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Eur J Med Chem. 2013 Dec;70:613-22. doi: 10.1016/j.ejmech.2013.10.048. Epub 2013 Oct 25.

Advances in the studies of roles of Rho/Rho-kinase in diseases and the development of its inhibitors.

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  • 1School of Pharmaceutical Sciences, Sun Yat-Sen University, Guangzhou 510006, China.


RhoA/Rho-kinase pathway plays a pivotal role in numerous fundamental cellular functions including contraction, motility, proliferation, differentiation and apoptosis. The pathway is also involved in the development of many diseases such as vasospasm, pulmonary hypertension, cancer and central nervous systems (CNS) disorders. The inhibitors of Rho kinase have been extensively studied since the Rho/Rho-kinase pathway was verified as a target for a number of diseases. Herein, we reviewed the advances in the studies of the roles of Rho/Rho-kinase in diseases and the development of Rho-kinase inhibitors in recent five years.

Copyright © 2013 Elsevier Masson SAS. All rights reserved.


5-HT; 5-hydroxytryptamine; ACS; AP-1; AT1; C-terminal cysteine-rich domain; CNS; CPI-17; CPK; CRD; CRMP-2; Central nervous system; DMPK; ERK; ERM; ET-1; Fasudil; GAPs; GDIs; GDP dissociation inhibitors; GEFs; GTPase-activating proteins; HCC; IP3; Inhibitors; LDH; MCP-1; MEK; MES; MLC; MRCK; MYPT-1; NLSs; OpN; PAH; PAI-1; PH; PKC-potentiated inhibitory protein 17; PTEN; PTZ; RBD; ROCK; Rho kinase; Rho-binding domain; Rho-kinase; RhoA; UPS; VA; VCAM-1; VSMC; activator protein-1; acute coronary syndrome; angiotensin II type 1 receptor; central nervous system; collapsin response mediator protein 2; creatine phosphokinase; endothelin-1; extracellular signal-regulated kinase; ezrin/radixin/moesin family; guanine nucleotide exchange factors; hepatocellular carcinoma; inositol 1,4,5-trisphosphate; lactate dehydrogenase; maximal electroconvulsive shock; mitogen-activated protein kinase; monocyte chemoattractant protein-1; myosin light chain; myosin phosphatase target subunit 1; myotonic dystrophy kinase; myotonic dystrophy kinase-related CDC42-binding kinase; nuclear localization signals; optic nerve; pentylenetetrazole; phosphatase and tensin homolog deleted on chromosome 10; plasminogen activator inhibitor-1; pleckstrin homology; pulmonary arterial hypertension; ubiquitin–proteasome system; vascular cell adhesion molecule-1; vascular smooth muscle cell; vasospastic angina

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