Compugen Ltd. has announced the positive in-vivo results for two novel peptide agonists of the MAS G-protein coupled receptor (GPCR), indicating cardio-protective effects and therapeutic potential for the treatment of various cardiovascular and other pathologies.
The two peptides – CGEN-856 and CGEN-857 – were identified using the Company’s previously announced GPCR ligand discovery platform. The in-vivo results will be presented at the VII International Symposium on Vasoactive Peptides to be held February 14-16, 2008 in Brazil.
In an in-vivo model of cardiac remodeling, CGEN-856 and CGEN-857 were shown to afford significant cardio protection, as manifested by reduction of both fibrosis and hypertrophy of cardiomyocytes. Moreover, picomolar concentrations of the peptides had an anti-arrhythmogenic effect in isolated rat hearts following ischemia-reperfusion, as demonstrated by a reduction in the incidence and duration of reperfusion arrhythmias.
In addition, sub-nanomolar concentrations of these peptides demonstrated significant dose-dependant relaxation of rat aorta. Through the reduction of cardiac remodeling and a unique vasodilatatory effect, these peptides could offer a novel approach to heart failure and other cardiovascular conditions. Heart failure is a major cause of morbidity and mortality worldwide. It affects millions of people in the US and, despite continued efforts, mortality remains very high.