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Discovery of AZD4747, a Potent and Selective Inhibitor of Mutant GTPase KRASG12C with Demonstrable CNS Penetration.
J Med Chem. 2023 Jul 13;66(13):9147-9160. doi: 10.1021/acs.jmedchem.3c00746. Epub 2023 Jul 3.
J Med Chem. 2023.
PMID: 37395055
Structure-Based Design and Pharmacokinetic Optimization of Covalent Allosteric Inhibitors of the Mutant GTPase KRASG12C.
Kettle JG, Bagal SK, Bickerton S, Bodnarchuk MS, Breed J, Carbajo RJ, Cassar DJ, Chakraborty A, Cosulich S, Cumming I, Davies M, Eatherton A, Evans L, Feron L, Fillery S, Gleave ES, Goldberg FW, Harlfinger S, Hanson L, Howard M, Howells R, Jackson A, Kemmitt P, Kingston JK, Lamont S, Lewis HJ, Li S, Liu L, Ogg D, Phillips C, Polanski R, Robb G, Robinson D, Ross S, Smith JM, Tonge M, Whiteley R, Yang J, Zhang L, Zhao X.
Kettle JG, et al. Among authors: gleave es.
J Med Chem. 2020 May 14;63(9):4468-4483. doi: 10.1021/acs.jmedchem.9b01720. Epub 2020 Feb 13.
J Med Chem. 2020.
PMID: 32023060
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Discovery of AZD4625, a Covalent Allosteric Inhibitor of the Mutant GTPase KRASG12C.
Kettle JG, Bagal SK, Bickerton S, Bodnarchuk MS, Boyd S, Breed J, Carbajo RJ, Cassar DJ, Chakraborty A, Cosulich S, Cumming I, Davies M, Davies NL, Eatherton A, Evans L, Feron L, Fillery S, Gleave ES, Goldberg FW, Hanson L, Harlfinger S, Howard M, Howells R, Jackson A, Kemmitt P, Lamont G, Lamont S, Lewis HJ, Liu L, Niedbala MJ, Phillips C, Polanski R, Raubo P, Robb G, Robinson DM, Ross S, Sanders MG, Tonge M, Whiteley R, Wilkinson S, Yang J, Zhang W.
Kettle JG, et al. Among authors: gleave es.
J Med Chem. 2022 May 12;65(9):6940-6952. doi: 10.1021/acs.jmedchem.2c00369. Epub 2022 Apr 26.
J Med Chem. 2022.
PMID: 35471939
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Cryo-EM structure determination of small therapeutic protein targets at 3 Å-resolution using a rigid imaging scaffold.
Castells-Graells R, Meador K, Arbing MA, Sawaya MR, Gee M, Cascio D, Gleave E, Debreczeni JÉ, Breed J, Leopold K, Patel A, Jahagirdar D, Lyons B, Subramaniam S, Phillips C, Yeates TO.
Castells-Graells R, et al.
Proc Natl Acad Sci U S A. 2023 Sep 12;120(37):e2305494120. doi: 10.1073/pnas.2305494120. Epub 2023 Sep 5.
Proc Natl Acad Sci U S A. 2023.
PMID: 37669364
Free PMC article.
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Single-molecule studies contrast ordered DNA replication with stochastic translesion synthesis.
Zhao G, Gleave ES, Lamers MH.
Zhao G, et al. Among authors: gleave es.
Elife. 2017 Dec 6;6:e32177. doi: 10.7554/eLife.32177.
Elife. 2017.
PMID: 29210356
Free PMC article.
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A structural analysis of the AAA+ domains in Saccharomyces cerevisiae cytoplasmic dynein.
Gleave ES, Schmidt H, Carter AP.
Gleave ES, et al.
J Struct Biol. 2014 Jun;186(3):367-75. doi: 10.1016/j.jsb.2014.03.019. Epub 2014 Mar 28.
J Struct Biol. 2014.
PMID: 24680784
Free PMC article.
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Insights into dynein motor domain function from a 3.3-Å crystal structure.
Schmidt H, Gleave ES, Carter AP.
Schmidt H, et al. Among authors: gleave es.
Nat Struct Mol Biol. 2012 Mar 14;19(5):492-7, S1. doi: 10.1038/nsmb.2272.
Nat Struct Mol Biol. 2012.
PMID: 22426545
Free PMC article.
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