The utility of stable cell lines to assess species differences in PXR transactivation.
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.
Sinz
Michael W
MW
Bristol-Myers Squibb Company, Wallingford, CT 06492, USA.
Pray
Devin
D
Raucy
Judy
J
D023401:Animal Use Alternatives / Q000379:methods; D000818:Animals; D002460:Cell Line; D051544:Cytochrome P-450 CYP3A / Q000187:drug effects* / Q000378:metabolism; D003907:Dexamethasone / Q000494:pharmacology; D004790:Enzyme Induction / Q000187:drug effects; D006801:Humans; D000077297:Pregnane X Receptor; D051381:Rats; D011987:Receptors, Steroid / Q000187:drug effects* / Q000378:metabolism; D012293:Rifampin / Q000494:pharmacology; D013045:Species Specificity; D015533:Transcriptional Activation / Q000187:drug effects*; D015262:Xenobiotics / Q000494:pharmacology*
D000077297:Pregnane X Receptor; D011987:Receptors, Steroid; D015262:Xenobiotics; D003907:Dexamethasone; D051544:Cytochrome P-450 CYP3A; D012293:Rifampin