The European ScreeningPort (ESP) is a public-private partnership that works for academic institutions to create and operate drug discovery programs that address novel therapeutic targets. Their key competency lies in early stage (target-to-lead) small molecule discovery, using a screening approach.
The ESP's state-of-the-art screening infrastructure includes access to up to 400,000 "ready-to-screen" compounds designed to address a range of target classes including those with specific relevance to neurological disease and protein::protein interactions like those associated with intracellular signaling pathways.
Getting Physiologically Relevant Results Is Not Always Easy
Promising results on the causes of disease, generated during basic research, require specific processes in order to accelerate the translation of these results into new therapeutics. Until recently, those processes have only been available to the pharmaceutical industry.
In addition, researchers often use synthetic peptides or engineered cell lines as they are easier to handle. However, they bear little relation to the underlying disease biology compared to the physiologically relevant results that can be obtained with native protein substrates or primary cells.
"Our infrastructure is based around the fully integrated PerkinElmer robotic cell::explorer® automated high content screening system, which forms the centerpiece of the ESPs in-vitro screening facility."
Pharmaceutical-Grade Results for Academia
To aid the acceleration of promising results into therapeutics, the ESP's core infrastructure is based around the fully-integrated PerkinElmer robotic cell::explorer® automated high content screening system. The system handles 96 to 1536 well microplates with integrated nanoliter-scale dispensing, industry standard liquid handling for larger volumes, robust plate handling and sensitive multi-mode optical based readouts. This infrastructure allows the ESP to provide mainstream, physiologically relevant optical assay readouts, commonly found within the pharmaceutical industry, to its academic customers, including high content imaging, AlphaScreen® assays and time-resolved FRET.
From Academic Target Identification to Identification of Potential Therapeutic Candidates
Approximately 40 percent of the academic targets investigated by ESP involve hit finding to identify small molecules that selectively disrupt protein::protein or protein::DNA interactions. PerkinElmer's AlphaScreen technology is used to identify hits in these target classes, and a "toolbox" of donor and acceptor bead combinations rapidly identifies optimal assay formats.
To follow up on hits, the ESP uses high content imaging, including PerkinElmer's confocal Opera® High Content Screening System, to directly visualize cellular processes and interactions, and to localize and quantify individual protein interactions and modifications.
ESP gives major German academic institutions, as well as academics in Canada, The Netherlands, New Zealand, Switzerland and the United Kingdom, a pathway to physiologically relevant results. Typical projects integrate medicinal chemistry insight with in-vitro and in-silico structural and disease biology knowledge to help researchers identify which molecules have the best chance of being translated from the laboratory to the clinical setting.
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