Abstract
The xenobiotic nuclear receptors pregnane X receptor (PXR) and constitutive androstane receptor (CAR) were discovered or characterized in 1998. PXR and CAR have since been defined as master regulators of xenobiotic responses through their transcriptional regulation of drug-metabolizing enzymes and transporters. This article aims to provide an overview on the discovery of PXR and CAR as xenobiotic receptors.
SIGNIFICANCE STATEMENT
The xenobiotic receptors PXR and CAR play a key role in drug metabolism and disposition through their regulation of drug-metabolizing enzymes and transporters.
Footnotes
- Received January 30, 2022.
- Accepted October 20, 2022.
My independent research at the University of Pittsburgh was supported in part by National Institutes of Health National Institute of Environmental Health Sciences [Grant ES012479], [Grant ES014626], [Grant ES019629], [Grant ES023438], and [Grant ES030429]; National Cancer Institute [Grant CA107011]; National Institute of Diabetes and Digestive and Kidney Diseases [Grant DK076962], [Grant DK099232], [Grant DK083952], and [Grant DK117370]; and Eunice Kennedy Shriver National Institute of Child Health and Human Development [Grant HD073070]. I am also grateful to be supported by the Joseph Koslow Endowed Professorship provided by the University of Pittsburgh School of Pharmacy.
The author does not have an actual or perceived conflict of interest with the contents of this article.
- Copyright © 2023 by The American Society for Pharmacology and Experimental Therapeutics
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