A
Ami S. Lakdawala
Researcher at GlaxoSmithKline
Publications - 18
Citations - 1409
Ami S. Lakdawala is an academic researcher from GlaxoSmithKline. The author has contributed to research in topics: Tubulin & Druggability. The author has an hindex of 13, co-authored 18 publications receiving 1150 citations. Previous affiliations of Ami S. Lakdawala include Binghamton University.
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Journal ArticleDOI
RIP3 induces apoptosis independent of pronecrotic kinase activity.
Pratyusha Mandal,Scott B. Berger,Sirika Pillay,Kenta Moriwaki,Chunzi Huang,Hongyan Guo,John D. Lich,Joshua N. Finger,Viera Kasparcova,Bart Votta,Michael T. Ouellette,Bryan W. King,David D. Wisnoski,Ami S. Lakdawala,Demartino Michael P,Linda N. Casillas,Pamela A. Haile,Clark A. Sehon,Robert W. Marquis,Jason W. Upton,Lisa P. Daley-Bauer,Linda Roback,Nancy F. Ramia,Cole M. Dovey,Jan E. Carette,Francis Ka-Ming Chan,John Bertin,Peter J. Gough,Edward S. Mocarski,William J. Kaiser +29 more
TL;DR: This work highlights a common mechanism unveiling RHIM-driven apoptosis by therapeutic or genetic perturbation of RIP3, which holds both necroptosis and apoptosis in balance through a Ripoptosome-like platform.
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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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Druggability Assessment of Allosteric Proteins by Dynamics Simulations in the Presence of Probe Molecules.
TL;DR: A new methodology that successfully predicts the druggability and maximal binding affinity for a series of challenging targets, including those that function through allosteric mechanisms, and provides insights into novel druggable sites and the target’s structural changes that would accommodate, if not promote and stabilize, drug binding.
Journal ArticleDOI
The bioactive Taxol conformation on β-tubulin: Experimental evidence from highly active constrained analogs
Thota Ganesh,Rebecca C. Guza,Susan Bane,Rudravajhala Ravindra,Natasha Shanker,Ami S. Lakdawala,James P. Snyder,David G. I. Kingston +7 more
TL;DR: Experimental and theoretical evidence that Taxol adopts a T-shaped conformation when it is bound to tubulin is presented.
Journal ArticleDOI
The Identification and Pharmacological Characterization of 6-(tert-Butylsulfonyl)-N-(5-fluoro-1H-indazol-3-yl)quinolin-4-amine (GSK583), a Highly Potent and Selective Inhibitor of RIP2 Kinase
Pamela A. Haile,Bartholomew J. Votta,Robert W. Marquis,Michael Jonathan Bury,John F. Mehlmann,Robert Singhaus,Adam Kenneth Charnley,Ami S. Lakdawala,Máire A. Convery,David B. Lipshutz,Biva M. Desai,Barbara A. Swift,Carol A. Capriotti,Scott B. Berger,Mukesh K. Mahajan,Michael Reilly,Elizabeth J. Rivera,Helen H. Sun,Rakesh Nagilla,Allison M. Beal,Joshua N. Finger,Michael Cook,Bryan W. King,Michael T. Ouellette,Rachel D. Totoritis,Maria Pierdomenico,Anna Negroni,Laura Stronati,Salvatore Cucchiara,Bartłomiej Ziółkowski,Anna Vossenkämper,Thomas T. MacDonald,Peter J. Gough,John Bertin,Linda N. Casillas +34 more
TL;DR: The discovery and pharmacological characterization of GSK583, a next-generation RIP2 inhibitor possessing exquisite selectivity and potency is presented, further clarifying the understanding of the role of RIP2 in NOD1 and NOD2 mediated disease pathogenesis.