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

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

doi:10.1016/j.drudis.2013.09.010

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

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

Authors

Peichen Pan¹, Mingyun Shen, Huidong Yu, Youyong Li, Dan Li, Tingjun Hou

Affiliation

¹ Institute of Functional Nano & Soft Materials (FUNSOM) and Jiangsu Key Laboratory for Carbon-Based Functional Materials & Devices, Soochow University, Suzhou, Jiangsu 215123, China.

PMID: 24076262
DOI: 10.1016/j.drudis.2013.09.010

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.

Publication types

Research Support, Non-U.S. Gov't
Review

MeSH terms

Animals
Drug Design*
Humans
Protein Kinase Inhibitors / pharmacology*
rho-Associated Kinases / antagonists & inhibitors*
rho-Associated Kinases / metabolism

Substances

Protein Kinase Inhibitors
ROCK1 protein, human
ROCK2 protein, human
rho-Associated Kinases