Compugen Presents Experimental Results for Three G-Protein Coupled Receptor (GPCR)...

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Tue May 20, 2008 7:30am EDT

Compugen Presents Experimental Results for Three G-Protein Coupled Receptor (GPCR) Ligands

  Results for Relaxin Related Peptides Presented at the Relaxin 2008
                              Conference
TEL AVIV, Israel--(Business Wire)--
Speaking before the 5th International Conference on Relaxin and
Related Peptides in Maui, Hawaii, Dr. Ronen Shemesh of Compugen Ltd.
(NASDAQ:CGEN) today presented experimental results for three Compugen
discovered Relaxin related molecules that could have therapeutic
activity in various clinical indications, including labor
complications, infertility, inflammation, congestive heart failure and
fibrotic diseases.

   The three novel peptides, CGEN-25009, 25010 and 25011, were
predicted in silico through the use of Compugen's GPCR Peptide
Discovery Platform and were then shown to activate the GPCRs LGR7
(RXFP1) and LGR8 (RXFP2). These receptors are known to be activated by
Relaxin and Insulin-like 3 (INSL3), respectively. CGEN-25009, 25010
and 25011 are short and linear peptides derived through the use of the
GPCR platform novel cleavage sites predictor from a precursor protein
for which there was no known function.

   In his presentation, Dr. Shemesh, project manager for the GPCR
platform, summarized recently obtained results from a series of
further experiments with the three peptides -- such as cAMP
measurements and downstream changes measured by cell impedance. In
these experiments, the activation of the GPCRs LGR7 and LGR8 was
further confirmed and additional information obtained regarding the
activity of these novel molecules. By activation of these receptors,
these peptides could potentially have a therapeutic effect in a large
number of key pathophysiological conditions. A provisional patent
application covering the peptides has been filed by Compugen.

   "Our GPCR Peptide Discovery Platform relies on a series of
sequential computational biology predictive models and machine
learning capabilities," stated Dr. Shemesh. "Therefore -- and
particularly in view of both the critical role of GPCR receptors in
the pharmaceutical world and the difficulty in finding novel ligands
through traditional experimental methods -- it is extremely rewarding
for the project team to see the continuing validation of the
platform's exceptional efficiency and accuracy," Dr. Shemesh
concluded.

   About Relaxin

   Substantial on-going world-wide research efforts are now
demonstrating that the natural peptide hormone Relaxin and its family
members (INSL3 and other insulin-like peptides) are multi-functional
factors in a broad range of target tissues including both reproductive
and other organs, in addition to their historical role as the
"pregnancy hormone". Known to activate the GPCR- LGR7 and LGR8
receptors, the diverse and vital currently known roles of Relaxin
include homeostatic roles in reproductive health, fertility and
ageing, as well as exhibiting therapeutic properties in various
pathophysiological conditions such as infertility, pregnancy and labor
complications, fibrotic diseases, inflammatory disorders, wound
healing, and cardiovascular diseases.

   About GPCRs and the GPCR Peptide Discovery Platform

   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 prescription
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.

   Compugen's previously disclosed GPCR discovery platform
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
-- which includes thousands of novel human peptide sequences -- is
based on predicting cleavage sites in precursor proteins. The
discovery platform utilizes proprietary machine-learning algorithms to
analyze the predictive peptidome and to identify peptides likely to
activate GPCRs. To date, a pilot validation discovery run and two
subsequent production runs of this platform have been completed by
Compugen. As previously disclosed with respect to the pilot run,
thirty three peptides, all novel, were synthesized and screened in a
functional assay against a panel of 152 GPCRs. Eight of these peptides
were shown to activate six different GPCRs in a
concentration-dependent manner, including some for which there are no
known endogenous ligands. CGEN-25009 and 25010, for which experimental
results are now being presented, are two of these eight peptides;
CGEN-25010 is a sub-segment of CGEN-25009, and CGEN-25011 constitutes
a smaller segment that is present in both CGEN-25009 and 25010. In
addition, this GPCR discovery platform is the basis of Compugen's
recently announced collaboration with Merck & Co., Inc.

   About Compugen

   Compugen's mission is to be the world leader in the discovery and
licensing of product candidates to the drug and diagnostic industries
under milestone and revenue sharing agreements. The Company's
increasing inventory of powerful and proprietary discovery platforms
is enabling the predictive discovery - field after field - of numerous
therapeutic and diagnostic product candidates. These discovery
platforms are based on the Company's decade-long focus on the
predictive understanding of important biological phenomena at the
molecular level. Compugen's current collaborations include Biosite,
Medarex, Inc., Merck & Co., Inc., Ortho-Clinical Diagnostics (a
Johnson & Johnson company), Roche, Siemens Healthcare Diagnostics,
Inc., and Teva Pharmaceutical Industries. In 2002, Compugen
established an affiliate -- Evogene Ltd. (TASE:EVGN.TA) -- to utilize
the Company's in-silico predictive discovery capabilities in the
agricultural biotechnology field. For additional information, please
visit Compugen's corporate Website at www.cgen.com and Evogene's
corporate Website at www.evogene.com.

   This press release may contain "forward-looking statements" within
the meaning of the Private Securities Litigation Reform Act of 1995.
These statements include words such as "may", "expects",
"anticipates", "believes", and "intends", and describe opinions about
future events. These forward-looking statements involve known and
unknown risks and uncertainties that may cause the actual results,
performance or achievements of Compugen to be materially different
from any future results, performance or achievements expressed or
implied by such forward-looking statements. Some of these risks are:
changes in relationships with collaborators; the impact of competitive
products and technological changes; risks relating to the development
of new products; and the ability to implement technological
improvements. These and other factors are identified and more fully
explained under the heading "Risk Factors" in Compugen's annual
reports filed with the Securities and Exchange Commission.

Compugen Ltd.
Dikla Czaczkes Axselbard, +972-54-530-4469
Acting Chief Financial Officer
dikla@cgen.com

Copyright Business Wire 2008
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