GPCR Ligands

GPCRs are desirable drugs targets – with at least 40% of drugs currently in the market thought to modulate GPCRs. Our GPCR platform aims at finding novel peptide ligand agonists to GPCRs that could become drug candidates and is based on ourcapability to identify GPCR activating peptides (Shemesh et al., 2008) from our predicted peptidome. Our underlying peptidome is a collection of thousands of novel human peptide sequences which are expected to be endogenous peptides, and was created by predicting novel cleavage sites in precursor proteins (Kliger et al., 2008). Using this proprietary platform we have to date, identified eight novel peptides that activate six different GPCRs and have advanced three peptides into in vivo studies.The receptors for which novel ligands have been discovered include the MAS1 and MAS-related GPCRs, MRGX1 and MRGX2, as well asFPRL1(Hecht et al., 2008) and two of the Relaxin family receptors, RXFP1 and RXFP2.

Compugen's GPCR targeted library is under a commercialization collaboration with DiscoveRx .