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Rho-associated kinase 1 (ROCK1) is a serine/threonine protein kinase that plays a central role in regulating the actin cytoskeleton, cell shape, motility, contraction, and adhesion. It is one of two closely related isoforms in mammals—the other being ROCK2—and acts as a major downstream effector of the small GTPase RhoA. ROCK1 regulates smooth muscle contraction, actin cytoskeleton organization, cell migration, and other cellular processes by phosphorylating substrates like MLC, MYPT1, and LIMK. Dysregulation has been implicated in cardiovascular diseases, cancer metastasis, neurodegenerative disorders, and fibrosis.
ROCK1 inhibitors block the kinase activity of ROCK1, preventing the phosphorylation of downstream targets such as MLC, MYPT1, and LIMK. This leads to decreased smooth muscle contraction, altered cytoskeletal organization, and reduced cell motility and invasion.
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