TRPV1:一种同时参与慢性痛外周敏化和疼痛中枢调制的重要分子

发布时间：2018-06-28 22:42

本文选题：疼痛 + TRPV　；参考：《生理学报》2017年05期

【摘要】：慢性痛是困扰临床的一大顽疾,关于慢性痛机制的研究和新型镇痛药物的研发具有重要意义。十多年来,本研究组围绕慢性痛外周敏化形成的关键分子——瞬时受体电位香草酸亚型1(transient receptor potential vanilloid type 1,TRPV1),对其敏化和膜定位机制进行了系列研究,揭示了蛋白激酶PKD1(protein kinase D1)、Cdk5(cyclin-dependent kinase 5)和LIMK(LIM-motif containing kinase)在炎症诱发热痛敏中的作用及其对TRPV1的功能调控,并据此开发出了一系列具有镇痛作用的Tat穿膜肽。本综述还围绕研究组近期工作所揭示的参与痛感觉和痛情绪相互作用的关键脑区——前额叶皮质的前边缘皮质亚区,对TRPV1在其中的可能作用进行了探讨。此外本综述也对研究组在改进TRPV1靶向药物,提高其镇痛疗效,降低副作用方面的工作进行了简要总结和回顾。
[Abstract]:Chronic pain is an intractable disease that puzzles the clinic. It is of great significance to study the mechanism of chronic pain and the development of new analgesic drugs. For more than a decade, our team has carried out a series of studies on the mechanism of sensitization and membrane localization of vanillic acid subtype 1 (transient receptor potential vanilloid type 1 / TRPV1, a key molecule formed by peripheral sensitization of chronic pain. It was revealed that protein kinase PKD1 (protein kinase D1) CDK5 (cyclin-dependent kinase 5) and LIMK (LIM-motif containing kinase) play an important role in inflammation induced thermosensitivity and its function on TRPV1. A series of tat transmembrane peptides with analgesic effect were developed. This review also discusses the possible role of TRPV1 in the prefrontal cortex, a key brain region involved in the interaction of pain sensation and pain emotion revealed by the recent work of the study group. In addition, the work of the study group in improving TRPV1 targeted drugs, improving its analgesic efficacy and reducing side effects were also reviewed.
【作者单位】：北京大学医学部基础医学院神经科学研究所神经生物学系教育部和卫生与计划生育委员会神经科学重点实验室;北京大学麦戈文脑科学研究所;
【基金】：supported by grants from the National Natural Science Foundation of China(No. 3153002, 30925015, 30830044, 31771295, and 31371143) the National Basic Research Development Program of China (No. 2014CB542204)
【分类号】：R402

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