S
Stuart E. Pearson
Researcher at AstraZeneca
Publications - 26
Citations - 881
Stuart E. Pearson is an academic researcher from AstraZeneca. The author has contributed to research in topics: Receptor tyrosine kinase & Nucleophile. The author has an hindex of 13, co-authored 25 publications receiving 747 citations. Previous affiliations of Stuart E. Pearson include University College London.
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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
Design and synthesis of novel lactate dehydrogenase A inhibitors by fragment-based lead generation.
Richard A. Ward,Claire Brassington,Alexander L. Breeze,Alessandro T. Caputo,Susan E. Critchlow,Gareth M. Davies,Louise Goodwin,Giles Hassall,Ryan Greenwood,Geoffrey A. Holdgate,Michael Mrosek,Richard A. Norman,Stuart E. Pearson,Jonathan Tart,Julie A. Tucker,Martin Vogtherr,David Whittaker,Jonathan Wingfield,Jon Winter,Kevin Hudson +19 more
TL;DR: Progress using fragment-based lead generation (FBLG), assisted by X-ray crystallography to develop small molecule LDHA inhibitors, which were identified through NMR and SPR screening and optimized into lead compounds with nanomolar binding affinities via fragment linking.
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
Discovery of 4-Amino-N-[(1S)-1-(4-chlorophenyl)-3-hydroxypropyl]-1-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)piperidine-4-carboxamide (AZD5363), an Orally Bioavailable, Potent Inhibitor of Akt Kinases.
Matt Addie,Peter Ballard,David Buttar,Claire Crafter,Gordon S. Currie,Barry R. Davies,Judit E. Debreczeni,Hannah Dry,Philippa Dudley,Ryan Greenwood,Johnson Paul David,Jason Grant Kettle,Clare Lane,Gillian M. Lamont,Andrew G. Leach,Richard W. A. Luke,Morris Jeffrey James,Donald J. Ogilvie,Ken Page,Martin Pass,Stuart E. Pearson,Linette Ruston +21 more
TL;DR: This compound demonstrated good preclinical drug metabolism and pharmacokinetics (DMPK) properties and, after oral dosing, showed pharmacodynamic knockdown of phosphorylation of Akt and downstream biomarkers in vivo, and inhibition of tumor growth in a breast cancer xenograft model.
Journal ArticleDOI
Inhibitors of epidermal growth factor receptor tyrosine kinase: optimisation of potency and in vivo pharmacokinetics.
Peter Ballard,Robert Hugh Bradbury,Craig S. Harris,Laurent Francois Andre Hennequin,Mark Hickinson,Jason Grant Kettle,Jane Kendrew,Teresa Klinowska,Donald J. Ogilvie,Stuart E. Pearson,Emma J. Williams,Ingrid Wilson +11 more
TL;DR: The structure-activity and structure-property relationships of anilinoquinazoline inhibitors of EGFR were investigated and strategies to lower volume of distribution and shorten half-life through structure and pKa modulation are discussed.