Compugen Ltd (CGEN)

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Compugen Announces Discovery of Eight Novel G-Protein Coupled Receptor (GPCR) Peptide Ligands
Tuesday February 20, 7:00 am ET
Results From Initial Use of New Discovery Engine to Be Presented at Two Leading International Conferences


TEL AVIV, Israel--(BUSINESS WIRE)--Compugen Ltd. (NASDAQ:CGEN - News) announced today that it has developed a GPCR ligand discovery engine and that use of the engine to date has resulted in Compugen's discovery of eight novel peptides that activate GPCRs. The new peptide ligands will be presented at Screening Europe (February 20-21, 2007, Barcelona, Spain) and at CHI's Molecular Medicine Tri-Conference (February 27-March 2, San Francisco, CA).

GPCRs are membrane protein receptors that are involved in signal transduction of numerous physiological processes. GPCRs are by far the largest family of known drug targets, and at least 40% of drugs currently available are thought to act on GPCRs. Furthermore, newly discovered GPCR peptide ligands have in the past shown a high probability of being successfully developed into new drugs.

The new discovery engine utilized by Compugen in making these discoveries incorporates a proprietary model of the "peptidome", an in silico prediction of probable human peptides. Peptides are formed through the cleavage of precursor proteins, and Compugen's proprietary peptidome -- already consisting of thousands of novel human peptide sequences -- is based on predicting cleavage sites in precursor proteins.

The discovery engine uses proprietary machine-learning algorithms to analyze the predictive peptidome and to date has identified hundreds of peptides likely to activate GPCRs. Thirty three of these peptides, all novel, have been synthesized and screened in a functional assay against a panel of 152 GPCRs. Eight peptides were shown to activate six different GPCRs in a concentration-dependent manner, including some for which there are no known endogenous ligands. The receptors for which novel ligands have been discovered include the MAS1 and MAS-related GPCRs, MRGX1 and MRGX2, as well as FPRL1 and two of the Relaxin family receptors, RXFP1 and RXFP2.

"This is another example of how the capabilities that have been developed over the past decade at Compugen now allow us to address important unmet needs in drug discovery with unique predictive platforms. In this case, our initial use of a newly developed engine incorporating our predicted peptidome has resulted in the identification of eight novel GPCR peptide ligands. In addition, we believe that the hundreds of candidates that we haven't yet tested hold potential for many similar discoveries," said Yossi Cohen, M.D., Vice President of Research and Development, Compugen Ltd. "Out of the eight ligands already discovered, we have selected two for further development at Compugen. Others are undergoing an evaluation process both for in-house development and for out-licensing opportunities."

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