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Richard A Ward
Richard A Ward
Verified email at astrazeneca.com
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AZD9291, an irreversible EGFR TKI, overcomes T790M-mediated resistance to EGFR inhibitors in lung cancer
DAE Cross, SE Ashton, S Ghiorghiu, C Eberlein, CA Nebhan, PJ Spitzler, ...
Cancer discovery 4 (9), 1046-1061, 2014
22212014
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
MRV Finlay, M Anderton, S Ashton, P Ballard, PA Bethel, MR Box, ...
Journal of medicinal chemistry 57 (20), 8249-8267, 2014
5832014
Structure-based design of targeted covalent inhibitors
R Lonsdale, RA Ward
Chemical Society Reviews 47 (11), 3816-3830, 2018
3222018
Characterization of VPS34-IN1, a selective inhibitor of Vps34, reveals that the phosphatidylinositol 3-phosphate-binding SGK3 protein kinase is a downstream target of class III …
R Bago, N Malik, MJ Munson, AR Prescott, P Davies, E Sommer, N Shpiro, ...
Biochemical Journal 463 (3), 413-427, 2014
3132014
Challenges and opportunities in cancer drug resistance
RA Ward, S Fawell, N Floc’h, V Flemington, D McKerrecher, PD Smith
Chemical Reviews 121 (6), 3297-3351, 2020
3122020
Structure-and reactivity-based development of covalent inhibitors of the activating and gatekeeper mutant forms of the epidermal growth factor receptor (EGFR)
RA Ward, MJ Anderton, S Ashton, PA Bethel, M Box, S Butterworth, ...
Journal of medicinal chemistry 56 (17), 7025-7048, 2013
2832013
Design and synthesis of novel lactate dehydrogenase A inhibitors by fragment-based lead generation
RA Ward, C Brassington, AL Breeze, A Caputo, S Critchlow, G Davies, ...
Journal of medicinal chemistry 55 (7), 3285-3306, 2012
1872012
Expanding the armory: predicting and tuning covalent warhead reactivity
R Lonsdale, J Burgess, N Colclough, NL Davies, EM Lenz, AL Orton, ...
Journal of Chemical Information and Modeling 57 (12), 3124-3137, 2017
1592017
Preclinical comparison of the blood–brain barrier permeability of osimertinib with other EGFR TKIs
N Colclough, K Chen, P Johnström, N Strittmatter, Y Yan, GL Wrigley, ...
Clinical Cancer Research 27 (1), 189-201, 2021
1522021
AZD9291, an irreversible EGFR TKI, overcomes T790M-mediated resistance to EGFR inhibitors in lung cancer. Cancer Discov. 2014; 4: 1046–1061. doi: 10.1158/2159-8290
DA Cross, SE Ashton, S Ghiorghiu, C Eberlein, CA Nebhan, PJ Spitzler, ...
CD-14-0337.[Europe PMC free article][Abstract][CrossRef][Google Scholar], 0
135
Comparison of the EGFR resistance mutation profiles generated by EGFR-targeted tyrosine kinase inhibitors and the impact of drug combinations
E Avizienyte, RA Ward, AP Garner
Biochemical Journal 415 (2), 197-206, 2008
1162008
Antitumor activity of osimertinib, an irreversible mutant-selective EGFR tyrosine kinase inhibitor, in NSCLC harboring EGFR exon 20 insertions
N Floc'h, MJ Martin, JW Riess, JP Orme, AD Staniszewska, L Ménard, ...
Molecular cancer therapeutics 17 (5), 885-896, 2018
1062018
Structure-guided design of highly selective and potent covalent inhibitors of ERK1/2
RA Ward, N Colclough, M Challinor, JE Debreczeni, K Eckersley, ...
Journal of medicinal chemistry 58 (11), 4790-4801, 2015
1042015
Identification and characterization of dual inhibitors of the USP25/28 deubiquitinating enzyme subfamily
JD Wrigley, G Gavory, I Simpson, M Preston, H Plant, J Bradley, ...
ACS chemical biology 12 (12), 3113-3125, 2017
832017
Insight into the therapeutic selectivity of the irreversible EGFR tyrosine kinase inhibitor osimertinib through enzyme kinetic studies
X Zhai, RA Ward, P Doig, A Argyrou
Biochemistry 59 (14), 1428-1441, 2020
622020
Alkynyl benzoxazines and dihydroquinazolines as cysteine targeting covalent warheads and their application in identification of selective irreversible kinase inhibitors
K McAulay, EA Hoyt, M Thomas, M Schimpl, MS Bodnarchuk, HJ Lewis, ...
Journal of the American Chemical Society 142 (23), 10358-10372, 2020
602020
Discovery of a potent and selective oral inhibitor of ERK1/2 (AZD0364) that is efficacious in both monotherapy and combination therapy in models of nonsmall cell lung cancer …
RA Ward, MJ Anderton, P Bethel, J Breed, C Cook, EJ Davies, A Dobson, ...
Journal of medicinal chemistry 62 (24), 11004-11018, 2019
592019
Structure-guided discovery of potent and selective inhibitors of ERK1/2 from a modestly active and promiscuous chemical start point
RA Ward, P Bethel, C Cook, E Davies, JE Debreczeni, G Fairley, L Feron, ...
Journal of medicinal chemistry 60 (8), 3438-3450, 2017
572017
The structure-guided discovery of osimertinib: the first US FDA approved mutant selective inhibitor of EGFR T790M
S Butterworth, DAE Cross, MRV Finlay, RA Ward, MJ Waring
Medchemcomm 8 (5), 820-822, 2017
482017
Systematic enumeration of heteroaromatic ring systems as reagents for use in medicinal chemistry
RA Ward, JG Kettle
Journal of medicinal chemistry 54 (13), 4670-4677, 2011
482011
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