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Current Pharmacogenomics


ISSN (Print): 1570-1603
ISSN (Online): 1570-1603

Nuclear Receptors CAR and PXR in Metabolism and Elimination of Drugs

Author(s): P. Honkakoski

Volume 1, Issue 2, 2003

Page: [75 - 85] Pages: 11

DOI: 10.2174/1570160033476296

Price: $65


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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