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Updated: Jul 15, 2026
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
Medications That Regulate Pregnane X Receptor: A Systematic Review of Current Evidence
Petra Czarniak1, Rachael Moorin2, Jeff Hughes1
1Curtin Medical School, Faculty of Health Sciences, Curtin University, Bentley, Western Australia, Australia.
Pharmacology Research & Perspectives
|July 14, 2026
Summary
The pregnane X receptor (PXR) is regulated by many drugs, impacting disease and drug efficacy. Understanding PXR drug interactions is key for improving patient health outcomes.
Area of Science:
- Pharmacology
- Molecular Biology
- Biochemistry
Background:
- The pregnane X receptor (PXR) is a nuclear receptor that regulates the metabolism of xenobiotics, including drugs and toxins.
- PXR is activated by a wide range of ligands, acting as either an agonist or antagonist.
- PXR activation influences drug metabolism, lipid and glucose homeostasis, and disease pathophysiology.
Purpose of the Study:
- To review the literature on drugs that regulate PXR.
- To discuss the potential clinical implications of PXR regulation by drugs.
- To identify knowledge gaps regarding PXR regulators.
Main Methods:
- A systematic literature search was conducted using CINAHL, Embase, Medline, Scopus, and Web of Science.
- PRISMA guidelines were followed for study selection.
- 12,236 studies were screened, with 101 meeting inclusion criteria, supplemented by 46 additional articles.
Main Results:
- 42 studies reported prescription drugs and 40 reported non-prescription drugs that regulate PXR.
- 47 studies detailed beneficial and detrimental PXR-mediated drug effects in various diseases, including cancer, metabolic, and inflammatory conditions.
- A broad spectrum of drugs were identified as PXR agonists or antagonists.
Conclusions:
- PXR is a significant target for drug regulation with wide-ranging clinical implications.
- PXR modulation by drugs can alter drug efficacy and disease progression.
- Further research is needed to fully understand the potency and clinical impact of known PXR regulators.
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