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Identification of a small-molecule inhibitor of class Ia PI3Ks with cell-based screening.
| Publication Type | Journal Article |
| Authors | Yang, J., Shamji A., Matchacheep S., and Schreiber SL |
| 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. |
| Year of Publication | 2007 |
| Journal | Chemistry & biology |
| Volume | 14 |
| Issue | 4 |
| Pages | 371-7 |
| Date Published (YYYY/MM/DD) | 2007/04/01 |
| ISSN Number | 1074-5521 |
| DOI | 10.1016/j.chembiol.2007.02.004 |
| PubMed | http://www.ncbi.nlm.nih.gov/pubmed/17462572?dopt=Abstract |
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