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Chemistry & biology DOI:10.1016/j.chembiol.2007.02.004

Identification of a small-molecule inhibitor of class Ia PI3Ks with cell-based screening.

Publication TypeJournal Article
Year of Publication2007
AuthorsYang, J, Shamji, A, Matchacheep, S, Schreiber, SL
JournalChemistry & biology
Volume14
Issue4
Pages371-7
Date Published2007/04/01
ISSN1074-5521
Abstract

The mammalian target of rapamycin (mTOR) signaling network is central to the regulation of cell growth in response to both growth factors and nutrients. We developed a high-throughput, cell-based assay to identify small-molecule modulators of the mTOR signaling network. One such compound, which we name quinostatin, potently inhibits this network by directly targeting the lipid-kinase activity of the catalytic subunits of class Ia PI3Ks. This study illustrates the power of unbiased, phenotypic screening as a means for illuminating cell circuitry, and resulted in the identification of a chemotype for selective inhibition of the class Ia PI3Ks.

URLhttp://linkinghub.elsevier.com/retrieve/pii/S1074-5521(07)00071-3
DOI10.1016/j.chembiol.2007.02.004
Pubmed

http://www.ncbi.nlm.nih.gov/pubmed/17462572?dopt=Abstract