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Rho相关蛋白激酶(ROCK)抑制剂的研发进展。

Advances in the development of Rho-associated protein kinase (ROCK) inhibitors.

作者信息

Pan Peichen, Shen Mingyun, Yu Huidong, Li Youyong, Li Dan, Hou Tingjun

机构信息

Institute of Functional Nano & Soft Materials (FUNSOM) and Jiangsu Key Laboratory for Carbon-Based Functional Materials & Devices, Soochow University, Suzhou, Jiangsu 215123, China.

出版信息

Drug Discov Today. 2013 Dec;18(23-24):1323-33. doi: 10.1016/j.drudis.2013.09.010. Epub 2013 Sep 25.

Abstract

Rho-associated protein kinases (ROCK1 and ROCK2) belong to the AGC family of serine-threonine kinases, and regulate a wide range of fundamental cell functions. Inhibition of ROCK has been proven to be of potential therapeutic benefit for a variety of diseases. In this review, the structures and therapeutic importance of ROCK are discussed briefly. Then, the recent status of the development of ROCK inhibitors is also summarized. Our review offers a foundation outline from which strategies to design new leads against ROCK can be developed.

摘要

Rho相关蛋白激酶(ROCK1和ROCK2)属于丝氨酸 - 苏氨酸激酶的AGC家族,可调节多种基本细胞功能。已证明抑制ROCK对多种疾病具有潜在的治疗益处。在本综述中,将简要讨论ROCK的结构和治疗重要性。然后,还将总结ROCK抑制剂的最新研发状况。我们的综述提供了一个基础框架,据此可以制定针对ROCK设计新先导化合物的策略。

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