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Updated: Aug 16, 2026

Reverse Yeast Two-hybrid System to Identify Mammalian Nuclear Receptor Residues that Interact with Ligands and/or Antagonists
10:51

Reverse Yeast Two-hybrid System to Identify Mammalian Nuclear Receptor Residues that Interact with Ligands and/or Antagonists

Published on: November 15, 2013

Animal models of xenobiotic receptors

Guoli Dai1, Yu-Jui Yvonne Wan

  • 1Department of Pharmacology, Toxicology and Therapeutics, University of Kansas Medical Center, 3901 Rainbow Blvd., Kansas City, KS 66160, USA.

Current Drug Metabolism
|August 17, 2005
PubMed

Insights

Animal models of Retinoid X receptors (RXRs), pregnane X receptor (PXR), and constitutive androstane receptor (CAR) have advanced understanding of xenobiotic and endobiotic metabolism. These models are crucial for drug screening and defining nuclear receptor pathways in health and disease.

Area of Science:

  • Biochemistry
  • Pharmacology
  • Molecular Biology

Background:

  • Retinoid X receptors (RXRs) heterodimerize with xenobiotic receptors pregnane X receptor (PXR) and constitutive androstane receptor (CAR).
  • These nuclear receptors mediate the metabolism of xenobiotics and endobiotics.
  • Understanding their function is vital for drug development and toxicology.

Purpose of the Study:

  • To review the progress in understanding nuclear receptor biology using animal models.
  • To highlight the utility of gene knockout and transgenic models for RXRs, PXR, and CAR.
  • To discuss the application of humanized and multiple gene knockout models.

Main Methods:

  • Utilizing gene knockout and transgenic mouse models for RXRs, PXR, and CAR.
  • Employing humanized mouse models to overcome species specificity.
  • Generating multiple gene knockout models to dissect pathway redundancy.

Main Results:

  • Significant research progress in elucidating molecular mechanisms of nuclear receptor-mediated metabolism.
  • Animal models facilitate screening of nuclear receptor ligands and identification of target genes.
  • Humanized models provide valuable insights into human xenobiotic responses.

Conclusions:

  • Animal models are indispensable tools for studying the physiological, pharmacological, and pathological roles of RXRs, PXR, and CAR.
  • These models have significantly advanced the field of nuclear receptor research.
  • Future research can leverage these models to further define complex metabolic pathways.

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