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Genome Biol DOI:10.1186/gb-2008-9-3-r47

Gene expression-based screening for inhibitors of PDGFR signaling.

Publication TypeJournal Article
Year of Publication2008
AuthorsAntipova, AA, Stockwell, BR, Golub, TR
JournalGenome Biol
Date Published2008
KeywordsAurintricarboxylic Acid, Cell Line, Tumor, Drug Evaluation, Preclinical, Extracellular Signal-Regulated MAP Kinases, Gene Expression, Humans, Protein Kinase Inhibitors, Receptor, Platelet-Derived Growth Factor alpha, Receptor, Platelet-Derived Growth Factor beta, Signal Transduction, Structure-Activity Relationship

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.


Alternate JournalGenome Biol.
PubMed ID18312689
PubMed Central IDPMC2397499
Grant ListR01 CA097061 / CA / NCI NIH HHS / United States
CA97061 / CA / NCI NIH HHS / United States
/ / Howard Hughes Medical Institute / United States