S
Steven D. Knight
Researcher at GlaxoSmithKline
Publications - 26
Citations - 1649
Steven D. Knight is an academic researcher from GlaxoSmithKline. The author has contributed to research in topics: Cancer & Urotensin-II receptor. The author has an hindex of 17, co-authored 25 publications receiving 1493 citations.
Papers
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Journal ArticleDOI
Identification of Potent, Selective, Cell-Active Inhibitors of the Histone Lysine Methyltransferase EZH2.
Sharad K. Verma,Xinrong Tian,Louis V. LaFrance,Celine Duquenne,Dominic Suarez,Kenneth A. Newlander,Stuart Paul Romeril,Joelle Lorraine Burgess,Seth W. Grant,Brackley James,Alan P. Graves,Daryl A. Scherzer,Art Shu,Christine Thompson,Heidi M. Ott,Glenn S. Van Aller,Carl A. Machutta,Elsie Diaz,Yong Jiang,Johnson Neil W,Steven D. Knight,Ryan G. Kruger,Michael T. McCabe,Dashyant Dhanak,Peter J. Tummino,Caretha L. Creasy,William H. Miller +26 more
TL;DR: This work has identified highly potent, selective, SAM-competitive, and cell-active EZH2 inhibitors, including GSK926 and GSK343, which are small molecule chemical tools that would be useful to further explore the biology of EZh2.
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
Antitumor activity of an allosteric inhibitor of centromere-associated protein-E
Kenneth Wood,Latesh Lad,Lusong Luo,Xiangping Qian,Steven D. Knight,Neysa Nevins,Katjuša Brejc,David Sutton,Aidan G. Gilmartin,Penelope Chua,Radhika Desai,Stephen Schauer,Dean E. McNulty,Roland S. Annan,Lisa D. Belmont,Carmen García,Yan Lee,Melody Diamond,Leo F. Faucette,Michele Giardiniere,Shu-Yun Zhang,Chiu-Mei Sun,Justin D. Vidal,Serge Lichtsteiner,William K. Cornwell,Joel Greshock,Richard Wooster,Jeffrey T. Finer,Robert A. Copeland,Pearl S. Huang,David J. Morgans,Dashyant Dhanak,Gustave Bergnes,Roman Sakowicz,Jeffrey R. Jackson +34 more
TL;DR: Inhibition of CENP-E motor activity in cultured cells and tumor xenografts caused failure of metaphase chromosome alignment and induced mitotic arrest, indicating that tight binding of C Enp-E to microtubules is insufficient to satisfy the mitotic checkpoint.
Journal ArticleDOI
Novel ATP-competitive kinesin spindle protein inhibitors.
Cynthia A. Parrish,Nicholas D. Adams,Kurt R. Auger,Joelle Lorraine Burgess,Jeffrey D. Carson,Amita M. Chaudhari,Robert A. Copeland,Melody Diamond,Carla A. Donatelli,Kevin J. Duffy,Leo F. Faucette,Jeffrey T. Finer,William F. Huffman,Erin D. Hugger,Jeffrey R. Jackson,Steven D. Knight,Lusong Luo,Michael L. Moore,Ken A. Newlander,Lance Ridgers,Roman Sakowicz,Antony N. Shaw,Chiu-Mei M Sung,David Sutton,Kenneth W. Wood,Shu-Yun Zhang,Michael N. Zimmerman,Dashyant Dhanak +27 more
TL;DR: In a murine xenograft model with HCT116 D130V tumors, 20 showed significant antitumor activity following intraperitoneal dosing, providing in vivo proof-of-principle of the efficacy of an ATP-competitive KSP inhibitor versus tumors that are resistant to the other known KSP inhibitors.
Patent
Quinoline derivatives as P13 kinase inhibitors
Nicholas D. Adams,Amita M. Chaudhari,Carla A. Donatelli,Steven D. Knight,Kenneth A. Newlander,Cynthia A. Parrish,Lance Ridgers,Martha A. Sarpong +7 more
TL;DR: In this article, a method of inhibiting the activity/function of PI3 kinases using quinoline derivatives was proposed, which is a method for treating one or more disease states selected from: autoimmune disorders, inflammatory diseases, cardiovascular diseases, neurodegenerative diseases, allergy, asthma, pancreatitis, multiorgan failure, kidney diseases, platelet aggregation, cancer, sperm motility, transplantation rejection, graft rejection and lung injuries.