R
Ronald Wegrzyn
Researcher at GlaxoSmithKline
Publications - 2
Citations - 462
Ronald Wegrzyn is an academic researcher from GlaxoSmithKline. The author has contributed to research in topics: PI3K/AKT/mTOR pathway & RPTOR. The author has an hindex of 2, co-authored 2 publications receiving 410 citations.
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Journal ArticleDOI
Discovery of GSK2126458, a Highly Potent Inhibitor of PI3K and the Mammalian Target of Rapamycin
Steven D. Knight,Nicholas D. Adams,Joelle Lorraine Burgess,Amita M. Chaudhari,Michael G. Darcy,Carla A. Donatelli,Juan I. Luengo,Ken A. Newlander,Cynthia A. Parrish,Lance Ridgers,Martha A. Sarpong,Schmidt Stanley J,Glenn S. Van Aller,Jeffrey D. Carson,Melody Diamond,Patricia A. Elkins,Christine M. Gardiner,Eric Garver,Seth A. Gilbert,Richard R. Gontarek,Jeffrey R. Jackson,Kevin L. Kershner,Lusong Luo,Kaushik Raha,Christian S. Sherk,Chiu-Mei Sung,David Sutton,Peter J. Tummino,Ronald Wegrzyn,Kurt R. Auger,Dashyant Dhanak +30 more
TL;DR: 2,4-Difluoro-N-{2-(methyloxy)-5-[4-(4-pyridazinyl)-6-quinolinyl]-3- pyridinyl}benzenesulfonamide (GSK2126458, 1) has been identified as a highly potent, orally bioavailable inhibitor of PI3Kα and mTOR with in vivo activity in both pharmacodynamic and tumor growth efficacy models.
Journal ArticleDOI
Molecular Target Class Is Predictive of In vitro Response Profile
Joel Greshock,Kurtis E. Bachman,Yan Degenhardt,Junping Jing,Yuan H. Wen,Stephen Eastman,Elizabeth McNeil,Christopher Moy,Ronald Wegrzyn,Kurt R. Auger,Mary Ann Hardwicke,Richard Wooster +11 more
TL;DR: A cohort of PI3K/AKT/mTOR inhibitors was more efficacious in breast cancers compared with other tumor types, whereas IGF-IR inhibitors more selectively inhibited growth in colon cancer lines.