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Updated: May 13, 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

[Modulation of nuclear receptors on drug-metabolizing enzymes and transporters]

Zhi-Hao Liu1, Yan Li

  • 1Department of Drug Metabolism and Pharmacokinetics of Institute of Materia Medica, Chinese Academy of Medical Sciences & Peking Union Medical College, Beijing 100050, China.

Yao Xue Xue Bao = Acta Pharmaceutica Sinica
|March 6, 2013
PubMed

Insights

Nuclear receptors (NRs) like PXR, CAR, and PPAR regulate drug metabolism and transport. Targeting these NRs offers a new strategy to overcome multidrug resistance (MDR) in cancer therapy.

Area of Science:

  • Pharmacology
  • Molecular Biology
  • Biochemistry

Background:

  • Nuclear receptors (NRs) are crucial regulators of drug disposition.
  • Drug-metabolizing enzymes (DMEs) and transporters are key to drug metabolism and clearance.
  • Multidrug resistance (MDR) is a major challenge in cancer treatment.

Purpose of the Study:

  • To review the role of PXR, CAR, and PPAR in regulating DMEs and transporters.
  • To explore the potential of NRs as a therapeutic target to overcome MDR.
  • To provide insights into NR transcriptional activation mechanisms.

Main Methods:

  • Literature review of research on PXR, CAR, and PPAR.
  • Analysis of NR-mediated regulation of DMEs and transporters.
  • Examination of NR transcriptional activation pathways.

Main Results:

  • NRs, including PXR, CAR, and PPAR, significantly influence drug metabolism and transport.
  • These NRs regulate the expression of key DMEs and transporters.
  • Modulation of NRs presents a promising approach to combat MDR.

Conclusions:

  • NRs play a critical role in drug disposition and MDR.
  • Targeting NRs offers a novel strategy for overcoming therapeutic resistance.
  • Further research into NR mechanisms can inform clinical medication strategies.

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