Title : Effect of the adrenal 11-beta-hydroxylase inhibitor metyrapone on human hepatic cytochrome P-450 expression: induction of cytochrome P-450 3A4.

Pub. Date : 2000 Jan

PMID : 10611146






6 Functional Relationships(s)
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1 Effect of the adrenal 11-beta-hydroxylase inhibitor metyrapone on human hepatic cytochrome P-450 expression: induction of cytochrome P-450 3A4. Metyrapone cytochrome P450 family 3 subfamily A member 4 Homo sapiens
2 Addition of metyrapone to human hepatocyte cultures resulted in the induction of CYP3A4 expression. Metyrapone cytochrome P450 family 3 subfamily A member 4 Homo sapiens
3 The pregnane X receptor (PXR), which has recently been shown to mediate the transcriptional induction of CYP3A4 expression in response to rifampicin, was activated by metyrapone in CV-1 cells transiently cotransfected with an expression vector encoding the human PXR and a reporter construct containing the everted repeat sequence that confers CYP3A4 induction responsiveness to inducers within its promoter. Metyrapone cytochrome P450 family 3 subfamily A member 4 Homo sapiens
4 The pregnane X receptor (PXR), which has recently been shown to mediate the transcriptional induction of CYP3A4 expression in response to rifampicin, was activated by metyrapone in CV-1 cells transiently cotransfected with an expression vector encoding the human PXR and a reporter construct containing the everted repeat sequence that confers CYP3A4 induction responsiveness to inducers within its promoter. Metyrapone cytochrome P450 family 3 subfamily A member 4 Homo sapiens
5 Metyrapone activated the human PXR at concentrations that also resulted in the induction of CYP3A4 in human cultured hepatocytes. Metyrapone cytochrome P450 family 3 subfamily A member 4 Homo sapiens
6 Metyrapone treatment is therefore unlikely to result in the induction of CYP1A1 but may induce the expression of CYP3A4 in humans. Metyrapone cytochrome P450 family 3 subfamily A member 4 Homo sapiens