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.
