J
Joelle Lorraine Burgess
Researcher at GlaxoSmithKline
Publications - 33
Citations - 1846
Joelle Lorraine Burgess is an academic researcher from GlaxoSmithKline. The author has contributed to research in topics: Pharmacophore & Transplantation. The author has an hindex of 15, co-authored 32 publications receiving 1702 citations.
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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
Identification of novel inhibitors of the transforming growth factor beta1 (TGF-beta1) type 1 receptor (ALK5).
James F. Callahan,Joelle Lorraine Burgess,James A. Fornwald,Laramie Mary Gaster,John D. Harling,Harrington Frank Peter,Jag Paul Heer,Chet Kwon,Ruth Lehr,A. Mathur,Barbara A. Olson,Joseph Weinstock,Nicholas J. Laping +12 more
TL;DR: Optimization of the triarylimidazole hit 8 gave the selective inhibitor 14, which inhibits TGF-beta1-induced fibronectin mRNA formation while displaying no measurable cytotoxicity in the 48 h XTT assay.
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
Direct design of a potent non-peptide fibrinogen receptor antagonist based on the structure and conformation of a highly constrained cyclic RGD peptide
Thomas W. Ku,Fadia E. Ali,Linda S. Barton,John W. Bean,William E. Bondinell,Joelle Lorraine Burgess,James F. Callahan,Raul R. Calvo,Lichong Chen +8 more