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A concise review on hPXR ligand-recognizing residues and structure-based strategies to alleviate hPXR transactivation risk.
- Source :
-
RSC medicinal chemistry [RSC Med Chem] 2022 Jan 19; Vol. 13 (2), pp. 129-137. Date of Electronic Publication: 2022 Jan 19 (Print Publication: 2022). - Publication Year :
- 2022
-
Abstract
- The human pregnane X receptor (hPXR) regulates the expression of major drug metabolizing enzymes. A wide range of drug candidates bind and activate hPXR, and hence are at risk of increasing drug-drug interactions and reducing clinical efficacy. hPXR structural features that function as hot spots for ligand binding are identified and highlighted in this concise review. Based on literature structure-activity relationship data as case studies, structure-based strategies to mitigate hPXR transactivation are summarized for medicinal chemists.<br />Competing Interests: All the authors are employees of Eli Lilly and Company.<br /> (This journal is © The Royal Society of Chemistry.)
Details
- Language :
- English
- ISSN :
- 2632-8682
- Volume :
- 13
- Issue :
- 2
- Database :
- MEDLINE
- Journal :
- RSC medicinal chemistry
- Publication Type :
- Academic Journal
- Accession number :
- 35308029
- Full Text :
- https://doi.org/10.1039/d1md00348h