Lauren Dare
GlaxoSmithKline
11 Papers
17 Citations
Lauren Dare is an academic researcher from GlaxoSmithKline. The author has contributed to research in topics: Necroptosis & Bone remodeling. The author has an hindex of 10, co-authored 11 publications.
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Papers
Discovery of a First-in-Class Receptor Interacting Protein 1 (RIP1) Kinase Specific Clinical Candidate (GSK2982772) for the Treatment of Inflammatory Diseases
Philip A. Harris,Scott B. Berger,Jae U. Jeong,Rakesh Nagilla,Deepak Bandyopadhyay,Nino Campobasso,Carol A. Capriotti,Julie A. Cox,Lauren Dare,Xiaoyang Dong,Patrick M. Eidam,Joshua N. Finger,Sandra J. Hoffman,James Kang,Viera Kasparcova,Bryan W. King,Ruth Lehr,Yunfeng Lan,Lara Kathryn Leister,John D. Lich,Thomas T. MacDonald,Nathan A. Miller,Michael T. Ouellette,Christina S. Pao,Attiq Rahman,Michael Reilly,Alan R. Rendina,Elizabeth J. Rivera,Michelle C. Schaeffer,Clark A. Sehon,Robert Singhaus,Helen H. Sun,Barbara A. Swift,Rachel D. Totoritis,Anna Vossenkämper,Paris Ward,David D. Wisnoski,Daohua Zhang,Robert W. Marquis,Peter J. Gough,John Bertin +40 more
TL;DR: Lead optimization of a benzoxazepinone hit from a DNA-encoded library and the discovery and profile of clinical candidate GSK2982772 (compound 5), currently in phase 2a clinical studies for psoriasis, rheumatoid arthritis, and ulcerative colitis, highlight its potential as a novel anti-inflammatory agent.
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Cutting Edge: RIP1 Kinase Activity Is Dispensable for Normal Development but Is a Key Regulator of Inflammation in SHARPIN-Deficient Mice
Scott B. Berger,Viera Kasparcova,Sandy Hoffman,Barb Swift,Lauren Dare,Michelle C. Schaeffer,Carol A. Capriotti,Michael Cook,Joshua N. Finger,Angela Hughes-Earle,Philip A. Harris,William J. Kaiser,Edward S. Mocarski,John Bertin,Peter J. Gough +14 more
TL;DR: The generated RIP1 kinase-dead mice are viable and healthy, indicating that the kinase activity of RIP1, but not its scaffolding function, is dispensable for viability and homeostasis, and suggest that RIP 1 kinase represents an attractive therapeutic target for TNF-driven inflammatory diseases.
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Autolytic Proteolysis within the Function to Find Domain (FIIND) Is Required for NLRP1 Inflammasome Activity
Joshua N. Finger,John D. Lich,Lauren Dare,Michael Cook,Kristin K. Brown,Chaya Duraiswami,John Bertin,Peter J. Gough +7 more
TL;DR: The requirements for activation of NLRP1, an NLR protein associated with a number of human pathologies, are identified and the results describe key molecular pathways that regulateNLRP1 activity offer insight on how small sequence variations in NLR genes may influence human disease pathogenesis.
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DNA-Encoded Library Screening Identifies Benzo[b][1,4]oxazepin-4-ones as Highly Potent and Monoselective Receptor Interacting Protein 1 Kinase Inhibitors.
Philip A. Harris,Bryan W. King,Deepak Bandyopadhyay,Scott B. Berger,Nino Campobasso,Carol A. Capriotti,Julie A. Cox,Lauren Dare,Xiaoyang Dong,Joshua N. Finger,LaShadric C. Grady,Sandra J. Hoffman,Jae U. Jeong,James Kang,Viera Kasparcova,Ami S. Lakdawala,Ruth Lehr,Dean E. McNulty,Rakesh Nagilla,Michael T. Ouellette,Christina S. Pao,Alan R. Rendina,Michelle C. Schaeffer,Jennifer Summerfield,Barbara A. Swift,Rachel D. Totoritis,Paris Ward,Aming Zhang,Daohua Zhang,Robert W. Marquis,John Bertin,Peter J. Gough +31 more
TL;DR: This work elucidate the conformation of RIP1 bound to this benzoxazepinone inhibitor driving its high kinase selectivity and design specific mutations in murine RIP1 to restore potency to levels similar to primate RIP1.
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Potent and selective inhibition of human cathepsin K leads to inhibition of bone resorption in vivo in a nonhuman primate.
George B. Stroup,Michael W. Lark,Daniel F. Veber,Amit Bhattacharyya,Simon M. Blake,Lauren Dare,Karl F. Erhard,Sandra J. Hoffman,Ian E. James,Robert W. Marquis,Ru Yu,Janice A. Vasko-Moser,Brian R. Smith,Thadeus Tomaszek,Maxine Gowen +14 more
TL;DR: Results suggests that inhibition of the human enzyme may provide protection from bone loss in states of elevated bone turnover, such as postmenopausal osteoporosis, and produces a small molecule inhibitor of cathepsin K that potently and selectively inhibits this enzyme.
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