Nuclear Receptors CAR and PXR in Metabolism and Elimination of Drugs

Author(s): P. Honkakoski.

Journal Name: Current Pharmacogenomics
Continued as Current Pharmacogenomics and Personalized Medicine

Volume 1 , Issue 2 , 2003


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.

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

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Article Details

Year: 2003
Page: [75 - 85]
Pages: 11
DOI: 10.2174/1570160033476296
Price: $58

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