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Page 1
Structure- and Property-Based Optimization of Efficient Pan-Bromodomain and Extra Terminal Inhibitors to Identify Oral and Intravenous Candidate I-BET787.
Hirst DJ, Bamborough P, Al-Mahdi N, Angell DC, Barnett HA, Baxter A, Bit RA, Brown JA, Chung CW, Craggs PD, Davis RP, Demont EH, Ferrie A, Gordon LJ, Harada I, Ho TCT, Holyer ID, Hooper-Greenhill E, Jones KL, Lindon MJ, Lovatt C, Lugo D, Maller C, McGonagle G, Messenger C, Mitchell DJ, Pascoe DD, Patel VK, Patten C, Poole DL, Shah RR, Rioja I, Stafford KAJ, Tape D, Taylor S, Theodoulou NH, Tomlinson L, Wall ID, Wellaway CR, White G, Prinjha RK, Humphreys PG. Hirst DJ, et al. J Med Chem. 2024 Jun 27;67(12):10464-10489. doi: 10.1021/acs.jmedchem.4c00959. Epub 2024 Jun 12. J Med Chem. 2024. PMID: 38866424
In skeletal muscle and neural crest cells, SMCHD1 regulates biological pathways relevant for Bosma syndrome and facioscapulohumeral dystrophy phenotype.
Laberthonnière C, Delourme M, Chevalier R, Dion C, Ganne B, Hirst D, Caron L, Perrin P, Adélaïde J, Chaffanet M, Xue S, Nguyen K, Reversade B, Déjardin J, Baudot A, Robin JD, Magdinier F. Laberthonnière C, et al. Among authors: hirst d. Nucleic Acids Res. 2023 Aug 11;51(14):7269-7287. doi: 10.1093/nar/gkad523. Nucleic Acids Res. 2023. PMID: 37334829 Free PMC article.
Identification and Optimization of a Ligand-Efficient Benzoazepinone Bromodomain and Extra Terminal (BET) Family Acetyl-Lysine Mimetic into the Oral Candidate Quality Molecule I-BET432.
Humphreys PG, Anderson NA, Bamborough P, Baxter A, Chung CW, Cookson R, Craggs PD, Dalton T, Fournier JCL, Gordon LJ, Gray HF, Gray MW, Gregory R, Hirst DJ, Jamieson C, Jones KL, Kessedjian H, Lugo D, McGonagle G, Patel VK, Patten C, Poole DL, Prinjha RK, Ramirez-Molina C, Rioja I, Seal G, Stafford KAJ, Shah RR, Tape D, Theodoulou NH, Tomlinson L, Ukuser S, Wall ID, Wellaway N, White G. Humphreys PG, et al. Among authors: hirst dj. J Med Chem. 2022 Nov 24;65(22):15174-15207. doi: 10.1021/acs.jmedchem.2c01102. Epub 2022 Nov 15. J Med Chem. 2022. PMID: 36378954
Public Health Actions to Control Measles Among Afghan Evacuees During Operation Allies Welcome - United States, September-November 2021.
Masters NB, Mathis AD, Leung J, Raines K, Clemmons NS, Miele K, Balajee SA, Lanzieri TM, Marin M, Christensen DL, Clarke KR, Cruz MA, Gallagher K, Gearhart S, Gertz AM, Grady-Erickson O, Habrun CA, Kim G, Kinzer MH, Miko S, Oberste MS, Petras JK, Pieracci EG, Pray IW, Rosenblum HG, Ross JM, Rothney EE, Segaloff HE, Shepersky LV, Skrobarcek KA, Stadelman AM, Sumner KM, Waltenburg MA, Weinberg M, Worrell MC, Bessette NE, Peake LR, Vogt MP, Robinson M, Westergaard RP, Griesser RH, Icenogle JP, Crooke SN, Bankamp B, Stanley SE, Friedrichs PA, Fletcher LD, Zapata IA, Wolfe HO, Gandhi PH, Charles JY, Brown CM, Cetron MS, Pesik N, Knight NW, Alvarado-Ramy F, Bell M, Talley LE, Rotz LD, Rota PA, Sugerman DE, Gastañaduy PA; Operation Allies Welcome Response Group. Masters NB, et al. MMWR Morb Mortal Wkly Rep. 2022 Apr 29;71(17):592-596. doi: 10.15585/mmwr.mm7117a2. MMWR Morb Mortal Wkly Rep. 2022. PMID: 35482557 Free PMC article.
Design, Synthesis, and Characterization of I-BET567, a Pan-Bromodomain and Extra Terminal (BET) Bromodomain Oral Candidate.
Humphreys PG, Atkinson SJ, Bamborough P, Bit RA, Chung CW, Craggs PD, Cutler L, Davis R, Ferrie A, Gong G, Gordon LJ, Gray M, Harrison LA, Hayhow TG, Haynes A, Henley N, Hirst DJ, Holyer ID, Lindon MJ, Lovatt C, Lugo D, McCleary S, Molnar J, Osmani Q, Patten C, Preston A, Rioja I, Seal JT, Smithers N, Sun F, Tang D, Taylor S, Theodoulou NH, Thomas C, Watson RJ, Wellaway CR, Zhu L, Tomkinson NCO, Prinjha RK. Humphreys PG, et al. Among authors: hirst dj. J Med Chem. 2022 Feb 10;65(3):2262-2287. doi: 10.1021/acs.jmedchem.1c01747. Epub 2022 Jan 7. J Med Chem. 2022. PMID: 34995458 Free article.
GSK137, a potent small-molecule BCL6 inhibitor with in vivo activity, suppresses antibody responses in mice.
Pearce AC, Bamford MJ, Barber R, Bridges A, Convery MA, Demetriou C, Evans S, Gobbetti T, Hirst DJ, Holmes DS, Hutchinson JP, Jayne S, Lezina L, McCabe MT, Messenger C, Morley J, Musso MC, Scott-Stevens P, Manso AS, Schofield J, Slocombe T, Somers D, Walker AL, Wyce A, Zhang XP, Wagner SD. Pearce AC, et al. Among authors: hirst dj. J Biol Chem. 2021 Aug;297(2):100928. doi: 10.1016/j.jbc.2021.100928. Epub 2021 Jul 15. J Biol Chem. 2021. PMID: 34274316 Free PMC article.
A practical catalytic reductive amination of carboxylic acids.
Stoll EL, Tongue T, Andrews KG, Valette D, Hirst DJ, Denton RM. Stoll EL, et al. Among authors: hirst dj. Chem Sci. 2020 Aug 12;11(35):9494-9500. doi: 10.1039/d0sc02271c. Chem Sci. 2020. PMID: 34123174 Free PMC article.
A Turing Test for Molecular Generators.
Bush JT, Pogany P, Pickett SD, Barker M, Baxter A, Campos S, Cooper AWJ, Hirst D, Inglis G, Nadin A, Patel VK, Poole D, Pritchard J, Washio Y, White G, Green DVS. Bush JT, et al. Among authors: hirst d. J Med Chem. 2020 Oct 22;63(20):11964-11971. doi: 10.1021/acs.jmedchem.0c01148. Epub 2020 Oct 12. J Med Chem. 2020. PMID: 32955254
239 results