Nuclear receptors and drug disposition gene regulation

In this minireview, the role of various nuclear receptors and transcription factors in the expression of drug disposition genes is summarized. Specifically, the molecular aspects and functional impact of the aryl hydrocarbon receptor (AhR), nuclear factor-E2 p45-related factor 2 (N(r)f2), hepatocyte nuclear factor 1 alpha (HNF1 alpha), constitutive androstane receptor (LAR), pregnane X receptor (PXR), farnesoid X receptor (FXR), peroxisome proliferator-activated receptor alpha (PPAR alpha), hepatocyte nuclear factor 4 alpha (HNF4 alpha), vitamin D receptor (VDR), liver receptor homolog 1 (LRH1), liver X receptor (LXR alpha), small heterodimer partner-1 (SHP-1), and glucocorticoid. receptor (GR) on gene expression are detailed. Finally, we discuss some current topics and themes in nuclear receptor-mediated regulation of drug metabolizing enzymes and drug transporters. (C) 2005Wiley-Liss, Inc. and the American Pharmacists Association.