatic Gene Regulation
