孕烷x受体的翻译后修饰及其功能调控作用研究进展 - 药学进展.pdf

PROGRESS IN PHARMACEUTICAL SCIENCES 2016,40 6 :453-459 ( ) 453 孕烷X受体的翻译后修饰及其功能调控作用研究进展 1 1 1* 2** 洛文靖 ，辛瑜 ，奚涛 ，熊晶 （1. 中国药科大学生命科学与技术学院，江苏 南京 210009；2. 南京医科大学基础医学院药理学系，江苏 南京 210029） [ 摘要 ] 孕烷 X 受体（PXR）是一类配体依赖性的核受体亚家族，可感受外源物质，被多种药物激活。PXR 可转录调控多种与药物代谢 相关的药物代谢酶和药物转运体的表达，参与药物代谢调控。PXR 转录活性的变化可改变药物在体内的代谢过程，继而诱发潜在药物不 良反应，与药物药代动力学研究和临床药物治疗密切相关，并有潜力成为防治药物介导的肝损伤和逆转化疗药物耐药的新型药物靶标。 综述了目前已发现的 PXR 翻译后修饰及其对 PXR 功能调控机制的研究进展。 [ 关键词 ] 孕烷 X 受体；翻译后修饰；药物代谢；药物研发 [ 中图分类号 ] R966 [ 文献标志码 ] A [ 文章编号 ] 1001-5094（2016）06-0453-07 Advances in Research on Post-translational Modifications of Pregnane X Receptor and Their Effects on Function Regulation 1 1 1 2 LUO Wenjing , XIN Yu , XI Tao , XIONG Jing (1. School of Life Science and Technology, China Pharmaceutical University, Nanjing 210009, China; 2. Department of Pharmacology, Nanjing Medical University, Nanjing 210029, China) [Abstract] Pregnane X receptor (PXR), a member of the nuclear receptor superfamily, is a ligand-dependent transcription factor. As a xenobiotic receptor, PXR is activated by a wide spectrum of structurally different substrates including clinical drugs, and subsequently regulates the expression of numerous drug metabolism enzymes and drug transporters at transcriptional level. PXR is closely related to pharmacokinetic study and clinical drug effect since changes in PXR transcriptional activity will result in altered in vivo drug metabolism and cause adverse drug reactions. PXR also has the potential to be developed into a novel drug target to prevent