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P2035
Receptor Selection & Amplification Technology  A Unique, Powerful Screening Platform for Drug Discovery
Presenter Fabrice Piu, ACADIA Pharmaceuticals, USA
Additional Authors: Ethan S. Burstein, Andria L. Del Tredici, Carsten B. Anderson, Jian-Nong MA, Erika A. Currier, Roger Olsson And Doug W. Bonhaus
In recent years, functional assays have become the tools of choice to support the identification and development of novel therapeutic drugs. However, many assay platforms have been encumbered by a number of limitations, which severely affect their broad effectiveness. The Receptor Selection and Amplification Technology (R-SAT®) offers a powerful alternative. R-SAT® has been successfully applied to various genomic targets from GPCRs, nuclear hormone receptors, cytokine receptors to receptor tyrosine kinases and intracellular signaling molecules.R-SAT® incorporates the molecular elements that drive oncogenic cell proliferation to provide a convenient, sensitive, economical and homogeneous readout to probe gene function and identify small molecule modulators. R-SAT® displays a number of unique features including enhanced sensitivity to the constitutive (non-liganded) activity of targets, and the ability to detect ligands with low intrinsic efficacy. These properties make R-SAT® particularly efficient in identifying surrogate ligands for constitutively activated receptors, peptide GPCRs and orphan receptors.R-SAT® further constitutes an ultra high-throughput platform, in which screening, pharmacology and profiling capabilities are optimally defined and merged into a single process. Combined with our integrated high-throughput medicinal chemistry functionality and large chemical library, the R-SAT® technology maximizes and accounts for rapid hit identification and Hit to Lead capabilities.