M
Michael Tonge
Researcher at AstraZeneca
Publications - 14
Citations - 686
Michael Tonge is an academic researcher from AstraZeneca. The author has contributed to research in topics: Estrogen receptor & Allosteric regulation. The author has an hindex of 10, co-authored 13 publications receiving 495 citations.
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Journal ArticleDOI
AZD9496: An Oral Estrogen Receptor Inhibitor That Blocks the Growth of ER-Positive and ESR1-Mutant Breast Tumors in Preclinical Models
Hazel M. Weir,Robert Hugh Bradbury,Mandy Lawson,Alfred A. Rabow,David Buttar,Rowena Callis,Jon Curwen,Camila de Almeida,Peter Ballard,Micheal Hulse,Craig S. Donald,Lyman Feron,Galith Karoutchi,Philip A. MacFaul,Thomas A. Moss,Richard A. Norman,Stuart E. Pearson,Michael Tonge,Gareth M. Davies,Graeme Walker,Zena Wilson,Rachel Rowlinson,Steve Powell,Claire Sadler,Graham Richmond,Brendon Ladd,Ermira Pazolli,Anne Marie Mazzola,Celina M. D'Cruz,Chris De Savi +29 more
TL;DR: The pharmacologic evidence showed that AZD9496 is an oral, nonsteroidal, selective estrogen receptor antagonist and downregulator in ER(+ breast cells that could provide meaningful benefit to ER(+) breast cancer patients.
Journal ArticleDOI
Optimization of a Novel Binding Motif to (E)-3-(3,5-Difluoro-4-((1R,3R)-2-(2-Fluoro-2-Methylpropyl)-3-Methyl-2, 3,4,9-Tetrahydro-1H-Pyrido[3,4-B]Indol-1-Yl)Phenyl)Acrylic Acid (Azd9496), a Potent and Orally Bioavailable Selective Estrogen Receptor Downregulator and Antagonist.
Chris De Savi,Robert Hugh Bradbury,Alfred A. Rabow,Richard A. Norman,Camila de Almeida,David M. Andrews,Peter Ballard,David Buttar,Rowena Callis,Gordon S. Currie,Jon Curwen,Christopher D. Davies,Craig S. Donald,Lyman Feron,H. Gingell,Steven C. Glossop,Barry R. Hayter,Syeed Hussain,Galith Karoutchi,Scott G. Lamont,Philip A. MacFaul,Thomas A. Moss,Stuart E. Pearson,Michael Tonge,Graeme Walker,Hazel M. Weir,Zena Wilson +26 more
TL;DR: The discovery of an orally bioavailable selective estrogen receptor downregulator (SERD) with equivalent potency and preclinical pharmacology to the intramuscular SERD fulvestrant is described.
Journal ArticleDOI
Acoustic Mist Ionization Platform for Direct and Contactless Ultrahigh-Throughput Mass Spectrometry Analysis of Liquid Samples
Ian Sinclair,Martin Bachman,Daniel H. Addison,Mattias Rohman,David Murray,Gareth M. Davies,Elizabeth Mouchet,Michael Tonge,Richard G. Stearns,Lucien P. Ghislain,Sammy S. Datwani,Lars Majlof,Eric W. Hall,Gareth Rhys Jones,Emmy Hoyes,Joe Olechno,Richard N. Ellson,Perdita E. Barran,Steven Derek Pringle,Michael Morris,Jonathan Wingfield +20 more
TL;DR: The development of an acoustic mist ionization (AMI) interface capable of contactless nanoliter-scale "infusion" of up to three individual samples per second into the mass detector is presented.
Journal ArticleDOI
Structure-Guided Design of Highly Selective and Potent Covalent Inhibitors of ERK1/2
Richard A. Ward,Nicola Colclough,Mairi Challinor,Judit E. Debreczeni,Kay Eckersley,Gary Fairley,Lyman Feron,Vikki Flemington,Mark A. Graham,Ryan Greenwood,Philip Hopcroft,Tina Howard,Michael James,Clifford David Jones,Christopher R. Jones,Jonathan Renshaw,Karen Roberts,Lindsay Snow,Michael Tonge,Kay Yeung +19 more
TL;DR: Multiple series of highly selective covalent ERK1/2 inhibitors informed by structure-based drug design (SBDD) are identified for potential in vitro and in vivo studies to assess the risks and or benefits of targeting this pathway through such a mechanism of action.
Journal ArticleDOI
Structure-Based Design and Pharmacokinetic Optimization of Covalent Allosteric Inhibitors of the Mutant GTPase KRASG12C.
Jason Grant Kettle,Sharanjeet Kaur Bagal,Sue Bickerton,Bodnarchuk,Jason Breed,Rodrigo J. Carbajo,Doyle Joseph Cassar,A. Chakraborty,Sabina Cosulich,Iain A. Cumming,Michael Davies,Andrew John Eatherton,L. Evans,Lyman Feron,Shaun M. Fillery,E.S. Gleave,Frederick W. Goldberg,S. Harlfinger,Lyndsey Hanson,M.R. Howard,Rachel L. Howells,A. Jackson,Paul D. Kemmitt,J.K. Kingston,Scott G. Lamont,Hilary J. Lewis,S. Li,L. Liu,Derek Ogg,Christopher R. Phillips,Radoslaw Polanski,Graeme R. Robb,David Robinson,Sarah Ross,James M. Smith,Michael Tonge,Rebecca Whiteley,Jun Yang,L. Zhang,X. Zhao +39 more
TL;DR: Attempts to directly drug the important oncogene KRAS have met with limited success despite numerous efforts across industry and academia, and the KRASG12C mutant represents an “Achilles heel” and has ...