Rho-kinase inhibitors (rho-associated protein kinase inhibitor or ROCK inhibitor) are a series of compounds that target rho kinase (ROCK) and inhibit the ROCK pathway. [1] Clinical trials have found that inhibition of the ROCK pathway contributes to the …

Rho kinases (ROCKs) are effectors of the Rho pathways (Rho activates ROCKs) [2] [3]. There are two identified types of ROCKs referred to as ROCK1 [4] and ROCK2 [5]. Both are serine/tyrosine kinases. One of the main functions of ROCKs is to aid …

Rho kinase inhibitors work to treat diabetic retinopathy by decreasing the adhesion of leukocytes and by slowing leukocyte-induced damage. Used as an intravitreal injection, the Rho kinase inhibitor slows the synthesis of various downstream proteins in the Rho pathway as well as ICAM-1.

The carboxy-terminal regions of ROCKs serve as an autoregulatory inhibitor of the amino-terminal kinase domain. 9 The interaction of the active GTP-bound form of Rho to ROCK’s RBD increases ROCK activity through derepression of the carboxyl-terminal RBD-PH domain on the amino-terminal kinase domain, leading to an active “open” kinase domain.

Rho kinase (ROCK) inhibitors are a new class of glaucoma drugs with a novel mechanism of action and good safety profile. They exert neuroprotective effects, act on the trabecular tissue, increase the outflow of aqueous humor, and reduce intraocular pressure.

2018年2月13日 · Rho kinase inhibitors are effective alone or when combined with other known ocular hypotensive medications. They also offer the possibility of neuroprotective activity, a favorable impact on ocular blood flow, and even an antifibrotic effect that may prove useful in conventional glaucoma surgery.

2016年3月24日 · 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.

Relaxing Trabecular meshwork (TM) tissue, Rho-Kinase (ROCK) inhibitors directly decrease resistance in the conventional AH outflow, thus resulting in a significant IOP-lowering effect.

2020年9月2日 · Rho Kinase Inhibitors increase drainage of intraocular fluid by improving outflow of the trabecular meshwork. Side Effects. Side effects can include eye redness, corneal deposits, stinging, and small bleeds on the white of the eye.

2024年9月16日 · Topical therapies targeting Rho-associated protein kinase (ROCK) signalling, including netarsudil (Rhopressa®) and ripasudil (Glanatec®), have become widely adopted as part of standard clinical...