The utility of stable cell lines to assess species differences in PXR transactivation

Drug Metab Lett. 2007 Apr;1(2):147-52. doi: 10.2174/187231207780363561.

Abstract

A stable cell line was developed to assess activation of rat pregnane X receptor (rPXR) by xenobiotics. Characterization revealed that the greatest response occurred with dexamethasone (6-10 fold increase) while rifampicin failed to transactivate rPXR. Rodent PXR transactivation assays can be used to understand species differences in enzyme induction.

MeSH terms

  • Animal Use Alternatives / methods
  • Animals
  • Cell Line
  • Cytochrome P-450 CYP3A / drug effects*
  • Cytochrome P-450 CYP3A / metabolism
  • Dexamethasone / pharmacology
  • Enzyme Induction / drug effects
  • Humans
  • Pregnane X Receptor
  • Rats
  • Receptors, Steroid / drug effects*
  • Receptors, Steroid / metabolism
  • Rifampin / pharmacology
  • Species Specificity
  • Transcriptional Activation / drug effects*
  • Xenobiotics / pharmacology*

Substances

  • Pregnane X Receptor
  • Receptors, Steroid
  • Xenobiotics
  • Dexamethasone
  • Cytochrome P-450 CYP3A
  • Rifampin