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J Pharm Sci. 2005 Jun;94(6):1169-86.

Nuclear receptors and drug disposition gene regulation.

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  • 1Department of Medicine and Pharmacology, Division of Clinical Pharmacology, Vanderbilt University School of Medicine, Nashville, TN, USA.


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 1alpha (HNF1alpha), constitutive androstane receptor (LAR), pregnane X receptor (PXR), farnesoid X receptor (FXR), peroxisome proliferator-activated receptor alpha (PPAR(alpha)), hepatocyte nuclear factor 4alpha (HNF4alpha), 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) 2005 Wiley-Liss, Inc.

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