Drug Metabolism Letters

Zhiyang Zhao
Amgen
Cambridge, MA
USA

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The Utility of Stable Cell Lines to Assess Species Differences in PXR Transactivation

Author(s): Michael W. Sinz, Devin Pray, Judy Raucy.

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.

Keywords: Rat PXR, stable cells, CYP3A induction, toxicity, high volume screening

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Article Details

VOLUME: 1
ISSUE: 2
Year: 2007
Page: [147 - 152]
Pages: 6
DOI: 10.2174/187231207780363561
Price: $58