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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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Orphan nuclear receptors, PXR and LXR: new ligands and therapeutic potential

Haibiao Gong1, Wen Xie

  • 1University of Pittsburgh, Center for Pharmacogenetics, PA 15261, USA. wex6@pitt.edu

Expert Opinion on Therapeutic Targets
|March 5, 2004
PubMed

Insights

Orphan nuclear receptors (NRs) are crucial for understanding health and disease. This review focuses on pregnane X receptor (PXR) and liver X receptor (LXR), exploring their therapeutic potential and challenges.

Area of Science:

  • Biochemistry
  • Molecular Biology
  • Pharmacology

Background:

  • Orphan nuclear receptors (NRs) are vital regulators in animal species, influencing health and disease.
  • Marketed drugs targeting NRs include bexarotene (anticancer, targeting retinoic X receptor) and thiazolidinediones (antidiabetic, targeting peroxisome proliferator-activated receptor-gamma).

Framework:

  • Recent conference insights highlighted several orphan NRs: pregnane X receptor (PXR), liver X receptor (LXR), constitutive androstane receptor (CAR), peroxisome proliferator-activated receptor (PPAR), and retinoic X receptor (RXR).
  • This paper specifically examines PXR and LXR.

Implementation:

  • Focus on PXR and LXR includes analysis of their target genes.
  • Recent ligand identification for PXR and LXR has been performed.

Implications:

  • The therapeutic targeting of PXR and LXR presents both significant promise and practical concerns.
  • Further research is needed to determine the clinical viability of PXR and LXR as drug targets.

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