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Rho-associated protein kinase or Rho-associated coiled-coil kinase (ROCK) is a kinase belonging to the AGC (PKA/ PKG/PKC) family of serine-threonine specific protein kinases. It is involved mainly in regulating the shape and movement of cells by acting on the cytoskeleton .
The ROCK1 structure is a serine/threonine kinase with molecular weight of 158 kDa. [7] It is a homodimer composed of a catalytic kinase domain (residues76-338) [11] located at the amino or N-terminus of the protein, a coiled-coil region (residues 425-1100) [11] containing the Rho-binding domain, and a pleckstrin-homology domain (residues 1118-1317) [11] with a cysteine-rich domain.
A number of Rho kinase inhibitors are known. [15] [16] [17]Chemical structure of fasudil. AT-13148 [18]; BA-210; β-ElemeneBelumosudil; Chroman 1 [19] [20]; DJ4, which is a selective multi-specific ATP competitive inhibitor of activity of ROCK1 (IC50 of 5 nM), ROCK2 (IC50 of 50 nM), MRCKα (IC50 of 10 nM) and MRCKβ (IC50 of 100 nM) kinases without affecting activity of PAK1 and DMPK at 5 μM ...
RhoA and Rho kinase mechanisms have been linked to diabetes due to the up-regulated expression of targets within type 1 and 2 diabetic animals. Inhibition of this pathway prevented and ameliorated pathologic changes in diabetic complications, indicating that RhoA pathway is a promising target for therapeutic development in diabetes treatment [68]
The Rho family of GTPases is a family of small (~21 kDa) signaling G proteins, and is a subfamily of the Ras superfamily.The members of the Rho GTPase family have been shown to regulate many aspects of intracellular actin dynamics, and are found in all eukaryotic kingdoms, including yeasts and some plants.
Fasudil is a potent Rho-kinase inhibitor and vasodilator. [1] Since it was discovered, it has been used for the treatment of cerebral vasospasm, which is often due to subarachnoid hemorrhage, [2] as well as to improve the cognitive decline seen in stroke patients. It has been found to be effective for the treatment of pulmonary hypertension. [3]
It is a selective rho-associated coiled-coil-containing protein kinase 1 (ROCK1) inhibitor, where ROCK1 is "an important downstream effector of Rho guanosine trisphosphates (GTP)," [2] proteins that are significant in the contractile control of smooth muscle tissue. The S configuration at the 2-position on the 1,4-diazepane ring of Ripasudil is ...
The protein encoded by this gene is a serine/threonine kinase that regulates cytokinesis, smooth muscle contraction, the formation of actin stress fibers and focal adhesions, and the activation of the c-fos serum response element. This protein, which is an isozyme of ROCK1 is a target for the small GTPase Rho.