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

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

Volume: 12 Issue: 14

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 and Mark R. Brann

Affiliation:

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

Abstract: 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.

Cite this article as:

Burstein S. Ethan, Piu Fabrice, Ma Jian-Nong, Weissman T. Jacques, Currier A. Erika, Nash R. Norman, Weiner M. David, Spalding A. Tracy, Schiffer H. Hans, Del Tredici L. Andria and Brann R. Mark, Integrative Functional Assays, Chemical Genomics and High Throughput Screening: Harnessing Signal Transduction Pathways to a Common HTS Readout, Current Pharmaceutical Design 2006; 12 (14) . https://dx.doi.org/10.2174/138161206776873662