Title : The nuclear receptors constitutive androstane receptor and pregnane X receptor cross-talk with hepatic nuclear factor 4alpha to synergistically activate the human CYP2C9 promoter.

Pub. Date : 2005 Sep

PMID : 15919766






2 Functional Relationships(s)
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1 Recent studies in our laboratory have shown that the nuclear receptor pregnane X receptor (PXR) is important in the transcriptional activation of the CYP2C9 promoter by drugs such as rifampicin and that the essential element is a constitutive androstane receptor (CAR)/PXR site -1839 bp upstream of the translation start site. Rifampin cytochrome P450 family 2 subfamily C member 9 Homo sapiens
2 Mutation of the two HNF4alpha binding sites differentially prevented up-regulation of CYP2C9 promoter by both CAR as well as HNF4alpha, synergy between the two receptors, and essentially abolished induction by rifampicin in HepG2 cells transfected with PXR. Rifampin cytochrome P450 family 2 subfamily C member 9 Homo sapiens