Dennis Lee
GlaxoSmithKline
13 Papers
34 Citations
Dennis Lee is an academic researcher from GlaxoSmithKline. The author has contributed to research in topics: Chemistry & Apoptosis. The author has an hindex of 10, co-authored 13 publications.
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Papers
Regulation of stress-induced cytokine production by pyridinylimidazoles; inhibition of CSBP kinase
Timothy Francis Gallagher,George Leslie Seibel,Shouki Kassis,Jeffrey T. Laydon,Mary Jane Blumenthal,John C. Lee,Dennis Lee,Jeffrey C. Boehm,Susan M. Fier-Thompson,Jeffrey W. Abt,Margaret E. Soreson,Juanita M. Smietana,Ralph Hall,Ravi Shanker Garigipati,Paul Elliot Bender,Karl F. Erhard,Arnold J. Krog,Glenn A. Hofmann,Peter L. Sheldrake,Peter C. McDonnell,Sanjay Kumar,Peter R. Young,Jerry L. Adams +22 more
TL;DR: Members of three classes of pyridinylimidazoles bind with varying affinities to CSBP (p38) kinase which is a member of a stress-induced signal transduction pathway, and binding is shown to correlate with inhibition of CSBP kinase activity.
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Development of dihydropyridone indazole amides as selective Rho-kinase inhibitors.
Krista B. Goodman,Haifeng Cui,Sarah E. Dowdell,Dimitri E. Gaitanopoulos,Robert L. Ivy,Clark A. Sehon,Robert A. Stavenger,Gren Z. Wang,Andrew Q. Viet,Weiwei Xu,Guosen Ye,Simon Semus,Christopher P. Evans,Harvey E. Fries,Larry J. Jolivette,Robert B. Kirkpatrick,Edward Dul,Sanjay S. Khandekar,Tracey Yi,David Kendallc Jung,Lois L Wright,Gary K Smith,David J. Behm,Ross Bentley,Christopher P. Doe,Erding Hu,Dennis Lee +26 more
TL;DR: Indazole substitution played a critical role in decreasing clearance and improving oral bioavailability and a series of dihydropyridones were discovered, exemplified by 13, with improved pharmacokinetic parameters relative to the initial lead.
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Discovery of GSK2193874: An Orally Active, Potent,and Selective Blocker of Transient Receptor Potential Vanilloid 4
Mui Cheung,Weike Bao,David J. Behm,Carl Brooks,Michael Jonathan Bury,Sarah E. Dowdell,Eidam Hilary Schenck,Fox Ryan Michael,Krista B. Goodman,Dennis A. Holt,Dennis Lee,Theresa J. Roethke,Robert N. Willette,Xiaoping Xu,Guosen Ye,Kevin S. Thorneloe +15 more
TL;DR: The discovery of an orally active, potent, and selective TRPV4 blocker, 3-(1,4'-bipiperidin-1'-ylmethyl)-7-bromo-N-(1-phenylcyclopropyl)-2-[3-(trifluoromethyl)phenyl]-4-quinolinecarboxamide (GSK2193874, 28) after addressing an unexpected off-target cardiovascular liability observed from in vivo studies.
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Discovery of potent, selective sulfonylfuran urea endothelial lipase inhibitors.
Krista B. Goodman,Michael Jonathan Bury,Mui Cheung,Maria Cichy-Knight,Sarah E. Dowdell,Allison K. Dunn,Dennis Lee,Jeffrey A. Lieby,Michael L. Moore,Daryl A. Scherzer,Deyou Sha,Dominic Suarez,Dennis Murphy,Mark R. Harpel,Eric S. Manas,Dean E. McNulty,Roland S. Annan,Rosalie Matico,Benjamin K. Schwartz,John J. Trill,Thomas D. Sweitzer,Da-Yuan Wang,Paul M. Keller,John A. Krawiec,Michael Jaye +24 more
TL;DR: Sulfonylfuran urea 1 was identified in a high-throughput screening campaign as a potent and non-selective EL inhibitor, and modifications leading to improved LPL selectivity were identified.
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High-resolution X-ray crystallography reveals precise binding interactions between human nonpancreatic secreted phospholipase A2 and a highly potent inhibitor (FPL67047XX).
Sun Shin Cha,Dennis Lee,Jerry L. Adams,Jeffrey T. Kurdyla,Christopher S. Jones,Lisa A. Marshall,Brian Bolognese,Sherin S. Abdel-Meguid,Byung-Ha Oh +8 more
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