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 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.
Tirona
Rommel G
RG
Department of Medicine and Pharmacology, Division of Clinical Pharmacology, Vanderbilt University School of Medicine, Nashville, TN, USA.
Kim
Richard B
RB
D000818:Animals; D004268:DNA-Binding Proteins / Q000502:physiology; D005420:Flavoproteins / Q000502:physiology; D005786:Gene Expression Regulation; D051557:Hepatocyte Nuclear Factor 4; D006801:Humans; D051267:NF-E2-Related Factor 2; D010088:Oxidoreductases / Q000502:physiology; D047493:PPAR alpha / Q000502:physiology; D004364:Pharmaceutical Preparations / Q000378:metabolism*; D010750:Phosphoproteins / Q000502:physiology; D018160:Receptors, Cytoplasmic and Nuclear / Q000502:physiology*; D015534:Trans-Activators / Q000502:physiology; D014157:Transcription Factors / Q000502:physiology; D014158:Transcription, Genetic; D000099150:Receptor, Farnesoid X-Activated
D004268:DNA-Binding Proteins; D005420:Flavoproteins; D051557:Hepatocyte Nuclear Factor 4; D051267:NF-E2-Related Factor 2; D010088:Oxidoreductases; D047493:PPAR alpha; D004364:Pharmaceutical Preparations; D010750:Phosphoproteins; D018160:Receptors, Cytoplasmic and Nuclear; D015534:Trans-Activators; D014157:Transcription Factors; D000099150:Receptor, Farnesoid X-Activated; C496592:HNF4A protein, human; C495635:NFE2L2 protein, human; C478386:NDOR1 protein, human