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Cytomics Systems identifies new anti-cancer molecules targeting the Ubiquitin-proteasome pathway
Second-generation proteasome inhibitors open
the way to new therapies in oncology and provide a further validation of
Cytomics' UbiScreen(R) screening technology
Paris, July 8, 2005 -
Cytomics Systems, a biopharmaceutical company pioneering the discovery of
small molecules that control the degradation of proteins, today announces that
it has identified compounds able to inhibit the in vitro proliferation of
human cancer cells. These molecules act on the non-catalytic activities of the
proteasome and represent a new generation of proteasome inhibitors with
potential to create new therapies for use in the fight against cancer.
Cytomics used its proprietary high-throughput
cell-based screening technology, UbiScreen(R) to identify
these new compounds. UbiScreen(R) is a platform designed
to help develop candidate molecules targeting the Ubiquitin-proteasome protein
degradation pathway. The announcement follows Cytomics' earlier success in
preclinical trials of its hospital-acquired fungal infection treatment using
molecules also identified through UbiScreen(R).
In vitro experiments carried out by Cytomics show that the new molecules target the regulating subunits of the proteasome and should provide more efficacy and selectivity than the compounds targeting the catalytic activities of the proteasome. At present, only one drug on the market targets the Ubiquitin-proteasome pathway and it has been very successful in treating multi-resistant myeloma from both a therapeutic and a commercial point of view.
"The identification of these molecules is a
further proof of the efficacy of Cytomics' UbiScreen(R)
platform," said Dr Cécile Bougeret, Director of Research and Development at
Cytomics Systems. "Using UbiScreen(R), we can select
molecules of therapeutic interest which regulate the degradation of proteins
by the Ubiquitin-proteasome pathway."
Cytomics Systems will further optimize the newly identified molecules and expects to carry out in vivo experiments in early 2006. These tests will be carried out on nude mice xenografted with human cancer cells. Assuming positive results, Cytomics will move them into pre-clinical trials.
"With this second series of molecules, Cytomics
has taken a significant stride forward," said Dominique Thomas, president of
Cytomics Systems. "We now believe that our molecules should lead to
significant improvements in the treatment of several types of cancer."
About the Ubiquitin Proteasome pathway:
The Ubiquitin Proteasome pathway is the universal
process of protein degradation in human cells. Ubiquitin ligases are the key
enzymes that regulate this degradation by attaching a Ubiquitin "label" to the
proteins that are to be destroyed. The proteins with this tag are recognized
and eliminated by the Proteasome which then breaks them down into inactive
peptides. By regulating the concentration of proteins present in a cell, the
Ubiquitin pathway plays a key role in a large number of cellular processes,
including regulation of the cellular cycle and immune response, the control of
gene expression, and apoptosis or cell-death. Faults in the degradation of
certain proteins are known to cause major pathologies including cancer,
inflammatory disease and neurodegenerative diseases as has been pointed out by
the Swedish Academy of Science when the Nobel Prize for Chemistry 2004 was
awarded to the team who discovered this mechanism.
About Cytomics Systems:
www.cytomics.fr
Cytomics Systems, Paris, is a biopharmaceutical
company pioneering the discovery and development of small molecules that
control the degradation of proteins to treat major human diseases such as
cancer and hospital-acquired fungal infections. The company was founded in
2000 by Dr Dominique Thomas, director of research at the CNRS Center for
Molecular Genetics, and internationally recognized for his work in the field
of the ubiquitin-proteasome pathway for protein degradation. Cytomics has so
far raised EUR3M from SGAM (Société Générale Asset Management) and has 15
employees. The company has developed a highly innovative high-throughput
screening technology, UbiScreen(R) for the discovery of
new therapeutic molecules controlling the degradation of target proteins.
Cytomics is initially using this technology to target fungal hospital-acquired
infections and some types of cancer. Favorable preclinical results demonstrate
how effective these molecules can be.
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