Nuclear Receptors CAR and PXR in Metabolism and Elimination of Drugs

Title: Nuclear Receptors CAR and PXR in Metabolism and Elimination of Drugs

Volume: 1 Issue: 2

Author(s): P. Honkakoski

Affiliation:

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

Abstract: 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.

Cite this article as:

Honkakoski P., Nuclear Receptors CAR and PXR in Metabolism and Elimination of Drugs, Current Pharmacogenomics 2003; 1 (2) . https://dx.doi.org/10.2174/1570160033476296