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Application of Off-Rate Screening in the Identification of Novel Pan-Isoform Inhibitors of Pyruvate Dehydrogenase Kinase.
Brough PA, Baker L, Bedford S, Brown K, Chavda S, Chell V, D'Alessandro J, Davies NG, Davis B, Le Strat L, Macias AT, Maddox D, Mahon PC, Massey AJ, Matassova N, McKenna S, Meissner JW, Moore JD, Murray JB, Northfield CJ, Parry C, Parsons R, Roughley SD, Shaw T, Simmonite H, Stokes S, Surgenor A, Stefaniak E, Robertson A, Wang Y, Webb P, Whitehead N, Wood M. Brough PA, et al. Among authors: le strat l. J Med Chem. 2017 Mar 23;60(6):2271-2286. doi: 10.1021/acs.jmedchem.6b01478. Epub 2017 Feb 15. J Med Chem. 2017. PMID: 28199108
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: le strat l. RSC Med Chem. 2023 Oct 19;14(12):2731-2737. doi: 10.1039/d3md00439b. eCollection 2023 Dec 13. RSC Med Chem. 2023. PMID: 38107172
Discovery and optimization of potent and selective functional antagonists of the human adenosine A2B receptor.
Bedford ST, Benwell KR, Brooks T, Chen I, Comer M, Dugdale S, Haymes T, Jordan AM, Kennett GA, Knight AR, Klenke B, LeStrat L, Merrett A, Misra A, Lightowler S, Padfield A, Poullennec K, Reece M, Simmonite H, Wong M, Yule IA. Bedford ST, et al. Bioorg Med Chem Lett. 2009 Oct 15;19(20):5945-9. doi: 10.1016/j.bmcl.2009.08.040. Epub 2009 Aug 14. Bioorg Med Chem Lett. 2009. PMID: 19733067