Gene expression-based screening for inhibitors of PDGFR signaling.

Genome Biol

Cancer Program, Broad Institute of Massachusetts Institute of Technology and Harvard University, Cambridge Center, Cambridge, MA 02142, USA.

Published: June 2008

Here we describe a proof-of-concept experiment designed to explore the possibility of using gene expression-based high-throughput screening (GE-HTS) to find inhibitors of a signaling cascade, using platelet derived growth factor receptor (PDGFR) signaling as the example. The previously unrecognized ability of aurintricarboxylic acid to inhibit PDGFR signaling, discovered through a screen of 1,739 compounds, demonstrates the feasibility and generalizability of GE-HTS for the discovery of small molecule modulators of any signaling pathway of interest.

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http://www.ncbi.nlm.nih.gov/pmc/articles/PMC2397499PMC
http://dx.doi.org/10.1186/gb-2008-9-3-r47DOI Listing

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