[HTML][HTML] The cAMP-responsive Rap1 guanine nucleotide exchange factor, Epac, induces smooth muscle relaxation by down-regulation of RhoA activity

BJ Zieba, MV Artamonov, L Jin, K Momotani… - Journal of Biological …, 2011 - ASBMB
Agonist activation of the small GTPase, RhoA, and its effector Rho kinase leads to down-
regulation of smooth muscle (SM) myosin light chain phosphatase activity, an increase in
myosin light chain (RLC 20) phosphorylation and force. Cyclic nucleotides can reverse this
process. We report a new mechanism of cAMP-mediated relaxation through Epac, a GTP
exchange factor for the small GTPase Rap1 resulting in an increase in Rap1 activity and
suppression of RhoA activity. An Epac-selective cAMP analog, 8-pCPT-2′-O-Me-cAMP (" …