L. Evans
AstraZeneca
7 Papers
9 Citations
L. Evans is an academic researcher from AstraZeneca. The author has contributed to research in topics: Chemistry & Medicine. The author has an hindex of 2, co-authored 4 publications.
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Papers
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 ...
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Discovery of AZD4625, a Covalent Allosteric Inhibitor of the Mutant GTPase KRASG12C.
Jason Grant Kettle,Sharan K. Bagal,Susan J. Bickerton,Michael S. Bodnarchuk,Scott Boyd,Jason Breed,Rodrigo J. Carbajo,Doyle Joseph Cassar,Atanu Chakraborty,Sabina Cosulich,Iain Cumming,Michael Davies,Nichola L. Davies,Andrew John Eatherton,L. Evans,Lyman Feron,Shaun M. Fillery,Emma S Gleave,Frederick W. Goldberg,Lyndsey Hanson,Stephanie Harlfinger,M.R. Howard,Rachel L. Howells,Anne U. Jackson,Paul D. Kemmitt,Gillian M. Lamont,Scott G. Lamont,Hilary J. Lewis,Libin Liu,Michael J. Niedbala,Christopher R. Phillips,R. Polanski,Piotr Raubo,Graeme R. Robb,David A. Robinson,Sarah Ross,Matthew Sanders,Michael Tonge,Rebecca Whiteley,Stephen D. Wilkinson,Junsheng Yang,Wenman Zhang +41 more
TL;DR: A structure-based drug design approach that led to the identification of 21, AZD4625, a clinical development candidate for the treatment of KRASG12C positive tumors, with an anticipated low clearance and high oral bioavailability profile in humans.
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Fragment-Based Design of a Potent MAT2a Inhibitor and in Vivo Evaluation in an MTAP Null Xenograft Model.
Claudia De Fusco,Marianne Schimpl,Ulf Börjesson,Tony Cheung,I. Collie,L. Evans,Priyanka Narasimhan,Christopher D. Stubbs,Mercedes Vazquez-Chantada,David J. Wagner,Michael Grondine,Matthew G Sanders,Sharon Tentarelli,Elizabeth Underwood,Argyrides Argyrou,James M. Smith,James T. Lynch,Elisabetta Chiarparin,Graeme R. Robb,S. Bagal,James S. Scott +20 more
TL;DR: In this paper, a fragment-based lead generation campaign identified weak but efficient hits binding in a known allosteric site and elaborated the hits through a merging and growing strategy into an arylquinazolinone series of potent MAT2a inhibitors.
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Potent and Selective Inhibitors of the Epidermal Growth Factor Receptor to Overcome C797S-Mediated Resistance.
M. Raymond V. Finlay,Peter Barton,Sue Bickerton,Michal Bista,Nicola Colclough,Darren Cross,L. Evans,Nicolas Floc'h,Clare Gregson,Carine M. Guérot,David J. Hargreaves,Xiaoming Kang,Eva M. Lenz,Xu Li,Yi Liu,Olivier Lorthioir,Matthew J. Martin,Darren Mckerrecher,Claire McWhirter,Daniel O'Neill,Jonathan P. Orme,Arash Mosallanejad,Amar Rahi,Paul D. Smith,Verity Talbot,Richard A. Ward,Gail L. Wrigley,Marta Wylot,Lin Xue,Tieguang Yao,Yang Ye,Xiliang Zhao +31 more
TL;DR: In this article, the authors describe the medicinal chemistry optimization of a biochemically potent but modestly cell-active, reversible EGFR inhibitor starting point with sub-optimal physicochemical properties.
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A patent review of MAT2a inhibitors (2018–2021)
TL;DR: This review covers patent applications between January 2018 and December 2021 that led to MAT2a inhibitors to phase I clinical studies to explore their benefit to patients suffering with MTAP-deficient solid tumors or lymphoma.
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