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Zap-Pano: a Photocaged Prodrug of the KDAC Inhibitor Panobinostat.
Troelsen KS, Calder EDD, Skwarska A, Sneddon D, Hammond EM, Conway SJ. Troelsen KS, et al. ChemMedChem. 2021 Dec 14;16(24):3691-3700. doi: 10.1002/cmdc.202100403. Epub 2021 Jul 29. ChemMedChem. 2021. PMID: 34259396 Free PMC article.
Controlling Intramolecular Interactions in the Design of Selective, High-Affinity Ligands for the CREBBP Bromodomain.
Brand M, Clayton J, Moroglu M, Schiedel M, Picaud S, Bluck JP, Skwarska A, Bolland H, Chan AKN, Laurin CMC, Scorah AR, See L, Rooney TPC, Andrews KH, Fedorov O, Perell G, Kalra P, Vinh KB, Cortopassi WA, Heitel P, Christensen KE, Cooper RI, Paton RS, Pomerantz WCK, Biggin PC, Hammond EM, Filippakopoulos P, Conway SJ. Brand M, et al. J Med Chem. 2021 Jul 22;64(14):10102-10123. doi: 10.1021/acs.jmedchem.1c00348. Epub 2021 Jul 13. J Med Chem. 2021. PMID: 34255515 Free PMC article.
Development and pre-clinical testing of a novel hypoxia-activated KDAC inhibitor.
Skwarska A, Calder EDD, Sneddon D, Bolland H, Odyniec ML, Mistry IN, Martin J, Folkes LK, Conway SJ, Hammond EM. Skwarska A, et al. Cell Chem Biol. 2021 Sep 16;28(9):1258-1270.e13. doi: 10.1016/j.chembiol.2021.04.004. Epub 2021 Apr 27. Cell Chem Biol. 2021. PMID: 33910023 Free PMC article.
Bifunctional Molecules beyond PROTACs.
Conway SJ. Conway SJ. J Med Chem. 2020 Mar 26;63(6):2802-2806. doi: 10.1021/acs.jmedchem.0c00293. Epub 2020 Mar 11. J Med Chem. 2020. PMID: 32157887
BET bromodomain ligands: Probing the WPF shelf to improve BRD4 bromodomain affinity and metabolic stability.
Jennings LE, Schiedel M, Hewings DS, Picaud S, Laurin CMC, Bruno PA, Bluck JP, Scorah AR, See L, Reynolds JK, Moroglu M, Mistry IN, Hicks A, Guzanov P, Clayton J, Evans CNG, Stazi G, Biggin PC, Mapp AK, Hammond EM, Humphreys PG, Filippakopoulos P, Conway SJ. Jennings LE, et al. Bioorg Med Chem. 2018 Jul 15;26(11):2937-2957. doi: 10.1016/j.bmc.2018.05.003. Epub 2018 May 15. Bioorg Med Chem. 2018. PMID: 29776834 Free article.