Cytomics Pharmaceuticals has currently several drug discovery programs in two major therapeutic areas.


• Anti-Fungal Program

The ubiquitin-proteasome pathway is essential for the growth and survival of pathogenic fungi such as Candida albicans, Candida glabrata and Aspergillus fumigatus. Cytomics Pharmaceuticals has identified a fungal cell regulator whose degradation by the ubiquitin-proteasome pathway is absolutely necessary for fungi survival. Furthermore, this protein is specific of these pathogenic fungi and is not found in human cells.

A large scale screening performed on this target thanks to UbiScreen proprietary technology allowed to identify several active molecules with a « Lead potential ».
In vitro testing demonstrated that these molecules are more active than Fluconazole (Triflucan®), on pathogenic fungi prolifération.
In vivo testing demonstrated that these molecules are very well-tolerated in animals and are active against systemic infection in mice.
These pre-Leads are in optimization phase.

• Anti-Cancer Program

Many form of cancers are linked to altered protein degradation rates. This is because the ubiquitin-proteasome pathway controls the degradation of important regulators of cell cycle progression. For instance, the ubiquitin-proteasome pathway controls the activity of many oncoproteins, such as c-Myc, c-Jun, c-Fos and beta-catenin, that if not properly removed from the cell, promote cancer. In addition, the ubiquitin-proteasome pathway controls the activity of many tumor suppressor genes, such as p53, p21 and p27, whose increased degradation promote cancer.
In the wake of the anti-tumoral activity of the proteasome inhibitor Velcade®, Cytomics Pharmaceuticals decided to use UbiScreen proprietary technology to identify new therapeutic class of proteasome inhibitors.

Two large scale screenings performed thanks to UbiScreen proprietary technology allowed to identify new inhibitors of proteasome activity.
Optimization of these new class of compounds is in progress.

 

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