Rho激酶与疼痛及其抑制剂的临床应用  

Rho kinase and pain and clinical application of its inhibitors

作　　者：张雪琼[1] 张永鹤[1] 

机构地区：[1]北京大学医学部基础医学院药理学系,北京100191

出　　处：《中国药理学通报》2014年第4期448-451,共4页Chinese Pharmacological Bulletin

基　　金：国家自然科学基金面上项目(No 81173031;81202511)

摘　　要：小分子GTP结合蛋白Rho及其下游Rho激酶对细胞的收缩、迁移、增殖、黏附和凋亡等活动具有重要的调控作用。该文通过阐述Rho/Rho激酶信号通路在疼痛的产生和持续过程中的作用及其抑制剂在临床研究中的使用案例,探讨Rho/Rho激酶作为镇痛药物的作用靶点的可能性。大量的实验和临床研究表明,Rho/Rho激酶通过其介导的细胞信号传导系统参与神经性疼痛、炎症性疼痛、糖尿病性周围神经疼痛、脑血管痉挛、血管痉挛性心绞痛及骨癌痛等,因此,Rho/Rho激酶可作为防治疼痛的潜在药物作用靶点,为临床上预防和治疗疼痛提供新的思路和策略。Small GTP binding protein Rho and its downstream Rho-kinase pathway play an important role in the various cellular functions, including contraction, migration, proliferation, adhe-sion and apoptosis, etc. This article reviews the role of Rho/Rho-kinase pathway in the pain generation and development and clinical application of Rho/Rho-kinase inhibitors. It discusses the feasibility of Rho/Rho-kinase as a target for analgesics. Ac-cumulating experimental and clinical evidences indicate that＆amp;nbsp;Rho/Rho-kinase pathway is involved in the neuropathic pain, inflammatory pain, diabetic painful neuropathy, cerebral vaso-spasm, vasospastic angina and cancer pain, etc. Therefore, Rho/Rho-kinase is a potential drug target of the pain, and it provides new therapeutic treatments and strategies for pain in clinic.

关 键 词：RHO蛋白 RHO激酶 疼痛 抑制剂 药物靶点 镇痛 

分 类 号：R-05[医药卫生] R341.3