N
Nicola Colclough
Researcher at AstraZeneca
Publications - 36
Citations - 1919
Nicola Colclough is an academic researcher from AstraZeneca. The author has contributed to research in topics: Epidermal growth factor receptor & Osimertinib. The author has an hindex of 16, co-authored 34 publications receiving 1444 citations.
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Journal ArticleDOI
Discovery of a potent and selective EGFR inhibitor (AZD9291) of both sensitizing and T790M resistance mutations that spares the wild type form of the receptor
M. Raymond V. Finlay,Mark J. Anderton,Susan Ashton,Peter Ballard,Paul A. Bethel,Matthew R. Box,Robert Hugh Bradbury,Simon J. Brown,Sam Butterworth,Andrew D. Campbell,Christopher G. Chorley,Nicola Colclough,Darren Cross,Gordon S. Currie,Matthew Grist,Lorraine A. Hassall,George B. Hill,Daniel S. James,Michael James,Paul D. Kemmitt,Teresa Klinowska,Gillian M. Lamont,Scott G. Lamont,Nathaniel G. Martin,Heather L. McFarland,Martine J. Mellor,Jonathon P. Orme,David Perkins,Paula Perkins,Graham Richmond,Peter D. Smith,Richard A. Ward,Michael J. Waring,David Whittaker,Stuart L. Wells,Gail L. Wrigley +35 more
TL;DR: Following observations of significant tumor inhibition in preclinical models, the clinical candidate AZD9291 was administered clinically to patients with T790M positive EGFR-TKI resistant NSCLC and early efficacy has been observed, accompanied by an encouraging safety profile.
Journal ArticleDOI
Matched molecular pairs as a guide in the optimization of pharmaceutical properties; a study of aqueous solubility, plasma protein binding and oral exposure.
Andrew G. Leach,H. Jones,David A. Cosgrove,Peter W. Kenny,Linette Ruston,Philip A. MacFaul,J. Matthew Wood,Nicola Colclough,Brian Law +8 more
TL;DR: The effects on aqueous solubility, plasma protein binding and oral exposure of adding substituents to aromatic rings and methylating heteroatoms are focused upon.
Journal ArticleDOI
Structure- and Reactivity-Based Development of Covalent Inhibitors of the Activating and Gatekeeper Mutant Forms of the Epidermal Growth Factor Receptor (EGFR)
Richard A. Ward,Mark J. Anderton,Susan Ashton,Paul A. Bethel,Matthew R. Box,Sam Butterworth,Nicola Colclough,Christopher G. Chorley,Claudio Chuaqui,Darren Cross,Les A. Dakin,Judit E. Debreczeni,Cath Eberlein,M. Raymond V. Finlay,George B. Hill,Matthew Grist,Teresa Klinowska,Clare Lane,Scott W. Martin,Jonathon P. Orme,Peter D. Smith,Fengjiang Wang,Michael J. Waring +22 more
TL;DR: A novel series of small-molecule inhibitors developed to target the double mutant form of the epidermal growth factor receptor (EGFR) tyrosine kinase, which is resistant to treatment with gefitinib and erlotinib, demonstrates high levels of activity and shows selectivity over wild-type EGFR.
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
Expanding the Armory: Predicting and Tuning Covalent Warhead Reactivity
Richard Lonsdale,Jonathan Burgess,Nicola Colclough,Nichola L. Davies,Eva M. Lenz,Alexandra L. Orton,Richard A. Ward +6 more
TL;DR: The ability of several experimental and computational approaches to predict GSH t1/2 for a range of cysteine targeting warheads is assessed, including a novel method based on pKa and matched molecular pairs analysis has been performed against the internal compound collection, revealing structure-activity relationships between a selection of different covalent warheads.