Issue 2, 2022

A concise review on hPXR ligand-recognizing residues and structure-based strategies to alleviate hPXR transactivation risk

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.

Graphical abstract: A concise review on hPXR ligand-recognizing residues and structure-based strategies to alleviate hPXR transactivation risk

Article information

Article type
Review Article
Submitted
29 Oct 2021
Accepted
03 Jan 2022
First published
19 Jan 2022

RSC Med. Chem., 2022,13, 129-137

A concise review on hPXR ligand-recognizing residues and structure-based strategies to alleviate hPXR transactivation risk

T. Liu, J. P. Beck and J. Hao, RSC Med. Chem., 2022, 13, 129 DOI: 10.1039/D1MD00348H

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