Gene expression-based screening for inhibitors of PDGFR signaling.
Genome Biol, 2008;9(3):R47.
Antipova AA[1], Stockwell BR, Golub TR
Affiliations
PMID: 18312689DOI: 10.1186/gb-2008-9-3-r47
Impact factor: 17.906
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.
MeSH terms
Aurintricarboxylic 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
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