Antipova Alena A, Stockwell Brent R, Golub Todd R
Cancer Program, Broad Institute of Massachusetts Institute of Technology and Harvard University, Cambridge Center, Cambridge, MA 02142, USA.
Genome Biol. 2008;9(3):R47. doi: 10.1186/gb-2008-9-3-r47. Epub 2008 Mar 1.
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.
在此我们描述了一项概念验证实验，该实验旨在探索利用基于基因表达的高通量筛选（GE-HTS）来寻找信号级联反应抑制剂的可能性，以血小板衍生生长因子受体（PDGFR）信号传导为例。通过对1739种化合物的筛选发现，金精三羧酸具有此前未被认识到的抑制PDGFR信号传导的能力，这证明了GE-HTS用于发现任何感兴趣信号通路的小分子调节剂的可行性和通用性。
