Small-molecule modulators of the constitutive androstane receptor

Abstract

Introduction: The constitutive androstane receptor (CAR) induces drug-metabolizing enzymes for xenobiotic metabolism.

Areas covered: This review covers recent advances in elucidating the biological functions of CAR and its modulation by a growing number of agonists and inhibitors.

Expert opinion: Extrapolation of animal CAR function to that of humans should be carefully scrutinized, particularly when rodents are used in evaluating the metabolic profile and carcinogenic properties of clinical drugs and environmental chemicals. Continuous efforts are needed to discover novel CAR inhibitors, with extensive understanding of their inhibitory mechanism, species selectivity, and discriminating power against other xenobiotic sensors.

Keywords:

• constitutive androstane receptor
• drug–drug interactions
• small-molecule
• xenobiotic metabolism

Acknowledgements

The authors thank Cherise Guess PhD, ELS, for editing the manuscript. MT Cherian and SC Chai contributed equally to this work.

Declaration of interest

This work was supported by the American Lebanese Syrian Associated Charities (ALSAC), St. Jude Children’s Research Hospital, National Institutes of Health National Institute of General Medical Sciences [GrantsRO1-GM086415&RO1-GM110034], and National Cancer Institute [Grant P30-CA21765]. The authors have no other relevant affiliations or financial involvement with any organization or entity with a financial interest in or financial conflict with the subject matter or materials discussed in the manuscript apart from those disclosed.

Notes

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