ROCK1

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ROCK1

A gene on chromosome 18q11.1 that encodes a protein kinase, which is a key regulator of actin cytoskeleton and cell polarity. It regulates smooth muscle contraction, actin cytoskeleton organisation, stress-fibre and focal adhesion formation, and neurite retraction, as well as cell adhesion and motility via phosphorylation of DAPK3, GFAP, LIMK1, LIMK2, MYL9/MLC2, PFN1 and PPP1R12A. It phosphorylates FHOD1, and both promote SRC-dependent non-apoptotic plasma membrane blebbing. ROCK1 also: phosphorylates JIP3 and regulates JNK to JIP3 recruitment in response to UVB-induced stress; suppresses inflammatory cell migration by regulating PTEN phosphorylation and stability; downregulates VEGF-induced angiogenic endothelial cell activation; promotes keratinocyte terminal differentiation; and plays a role in terminal erythroid differentiation. ROCK1 is required for centrosome positioning and centrosome-dependent exit from mitosis. It may regulate closure of the eyelids and ventral body wall by inducing the assembly of actomyosin bundles.
References in periodicals archive ?
Based on the results of these Phase 2 studies, Kowa will continue its clinical development program in Japan and will initiate Phase 3 studies with the aim of achieving marketing authorization as the world's first Rho kinase inhibitor for the treatment of glaucoma and ocular hypertension.
Phase 2 clinical pharmacology study: Efficacy and Safety of the Rho Kinase Inhibitor, K-115, over 24 Hours in Patients with Primary Open-angle Glaucoma and Ocular Hypertension (E-Poster Presentation)(*)
Dirk Leysen adds: "Although Rho kinase or ROCK is a key player in inflammation, it has so far not been an easy drug target as known ROCK inhibitors cause unwanted side effects due to activity in other organs.
Inspire will also have five presentations related to preclinical work conducted with novel Rho kinase inhibitors in respiratory-related applications.
Studies, showed that AMA0247, a highly selective Rho Kinase (ROCK) inhibitor, was very effective in inhibiting the inflammatory reaction in the lungs, as measured by neutrophil infiltration, but had no effect on blood pressure or heart rate.
INS117548 is a Rho kinase inhibitor designed to lower IOP in glaucoma patients by disrupting the actin cytoskeleton (cellular skeleton) of the trabecular meshwork, an ocular tissue responsible for most of the outflow of aqueous humor.
AMA0076 is a novel, highly potent Rho Kinase (ROCK) inhibitor for the treatment of glaucoma, a condition which damages the optic nerve resulting in vision loss and ultimately blindness.
INS117548 is a rho kinase inhibitor designed to lower intraocular pressure (IOP) in glaucoma patients by disrupting the actin cytoskeleton (cellular skeleton) of the trabecular meshwork, an ocular tissue responsible for most of the outflow of aqueous humor.
The second glaucoma-related poster, "Topical Administration of a Novel and Potent Rho Kinase (ROK) Inhibitor INS117548 Alters the Actin Cytoskeleton, Effectively Lowers IOP, and is Well Tolerated on the Ocular Surface," shows that INS117548, which is being developed by Inspire, reduced intraocular pressure (IOP) in animal models.
The company also recently in-licensed rho kinase inhibitor, Fasudil, for development in PAH and stable angina.
He will also give an overview of the preclinical data from the Rho Kinase (ROCK) program.