C
Chiu-Mei Sung
Researcher at GlaxoSmithKline
Publications - 6
Citations - 405
Chiu-Mei Sung is an academic researcher from GlaxoSmithKline. The author has contributed to research in topics: Cell growth & PI3K/AKT/mTOR pathway. The author has an hindex of 4, co-authored 6 publications receiving 351 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
Discovery of the First Potent and Selective Inhibitor of Centromere-Associated Protein E: GSK923295
Xiangping Qian,Andrew Mcdonald,Han-Jie Zhou,Nicholas D. Adams,Cynthia A. Parrish,Kevin J. Duffy,Duke M. Fitch,Rosanna Tedesco,Luke W. Ashcraft,Bing Yao,Hong Jiang,Jennifer Kuo Chen Huang,Melchor V. Marin,Carrie E. Aroyan,Jianchao Wang,Seyed Ahmed,Joelle Lorraine Burgess,Amita M. Chaudhari,Carla A. Donatelli,Michael G. Darcy,Lance Ridgers,Ken A. Newlander,Schmidt Stanley J,Deping Chai,Mariela Colón,Michael N. Zimmerman,Latesh Lad,Roman Sakowicz,Stephen Schauer,Lisa D. Belmont,Ramesh Baliga,Daniel W. Pierce,Jeffrey T. Finer,Zhengping Wang,Bradley P. Morgan,David J. Morgans,Kurt R. Auger,Chiu-Mei Sung,Jeffrey D. Carson,Lusong Luo,Erin D. Hugger,Robert A. Copeland,David Sutton,John D. Elliott,Jeffrey R. Jackson,Kenneth Wood,Dashyant Dhanak,Gustave Bergnes,Steven D. Knight +48 more
TL;DR: The discovery of the first potent and selective inhibitor of centromere-associated protein E (CENP-E) 3-chloro-N-{(1S)-2-[(N,N-dimethylglycyl)amino]-1-[(4-{8-[( 1S)-1-hydroxyethyl]imidazo[1,2-a]pyridin-2-yl}phenyl)methyl]ethyl-4-[(1
Journal ArticleDOI
Conformation-Dependent Ligand Regulation of ATP Hydrolysis by Human KSP: Activation of Basal Hydrolysis and Inhibition of Microtubule-Stimulated Hydrolysis by a Single, Small Molecule Modulator
Lusong Luo,Jeffrey D. Carson,Kathleen S. Molnar,Steven J. Tuske,Stephen J. Coales,Yoshitomo Hamuro,Chiu-Mei Sung,Valery Sudakin,Kurt R. Auger,Dashyant Dhanak,Jeffrey R. Jackson,Pearl S. Huang,Peter J. Tummino,Robert A. Copeland +13 more
TL;DR: A small-molecule modulator, KSPA-1, is reported that activates KSP-catalyzed ATP hydrolysis in the absence of microtubules yet inhibits microtubule-stimulated ATP Hydrolysis by KSP, providing a novel mechanism for targeting KSP and perhaps other mitotic kinesins.
Journal Article
A potent and selective inhibitor of the mitotic kinesin CENP-E (GSK923295A), demonstrates a novel mechanism of inhibiting tumor cell proliferation and shows activity against a broad panel of human tumor cell lines in vitro
David Sutton,Aidan G. Gilmartin,Anna Kusnierz,Chiu-Mei Sung,Lusong Luo,Jeffrey D. Carson,Sylvie Laquerre,William K. Cornwell,Andrew G. King,Steven D. Knight,Dashyant Dhanak,Gustave Bergnes,Xiangping Qian,Penelope Chua,Kenneth W. Wood,Pearl S. Huang,Barbara L. Weber,Robert A. Copeland,Jeffrey R. Jackson +18 more
TL;DR: GSK923295A, which is currently in Phase I clinical trials, is a novel and selective inhibitor of CENP-E ATPase activity with a Ki of 3.2nM, and it was tested for anti-proliferative activity against 214 solid and 85 hematological tumor cell lines.
Proceedings ArticleDOI
Abstract C62: Identification of GSK2126458, a highly potent inhibitor of phosphoinositide 3‐kinase (PI3K) and the mammalian target of rapamycin (mTOR)
Steven D. Knight,Nicholas D. Adams,Joelle Lorraine Burgess,Amita M. Chaudhari,Michael G. Darcy,Carla A. Donatelli,Ken A. Newlander,Cynthia A. Parrish,Lance Ridgers,Martha A. Sarpong,Schmidt Stanley J,Glenn S. Van Aller,Jeffrey D. Carson,Patricia A. Elkins,Melody Diamond,Christine M. Gardiner,Eric Garver,Lusong Luo,Kaushik Raha,Chiu-Mei Sung,Peter J. Tummino,Kurt R. Auger,Dashyant Dhanak +22 more
TL;DR: Following a chemistry lead optimization effort, the pyridylsulfonamide GSK2126458 was identified as a highly potent, orally bioavailable, pan‐PI3K and mTOR inhibitor and is being evaluated currently in human clinical trials for the treatment of cancer.