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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
Volume9
Issue3
PagesR47
Date Published2008
ISSN1474-760X
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
Abstract

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.

URLhttp://genomebiology.com/content/9/3/R47
DOI10.1186/gb-2008-9-3-r47
Pubmed

http://www.ncbi.nlm.nih.gov/pubmed/18312689?dopt=Abstract

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