| 引用本文: | 葛乐乐,范辉,马珂.孕烷X受体(PXR)对药物代谢途径的调控[J].中国现代应用药学,2013,30(12):1357-1359. |
| GE Lele,FAN Hui,MA Ke.Role of Pregnane X Receptor(PXR) in Drug Metabolism Modulation[J].Chin J Mod Appl Pharm(中国现代应用药学),2013,30(12):1357-1359. |
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| 摘要: |
| 目的 从孕烷X受体(PXR)对药物代谢途径的调控入手，在代谢性药物相互作用、PXR在CYP3A4调控中的作用及其调控机制等方面作分析和阐述。方法 结合近年来国内外相关文献进行评述。结果 PXR是CYP3A4的主要转录调控因子，药物通过PXR介导的信号通路调节CYP3A4的表达是影响药物体内代谢变化的重要途径。结论 就临床药物而言，由PXR介导的CYP3A4酶蛋白表达的改变可造成合用药物药效的减弱甚至丧失，因此必须引起广大临床药师的足够重视。 |
| 关键词: 孕烷X受体 CYP3A4 药物代谢 |
| DOI： |
| 分类号:R284.1 |
| 基金项目: |
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| Role of Pregnane X Receptor(PXR) in Drug Metabolism Modulation |
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GE Lele, FAN Hui, MA Ke
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Department of Pharmacy, Sir Run Run Shaw Hospital, School of Medicine, Zhejiang University, Hangzhou 310016, China
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| Abstract: |
| OBJECTIVE To summarize and analyze the metabolic drug interaction, the role of pregnane X receptor(PXR) in CYP3A4 modulation and its molecule mechanism. METHODS Related literatures in recent years were reviewed. RESULTS PXR was a key transcription factor that regulate CYP3A4 expression. CYP3A4 transcription could be activated by compound via PXR-mediated signaling pathway therefore results in changes of co-administered drug metabolism. CONCLUSION For clinical drug, caution should be taken when PXR agonist is used in combination with prescribed drugs metabolized by CYP3A4. |
| Key words: pregnane X receptor CYP3A4 drug metabolism |
