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Related Experiment Videos

Pregnane X receptor-mediated transcription.

Thomas K H Chang1, David J Waxman

  • 1Faculty of Pharmaceutical Sciences, The University of British Columbia, Vancouver, Canada.

Methods in Enzymology
|January 10, 2006
PubMed
Summary

The pregnane X receptor (PXR) is a key sensor for steroids and foreign chemicals, regulating metabolism and transport. A new assay helps identify PXR activators, aiding in predicting drug interactions and toxicity.

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Area of Science:

  • Biochemistry
  • Pharmacology
  • Toxicology

Background:

  • The pregnane X receptor (PXR) is a nuclear receptor superfamily member functioning as a crucial sensor for endogenous steroids and xenobiotics.
  • PXR is highly expressed in the liver and gastrointestinal tract, playing a vital role in regulating the metabolism and transport of various substances.

Purpose of the Study:

  • To summarize existing knowledge on PXR's biological functions.
  • To describe a novel cell culture-based luciferase reporter gene assay for assessing PXR transcriptional activity.

Main Methods:

  • Development and application of a luciferase reporter gene assay in cell culture.
  • Utilizing the assay to determine PXR transcriptional activity in response to various ligands.

Main Results:

  • The assay effectively measures PXR transcriptional activity.
  • The assay can identify novel drugs and environmental chemicals that act as PXR ligands.

Conclusions:

  • The developed assay is a valuable tool for identifying PXR ligands.
  • This assay can aid in predicting drug-drug interactions and xenobiotic-induced toxicities mediated by PXR activation.

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