Integrative Functional Assays, Chemical Genomics and High Throughput Screening: Harnessing Signal Transduction Pathways to a Common HTS Readout

Author(s): Ethan S. Burstein, Fabrice Piu, Jian-Nong Ma, Jacques T. Weissman, Erika A. Currier, Norman R. Nash, David M. Weiner, Tracy A. Spalding, Hans H. Schiffer, Andria L. Del Tredici, Mark R. Brann.

Journal Name: Current Pharmaceutical Design

Volume 12 , Issue 14 , 2006

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Chemical genomics is a drug discovery strategy that relies heavily on high-throughput screening (HTS) and therefore benefits from functional assay platforms that allow HTS against all relevant genomic targets. Receptor Selection and Amplification Technology (R-SAT™) is a cell-based, high-throughput functional assay where the receptor stimulus is translated into a measurable cellular response through an extensive signaling cascade occurring over several days. The large biological and chronological separation of stimulus from response provides numerous opportunities for enabling assays and increasing assay sensitivity. Here we review strategies for building homogeneous assay platforms across large gene families by redirecting and/or amplifying signal transduction pathways.

Keywords: Receptor Selection and Amplification Technology, G-protein coupled receptor (GPCR), GPCR assay, fluorescence polarization (FP), histone acetylase transfer activity (HAT)

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Article Details

Year: 2006
Page: [1717 - 1729]
Pages: 13
DOI: 10.2174/138161206776873662
Price: $65

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