Generic placeholder image

Current Pharmaceutical Design


ISSN (Print): 1381-6128
ISSN (Online): 1873-4286

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 and Mark R. Brann

Volume 12, Issue 14, 2006

Page: [1717 - 1729] Pages: 13

DOI: 10.2174/138161206776873662

Price: $65


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)

Rights & Permissions Print Cite
© 2024 Bentham Science Publishers | Privacy Policy