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

Published on: November 15, 2013

Interplay of pregnane X receptor with other nuclear receptors on gene regulation

Yun-Ping Lim1, Jin-ding Huang

  • 1Department of Pharmacology, Medical College, National Cheng Kung University, Tainan, Taiwan.

Drug Metabolism and Pharmacokinetics
|February 29, 2008
PubMed

Insights

The pregnane X receptor (PXR) regulates drug metabolism and protects against harmful chemicals by controlling gene expression. This review explores PXR

Area of Science:

  • Pharmacology and Toxicology
  • Molecular Biology
  • Biochemistry

Background:

  • The human body encounters numerous harmful chemicals, necessitating protective mechanisms.
  • Chemicals influence drug metabolism, enzyme induction, and can lead to adverse drug-drug interactions.
  • Nuclear receptors (NRs) play crucial roles in cellular responses to xenobiotics.

Purpose of the Study:

  • To review the role of pregnane X receptor (PXR) in xenobiotic response.
  • To explore the crosstalk between PXR and other nuclear receptors.
  • To understand the involvement of coregulators in PXR-mediated gene expression.

Main Methods:

  • Literature review of studies on nuclear receptors and xenobiotic metabolism.
  • Analysis of PXR's function as a transcriptional regulator.
  • Examination of interactions between PXR and other nuclear receptors (FXR, SHP, HNF-4alpha, LXR, GR, CAR).

Main Results:

  • PXR is a key regulator of cytochrome P450 (CYP) and transporter expression.
  • PXR interacts with multiple nuclear receptors, forming a complex regulatory network.
  • Coregulators are essential for PXR's control over target gene expression.

Conclusions:

  • PXR is a central player in the body's defense against xenobiotics.
  • Understanding PXR's interactions with other nuclear receptors provides insights into drug metabolism and interactions.
  • The PXR network, involving coregulators, is critical for maintaining cellular homeostasis.

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