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Discovering cell-active BCL6 inhibitors: effectively combining biochemical HTS with multiple biophysical techniques, X-ray crystallography and cell-based assays.
Pierrat OA, Liu M, Collie GW, Shetty K, Rodrigues MJ, Le Bihan YV, Gunnell EA, McAndrew PC, Stubbs M, Rowlands MG, Yahya N, Shehu E, Talbot R, Pickard L, Bellenie BR, Cheung KJ, Drouin L, Innocenti P, Woodward H, Davis OA, Lloyd MG, Varela A, Huckvale R, Broccatelli F, Carter M, Galiwango D, Hayes A, Raynaud FI, Bryant C, Whittaker S, Rossanese OW, Hoelder S, Burke R, van Montfort RLM. Pierrat OA, et al. Among authors: rowlands mg. Sci Rep. 2022 Nov 3;12(1):18633. doi: 10.1038/s41598-022-23264-z. Sci Rep. 2022. PMID: 36329085 Free PMC article.
Discovery of 2-(3-Benzamidopropanamido)thiazole-5-carboxylate Inhibitors of the Kinesin HSET (KIFC1) and the Development of Cellular Target Engagement Probes.
Saint-Dizier F, Matthews TP, Gregson AM, Prevet H, McHardy T, Colombano G, Saville H, Rowlands M, Ewens C, McAndrew PC, Tomlin K, Guillotin D, Mak GW, Drosopoulos K, Poursaitidis I, Burke R, van Montfort R, Linardopoulos S, Collins I. Saint-Dizier F, et al. J Med Chem. 2023 Feb 23;66(4):2622-2645. doi: 10.1021/acs.jmedchem.2c01591. Epub 2023 Feb 7. J Med Chem. 2023. PMID: 36749938 Free PMC article.
A fragment-based approach applied to a highly flexible target: Insights and challenges towards the inhibition of HSP70 isoforms.
Jones AM, Westwood IM, Osborne JD, Matthews TP, Cheeseman MD, Rowlands MG, Jeganathan F, Burke R, Lee D, Kadi N, Liu M, Richards M, McAndrew C, Yahya N, Dobson SE, Jones K, Workman P, Collins I, van Montfort RL. Jones AM, et al. Among authors: rowlands mg. Sci Rep. 2016 Oct 6;6:34701. doi: 10.1038/srep34701. Sci Rep. 2016. PMID: 27708405 Free PMC article.
Design and synthesis of novel pyrimidine hydroxamic acid inhibitors of histone deacetylases.
Donald AD, Clark VL, Patel S, Day FA, Rowlands MG, Wibata J, Stimson L, Hardcastle A, Eccles SA, McNamara D, Needham LA, Raynaud FI, Aherne W, Moffat DF. Donald AD, et al. Among authors: rowlands mg. Bioorg Med Chem Lett. 2010 Nov 15;20(22):6657-60. doi: 10.1016/j.bmcl.2010.09.016. Epub 2010 Sep 21. Bioorg Med Chem Lett. 2010. PMID: 20884208
72 results