Nuclear receptors and drug disposition gene regulation

J Pharm Sci. 2005 Jun;94(6):1169-86. doi: 10.1002/jps.20324.


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.

Publication types

  • Review

MeSH terms

  • Animals
  • DNA-Binding Proteins / physiology
  • Flavoproteins / physiology
  • Gene Expression Regulation*
  • Hepatocyte Nuclear Factor 4
  • Humans
  • NF-E2-Related Factor 2
  • Oxidoreductases / physiology
  • PPAR alpha / physiology
  • Pharmaceutical Preparations / metabolism*
  • Phosphoproteins / physiology
  • Receptors, Cytoplasmic and Nuclear / physiology*
  • Trans-Activators / physiology
  • Transcription Factors / physiology
  • Transcription, Genetic


  • DNA-Binding Proteins
  • Flavoproteins
  • HNF4A protein, human
  • Hepatocyte Nuclear Factor 4
  • NF-E2-Related Factor 2
  • NFE2L2 protein, human
  • PPAR alpha
  • Pharmaceutical Preparations
  • Phosphoproteins
  • Receptors, Cytoplasmic and Nuclear
  • Trans-Activators
  • Transcription Factors
  • farnesoid X-activated receptor
  • NDOR1 protein, human
  • Oxidoreductases