Discovery of GSK2126458, a Highly Potent Inhibitor of PI3K and the Mammalian Target of Rapamycin.

Abstract

Phosphoinositide 3-kinase α (PI3Kα) is a critical regulator of cell growth and transformation, and its signaling pathway is the most commonly mutated pathway in human cancers. The mammalian target of rapamycin (mTOR), a class IV PI3K protein kinase, is also a central regulator of cell growth, and mTOR inhibitors are believed to augment the antiproliferative… (More)
DOI: 10.1021/ml900028r

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@article{Knight2010DiscoveryOG, title={Discovery of GSK2126458, a Highly Potent Inhibitor of PI3K and the Mammalian Target of Rapamycin.}, author={Steven D. Knight and Nicholas D Adams and Joelle L Burgess and Amita M Chaudhari and Michael G Darcy and Carla A Donatelli and Juan I Luengo and Ken A Newlander and Cynthia A Parrish and Lance H Ridgers and Martha A Sarpong and Stanley J Schmidt and Glenn S. Van Aller and Jeffrey D Carson and Melody A Diamond and Patricia A Elkins and Christine M Gardiner and Eric M. Garver and Seth A Gilbert and Richard R. Gontarek and Jeffrey R. Jackson and Kevin L Kershner and Lusong Luo and Kaushik Raha and Christian S Sherk and Chiu-mei Sung and D. Sutton and Peter J. Tummino and Ronald J Wegrzyn and Kurt R. Auger and Dashyant Dhanak}, journal={ACS medicinal chemistry letters}, year={2010}, volume={1 1}, pages={39-43} }