中国药理学通报
中國藥理學通報
중국약이학통보
CHINESE PHARMACOLOGICAL BULLETIN
2014年
4期
448-451
,共4页
Rho蛋白%Rho激酶%疼痛%抑制剂%药物靶点%镇痛
Rho蛋白%Rho激酶%疼痛%抑製劑%藥物靶點%鎮痛
Rho단백%Rho격매%동통%억제제%약물파점%진통
Rho%Rho-kinase%pain%inhibitor%drug target%analgesia
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。
小分子GTP結閤蛋白Rho及其下遊Rho激酶對細胞的收縮、遷移、增殖、黏附和凋亡等活動具有重要的調控作用。該文通過闡述Rho/Rho激酶信號通路在疼痛的產生和持續過程中的作用及其抑製劑在臨床研究中的使用案例,探討Rho/Rho激酶作為鎮痛藥物的作用靶點的可能性。大量的實驗和臨床研究錶明,Rho/Rho激酶通過其介導的細胞信號傳導繫統參與神經性疼痛、炎癥性疼痛、糖尿病性週圍神經疼痛、腦血管痙攣、血管痙攣性心絞痛及骨癌痛等,因此, Rho/Rho激酶可作為防治疼痛的潛在藥物作用靶點,為臨床上預防和治療疼痛提供新的思路和策略。
소분자GTP결합단백Rho급기하유Rho격매대세포적수축、천이、증식、점부화조망등활동구유중요적조공작용。해문통과천술Rho/Rho격매신호통로재동통적산생화지속과정중적작용급기억제제재림상연구중적사용안례,탐토Rho/Rho격매작위진통약물적작용파점적가능성。대량적실험화림상연구표명,Rho/Rho격매통과기개도적세포신호전도계통삼여신경성동통、염증성동통、당뇨병성주위신경동통、뇌혈관경련、혈관경련성심교통급골암통등,인차, Rho/Rho격매가작위방치동통적잠재약물작용파점,위림상상예방화치료동통제공신적사로화책략。
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 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.
