< Back to Publications
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|
|Date Published (YYYY/MM/DD)||2007/04/01|