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2003•Zhongguo yaolixue yu dulixue zazhiRequires access

Progresses of researches on the correlation between pregnane X receptor and CYP3A

Sun Jian

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Abstract

Cytochrome P450 monooxygenase 3A(CYP3A) is one of the key enzymes for the metabolism of endogenous steroids and foreign chemicals in liver. Pregnane X receptor(PXR) is a critical regulator of CYP3A gene expression and activation of PXR is predictive of CYP3A induction. Sequence differences in the ligand binding domain of PXR serve as the molecular basis for the species difference in CYP3A induction. Studies on the correlation between CYP3A and PXR would have practical applications especially in the direction of clinical drug usage.

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What this paper is about

Cytochrome P450 monooxygenase 3A(CYP3A) is one of the key enzymes for the metabolism of endogenous steroids and foreign chemicals in liver. Pregnane X receptor(PXR) is a critical regulator of CYP3A gene expression and activation of PXR is predictive of CYP3A induction. Sequence differences in the ligand binding domain of PXR serve as the molecular basis for the species difference in CYP3A induction. Studies on the correlation between CYP3A and PXR would have practical applications especially in the direction of clinical drug usage.

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Available abstract

Cytochrome P450 monooxygenase 3A(CYP3A) is one of the key enzymes for the metabolism of endogenous steroids and foreign chemicals in liver. Pregnane X receptor(PXR) is a critical regulator of CYP3A gene expression and activation of PXR is predictive of CYP3A induction. Sequence differences in the ligand binding domain of PXR serve as the molecular basis for the species difference in CYP3A induction. Studies on the correlation between CYP3A and PXR would have practical applications especially in the direction of clinical drug usage.

Key concepts: Pregnane X receptor, CYP3A, Cytochrome P450, Pregnane, Constitutive androstane receptor, Regulator, Drug metabolism, Monooxygenase

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