• A high throughput screening technology

Cytomics Pharmaceuticals is utilizing its proprietary UbiScreen technology to advance the discovery of drugs controlling protein turnover. This technology provides a cell-based screening method applicable to all proteins known to be degraded by the ubiquitin-proteasome pathway.

The UbiScreen platform represents a breakthrough technology that bridges high throughput and high specificity within the same screening assay. With this technology, Cytomics Pharmaceuticals has already identified compounds that modulate the degradation of a key substrate of the ubiquitin-proteasome pathway.

• Yeast micro-laboratories

The UbiScreen technology is using genetically modified yeast cells as "micro laboratories" in which the degradation mechanisms of human proteins are reconstituted.

The use of yeast ensures high throughput screening capabilities and provides functional assays with a physiological environment mimicking the final therapeutic environment. This offers the important advantage of eliminating very early compounds that could never be developed into drugs because of their toxicity, metabolic instability or insufficient ability to cross cell membranes.

• Monitoring protein degradation

Cytomics Pharmaceuticals has developed specific molecular tools allowing the reconstitution of the human protein degradation mechanisms in yeast cells. These tools allow to tightly regulate the co-expression of human protein targets and key components of the human proteasome pathway, in the same yeast cell line. Cytomics Pharmaceuticals has already generated a unique collection of yeast cell lines that provide assays to screen for compounds modulating the turnover of human proteins.

The UbiScreen technology can be automated to perform high throughput screening of large compound libraries. In its Gif-sur-Yvette facilities, Cytomics Pharmaceuticals has implemented its UbiScreen technology on a Tecan Genesis Freedom platform and works with a 125.000 small molecules library.

• UbiScreen competitive advantages

The UbiScreen technology offers significant advantages over other screening methods including :

• Universally applicable to all proteins recognized
  by the ubiquitin-proteasome pathway
• Highly reproducible and highly sensitive assays
• Highly specific assays with low background

Cytomics Pharmaceuticals possesses a highly competitive cell-based screening technology to identify promising leads for therapeutic intervention.

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