Novel antagonists reveal the mechanism of PXR inhibition
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.
Authors
- Rajamanikkam Kamaraj (ORCID: https://orcid.org/0000-0001-7115-0178)
- Petr Pávek (ORCID: https://orcid.org/0000-0001-8769-4196)
Institutions
- Charles University (CZ)
- University Hospital Hradec Králové (CZ)
- University of Hradec Králové (CZ)
Publication Details
- Journal
- Trends in Pharmacological Sciences
- Published
- 2024-10-16
- DOI
- https://doi.org/10.1016/j.tips.2024.10.002
- Citations
- 5
- Primary Topic
- Retinoids in leukemia and cellular processes
- Type
- article
- Field-Weighted Citation Impact
- 1.17