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Nuclear Receptors CAR and PXR in Metabolism and Elimination of Drugs

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The metabolism and elimination of drugs is mainly mediated by various cytochrome P450 (CYP) enzymes, conjugative enzymes, transporters, and efflux proteins. Members of these gene families are up-regulated at transcriptional level by drug exposure, thus leading to induction of drug metabolism and elimination. There is compelling evidence that this induction is controlled by two drug-activated nuclear receptors, constitutive androstane receptor (CAR), and pregnane X receptor (PXR). This mini-review summarizes the current knowledge of CAR and PXR, their DNA and ligand binding preferences, expression patterns and polymorphisms, mechanisms of activation, and target genes.

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Keywords: cytochrome p450; drugs elimination; efflux proteins; nuclear receptors car; pregnane; pxr; target genes

Document Type: Review Article

Publication date: June 1, 2003

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  • Current Pharmacogenomics provides comprehensive overviews of all current research on pharmacogenomics and pharmacogenetics. All areas of the field from pre-clinical to clinical research are covered, including related areas such as genomics, proteomics, target discovery, bioinformatics and novel diagnostics. This international journal is peer-reviewed and publishes both mini- and full review articles.

    The journal has become essential reading for all researchers and clinicians with interests in pharmacogenomics and pharmacogenetics.
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