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Review ArticleMinireview

Pregnane X Receptor and Constitutive Androstane Receptor at the Crossroads of Drug Metabolism and Energy Metabolism

Jie Gao and Wen Xie
Drug Metabolism and Disposition December 2010, 38 (12) 2091-2095; DOI: https://doi.org/10.1124/dmd.110.035568
Jie Gao
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Wen Xie
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Abstract

The pregnane X receptor (PXR) and the constitutive androstane receptor (CAR) are two closely related and liver-enriched nuclear hormone receptors originally defined as xenobiotic receptors. PXR and CAR regulate the transcription of drug-metabolizing enzymes and transporters, which are essential in protecting our bodies from the accumulation of harmful chemicals. An increasing body of evidence suggests that PXR and CAR also have an endobiotic function that impacts energy homeostasis through the regulation of glucose and lipids metabolism. Of note and in contrast, disruptions of energy homeostasis, such as those observed in obesity and diabetes, also have a major impact on drug metabolism. This review will focus on recent progress in our understanding of the integral role of PXR and CAR in drug metabolism and energy homeostasis.

Footnotes

  • This work was supported in part by the National Institutes of Health National Institute of Environmental Health Sciences [Grant ES014626]; the National Institutes of Health National Institute of Diabetes and Digestive and Kidney Diseases [Grant DK076962]; and a Molecular Pharmacology Fellowship funded by the University of Pittsburgh Department of Pharmacology and Chemical Biology.

  • Article, publication date, and citation information can be found at http://dmd.aspetjournals.org.

    doi:10.1124/dmd.110.035568.

  • ABBREVIATIONS:

    P450
    cytochrome P450
    PXR
    pregnane X receptor
    SULTs
    sulfotransferases
    CAR
    constitutive androstane receptor
    PB
    phenobarbital
    TCPOBOP
    1,4-Bis[2-(3,5-dichloropyridyloxy)]benzene
    LXR
    liver X receptor
    NASH
    nonalcoholic steatohepatitis
    SREBP-1
    sterol regulatory element-binding protein 1
    AMPK
    AMP-activated protein kinase
    PAR bZip
    PAR-domain basic leucine zipper
    PGC-1α
    peroxisome-proliferator-activated-receptor-γ-coactivator-1α
    FOXO1
    Forkhead box O1 protein
    CPR
    cytochrome P450 reductase
    PPARγ2
    peroxisome proliferator-activated receptor γ2
    TH
    thyroid hormone
    PCN
    pregnenolone-16α-carbonitrile
    CPT1α
    carnitine palmitoyltransferase 1α
    HMGCS2
    3-hydroxy-3-methylglutarate-CoA synthase 2
    FoxA2
    Forkhead box A2
    CREB
    cAMP response element-binding protein
    PEPCK
    phosphoenolpyruvate carboxykinase
    AICAR
    5-amino-1-β-d-ribofuranosyl-1H-imidazole-4-carboxamide.

  • Received July 18, 2010.
  • Accepted August 23, 2010.
  • Copyright © 2010 by The American Society for Pharmacology and Experimental Therapeutics
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Drug Metabolism and Disposition: 38 (12)
Drug Metabolism and Disposition
Vol. 38, Issue 12
1 Dec 2010
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Review ArticleMinireview

Pregnane X Receptor and Constitutive Androstane Receptor at the Crossroads of Drug Metabolism and Energy Metabolism

Jie Gao and Wen Xie
Drug Metabolism and Disposition December 1, 2010, 38 (12) 2091-2095; DOI: https://doi.org/10.1124/dmd.110.035568

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Review ArticleMinireview

Pregnane X Receptor and Constitutive Androstane Receptor at the Crossroads of Drug Metabolism and Energy Metabolism

Jie Gao and Wen Xie
Drug Metabolism and Disposition December 1, 2010, 38 (12) 2091-2095; DOI: https://doi.org/10.1124/dmd.110.035568
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    • Abstract
    • Pregnane X Receptor and Constitutive Androstane Receptor As Master Regulators of Drug Metabolism and Drug Transporter
    • Drug Metabolism Can Be Affected by Energy Metabolism
    • Energy Metabolism Can Be Affected by Drug Metabolism and Xenobiotic Receptors PXR and CAR
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