L
Lance Ridgers
Researcher at GlaxoSmithKline
Publications - 19
Citations - 957
Lance Ridgers is an academic researcher from GlaxoSmithKline. The author has contributed to research in topics: Transplantation & Cancer. The author has an hindex of 13, co-authored 19 publications receiving 897 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.
Patent
Quinoline derivatives as pi3 kinase inhibitors
Nicholas D. Adams,Joelle Lorraine Burgess,Darcy Michael Gerard,Carla A. Donatelli,Steven David Knight,Kenneth A. Newlander,Lance Ridgers,Martha A. Sarpong,Schmidt Stanley J +8 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.
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.
Journal ArticleDOI
Nonpeptidic urotensin‐II receptor antagonists I: in vitro pharmacological characterization of SB‐706375
Stephen A. Douglas,David J. Behm,Nambi Aiyar,Diane Naselsky,Jyoti Disa,David P. Brooks,Eliot H. Ohlstein,John G Gleason,Henry M. Sarau,James J. Foley,Peter T. Buckley,Dulcie B. Schmidt,William E. Wixted,Widdowson Katherine L,Graham J. Riley,Jian Jin,Timothy Francis Gallagher,Schmidt Stanley J,Lance Ridgers,Lisa T. Christmann,Richard M. Keenan,Steven D. Knight,Dashyant Dhanak +22 more
TL;DR: SB‐706375 is a high‐affinity, surmountable, reversible and selective nonpeptide UT receptor antagonist with cross‐species activity that will assist in delineating the pathophysiological actions of U‐II in mammals.