Method
Gene expression-based screening for inhibitors of PDGFR signaling
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* Corresponding author: Todd R Golub golub@broad.harvard.edu
1 Cancer Program, Broad Institute of Massachusetts Institute of Technology and Harvard University, Cambridge Center, Cambridge, MA 02142, USA
2 Department of Pediatric Oncology, Dana-Farber Cancer Institute and Harvard Medical School, Binney Street, Boston, MA 02115, USA
3 Department of Chemistry, Massachusetts Institute of Technology, Massachusetts Avenue, Cambridge, MA 02139, USA
4 Departments of Biological Sciences and Chemistry, Columbia University, Fairchild Center MC2406, Amsterdam Avenue, New York, NY 10027, USA
5 Howard Hughes Medical Institute, Jones Boulevard, Chevy Chase, MD 20815, USA
6 Current address: Advanced Genetic Analysis, Applied Biosystems, Cummings Center, Beverly, MA 01915, USA
Genome Biology 2008, 9:R47 doi:10.1186/gb-2008-9-3-r47
Published: 1 March 2008Abstract
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.