Rho Kinase (ROCK) Inhibitors and Their Therapeutic Potential

J Med Chem. 2016 Mar 24;59(6):2269-300. doi: 10.1021/acs.jmedchem.5b00683.

Yangbo Feng, Philip V LoGrasso, Olivier Defert ¹, Rongshi Li ²

Affiliations

1 Amakem Therapeutics , Agoralaan A bis, 3590 Diepenbeek, Belgium.
2 Center for Drug Discovery and Department of Pharmaceutical Sciences, College of Pharmacy, Cancer Genes and Molecular Regulation Program, Fred and Pamela Buffett Cancer Center, University of Nebraska Medical Center , 986805 Nebraska Medical Center, Omaha, Nebraska 68198, United States.

PMID: 26486225 DOI: 10.1021/acs.jmedchem.5b00683

Abstract

Rho kinases (ROCKs) belong to the serine-threonine family, the inhibition of which affects the function of many downstream substrates. As such, ROCK inhibitors have potential therapeutic applicability in a wide variety of pathological conditions including asthma, Cancer, erectile dysfunction, glaucoma, Insulin resistance, kidney failure, neuronal degeneration, and osteoporosis. To date, two ROCK inhibitors have been approved for clinical use in Japan (fasudil and ripasudil) and one in China (fasudil). In 1995 fasudil was approved for the treatment of cerebral vasospasm, and more recently, ripasudil was approved for the treatment of glaucoma in 2014. In this Perspective, we present a comprehensive review of the physiological and biological functions for ROCK, the properties and development of over 170 ROCK inhibitors as well as their therapeutic potential, the current status, and future considerations.

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