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Pregnane X receptor in the regulation mechanism to cytochrome P450 3A:research progress

Yan Li

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Abstract

Cytochrome P450 3A(CYP3A) is one of the key isoenzymes involved in the metabolism of clinical drugs. Pregnane X receptor ( PXR) belongs to NR1 Ⅰ subfamily of the nuclear receptor superfamily(NR). As a transcriptive regulatory factor of drug metabolism,PXR plays an important role in the induction of cyp3a gene expression. The expression of CYP3A can be regulated by certain drugs through activating PXR receptor by several pathways,including the interactions between PXR and other nuclear receptors,transcription factors or cellular signal transduction etc. The screening methods based on PXR have been widely applied to the early-term new drug discovery.

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What this paper is about

Cytochrome P450 3A(CYP3A) is one of the key isoenzymes involved in the metabolism of clinical drugs. Pregnane X receptor ( PXR) belongs to NR1 Ⅰ subfamily of the nuclear receptor superfamily(NR). As a transcriptive regulatory factor of drug metabolism,PXR plays an important role in the induction of cyp3a gene expression. The expression of CYP3A can be regulated by certain drugs through activating PXR receptor by several pathways,including the interactions between PXR and other nuclear receptors,transcription factors or cellular signal transduction etc. The screening methods based on PXR have been widely applied to the early-term new drug discovery.

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Available abstract

Cytochrome P450 3A(CYP3A) is one of the key isoenzymes involved in the metabolism of clinical drugs. Pregnane X receptor ( PXR) belongs to NR1 Ⅰ subfamily of the nuclear receptor superfamily(NR). As a transcriptive regulatory factor of drug metabolism,PXR plays an important role in the induction of cyp3a gene expression. The expression of CYP3A can be regulated by certain drugs through activating PXR receptor by several pathways,including the interactions between PXR and other nuclear receptors,transcription factors or cellular signal transduction etc. The screening methods based on PXR have been widely applied to the early-term new drug discovery.

Key concepts: Pregnane X receptor, Nuclear receptor, CYP3A, Cytochrome P450, Constitutive androstane receptor, Biology, CYP3A4, Signal transduction

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