Journal
RSC MEDICINAL CHEMISTRY
Volume 13, Issue 2, Pages 129-137Publisher
ROYAL SOC CHEMISTRY
DOI: 10.1039/d1md00348h
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This concise review identifies the structural features of the human pregnane X receptor (hPXR) that serve as hot spots for ligand binding. It also summarizes structure-based strategies to mitigate hPXR transactivation, providing valuable insights for medicinal chemists.
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.
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