K
Kurt Gordon Pike
Researcher at AstraZeneca
Publications - 99
Citations - 2171
Kurt Gordon Pike is an academic researcher from AstraZeneca. The author has contributed to research in topics: Glucokinase & Glioma. The author has an hindex of 26, co-authored 98 publications receiving 1820 citations. Previous affiliations of Kurt Gordon Pike include University of Southampton.
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Journal ArticleDOI
Optimization of potent and selective dual mTORC1 and mTORC2 inhibitors: the discovery of AZD8055 and AZD2014
Kurt Gordon Pike,Karine Malagu,Marc Geoffrey Hummersone,Keith Allan Menear,Heather Mary Ellen Duggan,Sylvie Gomez,Niall M. B. Martin,Linette Ruston,Sarah L. Pass,Martin Pass +9 more
TL;DR: The optimization of a potent and highly selective series of dual m TORC1 and mTORC2 inhibitors is described, particularly aimed at reducing the rate of metabolism in human hepatocyte incubations, resulted in the discovery of the clinical candidate AZD2014.
Journal ArticleDOI
The brain-penetrant clinical ATM inhibitor AZD1390 radiosensitizes and improves survival of preclinical brain tumor models
Stephen T. Durant,Li Zheng,Yingchun Wang,Kan Chen,Lingli Zhang,Tianwei Zhang,Zhenfan Yang,Lucy Riches,Antonio García Trinidad,Jacqueline H. L. Fok,Thomas Anthony Hunt,Kurt Gordon Pike,Joanne Wilson,Aaron Smith,Nicola Colclough,Venkatesh Pilla Reddy,Andrew Sykes,Annika Janefeldt,Peter Johnström,Katarina Varnäs,Akihiro Takano,Stephanie Ling,Jonathan P. Orme,Jonathan Stott,Caroline Roberts,Ian P. Barrett,Gemma N Jones,Martine P. Roudier,Andrew J. Pierce,Jasmine Allen,Jenna M. Kahn,Amrita Sule,Jeremy Karlin,Anna Cronin,Melissa Chapman,Kristoffer Valerie,Ruth Illingworth,Martin Pass +37 more
TL;DR: A pharmacokinetic-pharmacodynamic-efficacy relationship is established by correlating free brain concentrations, tumor phospho-ATM/phospho-Rad50 inhibition, apoptotic biomarker induction, tumor regression, and survival.
Journal ArticleDOI
AZD2014, an inhibitor of mTORC1 and mTORC2, is highly effective in ER+ breast cancer when administered using intermittent or continuous schedules.
Sylvie Guichard,Jon Curwen,Teeru Bihani,Celina M. D'Cruz,James W.T. Yates,Michael Grondine,Zoe Howard,Barry R. Davies,Graham Bigley,Teresa Klinowska,Kurt Gordon Pike,Martin Pass,Christine M. Chresta,Urszula M. Polanska,Robert McEwen,Oona Delpuech,Stephen Green,Sabina Cosulich +17 more
TL;DR: It is demonstrated that AZD2014 has broad antiproliferative effects across multiple cell lines, including ER+ breast models with acquired resistance to hormonal therapy and cell lines with acquired Resistance to rapalogs, an ideal candidate for combining with endocrine therapies in the clinic.
Journal ArticleDOI
Pharmacology of the ATM Inhibitor AZD0156: Potentiation of Irradiation and Olaparib Responses Preclinically.
Lucy Riches,Antonio García Trinidad,Gareth Hughes,Gemma N Jones,A. Hughes,Andrew G. Thomason,Paul R. Gavine,Andy Cui,Stephanie Ling,Jonathan Stott,Roger Clark,Samantha Peel,Pendeep Gill,Louise Goodwin,Aaron Smith,Kurt Gordon Pike,Barlaam Bernard Christophe,Martin Pass,Mark J. O'Connor,Graeme C. M. Smith,Elaine Cadogan +20 more
TL;DR: It is demonstrated that AZD0156 impedes the repair of olaparib-induced DNA damage, resulting in elevated DNA double-strand break signaling, cell-cycle arrest, and apoptosis, as measured by phosphorylation of ATM substrates.
Journal ArticleDOI
Design of a potent, soluble glucokinase activator with excellent in vivo efficacy.
Darren Mckerrecher,Joanne V. Allen,Peter William Rodney Caulkett,Craig S. Donald,Mark L. Fenwick,Emma Grange,Keith M. Johnson,Craig Johnstone,Clifford David Jones,Kurt Gordon Pike,Rayner John Wall,Rolf Peter Walker +11 more
TL;DR: The use of unbound clearance as an optimisation parameter facilitated the identification of GKA50, a compound which combines excellent potency and pharmacokinetics with good free drug levels and solubility, and exhibits in vivo efficacy at 1mg/kg po in an acute rat OGTT model.