孕烷X受体对细胞色素P450 3A调控机制的研究进展

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

细胞色素P450 3A(CYP3A)是参与临床药物代谢的主要CYP同工酶之一。孕烷X受体(PXR)属于核受体超家族(NR)的NR1Ⅰ亚家族。该受体作为药物代谢的关键转录调控因子,参与CYP3A的诱导表达。药物可通过多种途径激活PXR受体调控cyp3a基因的表达,其中包括PXR与其他核受体、转录因子及细胞信号转导通路间的相互作用等多种途径。目前,基于PXR的筛选方法已广泛应用于早期新药研发。

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 super-family（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.