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Pregnane X Receptor: Understanding Its Function and Activity at the Molecular Level

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Nuclear Receptors

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Abstract

The pregnane X receptor (PXR) is a ligand-activated nuclear receptor recognized as an important player in xenobiotic detoxification because it regulates the expression of drug-metabolizing enzymes and transporters. Because of its notorious role in drug metabolism and disposition, PXR’s activity may result in unintended drug-drug interactions, decreasing drug efficacy, inducing resistance, and causing toxicity. As such, PXR has become an attractive target for the development of PXR antagonists that can be used as co-drugs. However, PXR agonists have emerged as potential therapeutics against certain diseases, such as inflammatory bowel disease. This book chapter describes the molecular basis of PXR activity, correlating biochemical and structural elements to describe the promiscuous nature of PXR in recognizing a wide array of chemicals and the challenges in developing PXR modulators.

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Acknowledgment

The work reported in this publication was supported by the National Institute of General Medical Sciences of the National Institutes of Health under award number R35GM118041. The content is solely the responsibility of the authors and does not necessarily represent the official views of the National Institutes of Health. The authors thank ALSAC for their support, Cherise Guess, PhD, ELS, for editing the manuscript, and other members of the Chen research laboratory for valuable discussions of the paper.

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  1. Department of Chemical Biology and Therapeutics, St. Jude Children’s Research Hospital, Memphis, TN, USA

    Sergio C. Chai & Taosheng Chen

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  1. Sergio C. Chai
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Correspondence to Taosheng Chen .

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  1. School of Pharmacy, University of Missouri-Kansas City, Kansas City, MO, USA

    Mostafa Z. Badr

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Chai, S.C., Chen, T. (2021). Pregnane X Receptor: Understanding Its Function and Activity at the Molecular Level. In: Badr, M.Z. (eds) Nuclear Receptors. Springer, Cham. https://doi.org/10.1007/978-3-030-78315-0_7

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