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A covalent fragment-based strategy targeting a novel cysteine to inhibit activity of mutant EGFR kinase.
Kuki N, Walmsley DL, Kanai K, Takechi S, Yoshida M, Murakami R, Takano K, Tominaga Y, Takahashi M, Ito S, Nakao N, Angove H, Baker LM, Carter E, Dokurno P, Le Strat L, Macias AT, Molyneaux CA, Murray JB, Surgenor AE, Hamada T, Hubbard RE. Kuki N, et al. Among authors: walmsley dl. RSC Med Chem. 2023 Oct 19;14(12):2731-2737. doi: 10.1039/d3md00439b. eCollection 2023 Dec 13. RSC Med Chem. 2023. PMID: 38107172
Fragment-Based Discovery of Novel Non-Hydroxamate LpxC Inhibitors with Antibacterial Activity.
Yamada Y, Takashima H, Walmsley DL, Ushiyama F, Matsuda Y, Kanazawa H, Yamaguchi-Sasaki T, Tanaka-Yamamoto N, Yamagishi J, Kurimoto-Tsuruta R, Ogata Y, Ohtake N, Angove H, Baker L, Harris R, Macias A, Robertson A, Surgenor A, Watanabe H, Nakano K, Mima M, Iwamoto K, Okada A, Takata I, Hitaka K, Tanaka A, Fujita K, Sugiyama H, Hubbard RE. Yamada Y, et al. Among authors: walmsley dl. J Med Chem. 2020 Dec 10;63(23):14805-14820. doi: 10.1021/acs.jmedchem.0c01215. Epub 2020 Nov 19. J Med Chem. 2020. PMID: 33210531
Structure-Guided Discovery of Potent and Selective DYRK1A Inhibitors.
Weber C, Sipos M, Paczal A, Balint B, Kun V, Foloppe N, Dokurno P, Massey AJ, Walmsley DL, Hubbard RE, Murray J, Benwell K, Edmonds T, Demarles D, Bruno A, Burbridge M, Cruzalegui F, Kotschy A. Weber C, et al. Among authors: walmsley dl. J Med Chem. 2021 May 27;64(10):6745-6764. doi: 10.1021/acs.jmedchem.1c00023. Epub 2021 May 12. J Med Chem. 2021. PMID: 33975430
4,5-diarylisoxazole Hsp90 chaperone inhibitors: potential therapeutic agents for the treatment of cancer.
Brough PA, Aherne W, Barril X, Borgognoni J, Boxall K, Cansfield JE, Cheung KM, Collins I, Davies NG, Drysdale MJ, Dymock B, Eccles SA, Finch H, Fink A, Hayes A, Howes R, Hubbard RE, James K, Jordan AM, Lockie A, Martins V, Massey A, Matthews TP, McDonald E, Northfield CJ, Pearl LH, Prodromou C, Ray S, Raynaud FI, Roughley SD, Sharp SY, Surgenor A, Walmsley DL, Webb P, Wood M, Workman P, Wright L. Brough PA, et al. Among authors: walmsley dl. J Med Chem. 2008 Jan 24;51(2):196-218. doi: 10.1021/jm701018h. Epub 2007 Nov 20. J Med Chem. 2008. PMID: 18020435
Structure-based design of peptidomimetic antagonists of p56(lck) SH2 domain.
Hobbs CJ, Bit RA, Cansfield AD, Harris B, Hill CH, Hilyard KL, Kilford IR, Kitas E, Kroehn A, Lovell P, Pole D, Rugman P, Sherborne BS, Smith IE, Vesey DR, Walmsley DL, Whittaker D, Williams G, Wilson F, Banner D, Surgenor A, Borkakoti N. Hobbs CJ, et al. Among authors: walmsley dl. Bioorg Med Chem Lett. 2002 May 20;12(10):1365-9. doi: 10.1016/s0960-894x(02)00167-1. Bioorg Med Chem Lett. 2002. PMID: 11992778