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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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Regulation of transporters by nuclear hormone receptors: implications during inflammation

Shirley Teng1, Micheline Piquette-Miller

  • 1Leslie Dan Faculty of Pharmacy, University of Toronto, Toronto, Ontario, M5S 3M2, Canada.

Molecular Pharmaceutics
|December 13, 2007
PubMed

Insights

Nuclear receptors regulate membrane transporters, impacting drug absorption and elimination. Understanding this regulation is key to predicting drug responses during inflammation and developing new therapies.

Area of Science:

  • Pharmacology
  • Molecular Biology
  • Drug Metabolism

Background:

  • Membrane transporters are crucial for drug disposition, influencing efficacy and toxicity.
  • Altered transporter expression during inflammation causes variable drug responses.
  • Nuclear hormone receptors are key regulators of transporter genes.

Purpose of the Study:

  • To review the role of nuclear receptors in regulating membrane transporters during inflammation.
  • To explore how this knowledge can predict drug disposition variations and inform therapeutic development.

Main Methods:

  • Literature review of nuclear receptor and transporter interactions.
  • Analysis of transporter gene expression changes during inflammatory conditions.
  • Discussion of xenobiotic-activated nuclear receptors (e.g., PXR, CAR, FXR).

Main Results:

  • Nuclear receptors (PXR, CAR, FXR) modulate the expression of key transporters (e.g., P-gp, MRP2, BCRP, OATP2).
  • These transporters exhibit altered expression patterns during inflammatory responses.
  • Nuclear receptors are implicated as mediators of transporter regulation in inflammation.

Conclusions:

  • Nuclear receptors play a significant role in transporter regulation during inflammation.
  • Understanding these mechanisms aids in predicting interindividual drug response variations and drug interactions.
  • This knowledge can guide the development of therapeutics for transporter-related diseases.

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