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CGEN-855
FPRL1 (also known as FPR2, ALX or ALXR) belongs to the FPR family of GPCRs that also includes FPR1 and FPRL2. It is expressed mainly by neutrophils and monocytes, as well as T-cells and other non-hematopoietic cell types, and its activation promotes resolution of inflammation, leading to prominent anti-inflammatory activity. Experiments in animal models indicate that FPRL1 agonists have a beneficial effect in acute inflammatory conditions, such as ischemia-reperfusion injury and organ transplantation, as well as in chronic inflammatory diseases such as inflammatory bowel disease and asthma. In accordance with these findings, the FPRL1 pathway has recently gained high recognition for its significance in therapy of inflammatory diseases.
Using a proprietary discovery platform aimed at the discovery of novel GPCR ligands (Shemesh et al., 2008), Compugen recently revealed a novel FPRL1 agonistic peptide, designated CGEN-855. CGEN-855 has shown anti inflammatory activity when tested in animal models of acute inflammation (air pouch model) and exhibited a cardioprotective effect following reperfusion-injury in models of acute myocardial infarction in mice and rats (Hecht et al., 2008). The beneficial activity of CGEN-855 observed in these models was accompanied by inhibition of PMNs recruitment to the inflamed site. CGEN-855 has also shown to be beneficial in a model of inflammatory bowel disease. These results support the potential of CGEN-855 to have beneficial therapeutic effects in the treatment of acute and chronic inflammation, as well as cardiovascular diseases.
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