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Page 1
Discovery of a Bromodomain and Extraterminal Inhibitor with a Low Predicted Human Dose through Synergistic Use of Encoded Library Technology and Fragment Screening.
Wellaway CR, Amans D, Bamborough P, Barnett H, Bit RA, Brown JA, Carlson NR, Chung CW, Cooper AWJ, Craggs PD, Davis RP, Dean TW, Evans JP, Gordon L, Harada IL, Hirst DJ, Humphreys PG, Jones KL, Lewis AJ, Lindon MJ, Lugo D, Mahmood M, McCleary S, Medeiros P, Mitchell DJ, O'Sullivan M, Le Gall A, Patel VK, Patten C, Poole DL, Shah RR, Smith JE, Stafford KAJ, Thomas PJ, Vimal M, Wall ID, Watson RJ, Wellaway N, Yao G, Prinjha RK. Wellaway CR, et al. J Med Chem. 2020 Jan 23;63(2):714-746. doi: 10.1021/acs.jmedchem.9b01670. Epub 2020 Jan 6. J Med Chem. 2020. PMID: 31904959
Fragment-Based Discovery of Low-Micromolar ATAD2 Bromodomain Inhibitors.
Demont EH, Chung CW, Furze RC, Grandi P, Michon AM, Wellaway C, Barrett N, Bridges AM, Craggs PD, Diallo H, Dixon DP, Douault C, Emmons AJ, Jones EJ, Karamshi BV, Locke K, Mitchell DJ, Mouzon BH, Prinjha RK, Roberts AD, Sheppard RJ, Watson RJ, Bamborough P. Demont EH, et al. J Med Chem. 2015 Jul 23;58(14):5649-73. doi: 10.1021/acs.jmedchem.5b00772. Epub 2015 Jul 9. J Med Chem. 2015. PMID: 26155854
Click chemistry enables preclinical evaluation of targeted epigenetic therapies.
Tyler DS, Vappiani J, Cañeque T, Lam EYN, Ward A, Gilan O, Chan YC, Hienzsch A, Rutkowska A, Werner T, Wagner AJ, Lugo D, Gregory R, Ramirez Molina C, Garton N, Wellaway CR, Jackson S, MacPherson L, Figueiredo M, Stolzenburg S, Bell CC, House C, Dawson SJ, Hawkins ED, Drewes G, Prinjha RK, Rodriguez R, Grandi P, Dawson MA. Tyler DS, et al. Among authors: wellaway cr. Science. 2017 Jun 30;356(6345):1397-1401. doi: 10.1126/science.aal2066. Epub 2017 Jun 15. Science. 2017. PMID: 28619718 Free PMC article.
Selective targeting of BD1 and BD2 of the BET proteins in cancer and immunoinflammation.
Gilan O, Rioja I, Knezevic K, Bell MJ, Yeung MM, Harker NR, Lam EYN, Chung CW, Bamborough P, Petretich M, Urh M, Atkinson SJ, Bassil AK, Roberts EJ, Vassiliadis D, Burr ML, Preston AGS, Wellaway C, Werner T, Gray JR, Michon AM, Gobbetti T, Kumar V, Soden PE, Haynes A, Vappiani J, Tough DF, Taylor S, Dawson SJ, Bantscheff M, Lindon M, Drewes G, Demont EH, Daniels DL, Grandi P, Prinjha RK, Dawson MA. Gilan O, et al. Science. 2020 Apr 24;368(6489):387-394. doi: 10.1126/science.aaz8455. Epub 2020 Mar 19. Science. 2020. PMID: 32193360 Free PMC article.
Structure-Based Design of a Bromodomain and Extraterminal Domain (BET) Inhibitor Selective for the N-Terminal Bromodomains That Retains an Anti-inflammatory and Antiproliferative Phenotype.
Wellaway CR, Bamborough P, Bernard SG, Chung CW, Craggs PD, Cutler L, Demont EH, Evans JP, Gordon L, Karamshi B, Lewis AJ, Lindon MJ, Mitchell DJ, Rioja I, Soden PE, Taylor S, Watson RJ, Willis R, Woolven JM, Wyspiańska BS, Kerr WJ, Prinjha RK. Wellaway CR, et al. J Med Chem. 2020 Sep 10;63(17):9020-9044. doi: 10.1021/acs.jmedchem.0c00566. Epub 2020 Aug 3. J Med Chem. 2020. PMID: 32787145 Free article.
Investigation of Janus Kinase (JAK) Inhibitors for Lung Delivery and the Importance of Aldehyde Oxidase Metabolism.
Wellaway CR, Baldwin IR, Bamborough P, Barker D, Bartholomew MA, Chung CW, Dümpelfeld B, Evans JP, Fazakerley NJ, Homes P, Keeling SP, Lewell XQ, McNab FW, Morley J, Needham D, Neu M, van Oosterhout AJM, Pal A, Reinhard FBM, Rianjongdee F, Robertson CM, Rowland P, Shah RR, Sherriff EB, Sloan LA, Teague S, Thomas DA, Wellaway N, Wojno-Picon J, Woolven JM, Coe DM. Wellaway CR, et al. J Med Chem. 2022 Jan 13;65(1):633-664. doi: 10.1021/acs.jmedchem.1c01765. Epub 2021 Dec 20. J Med Chem. 2022. PMID: 34928601
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: wellaway cr. 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.
Structure-Guided Design of a Domain-Selective Bromodomain and Extra Terminal N-Terminal Bromodomain Chemical Probe.
Bradley E, Fusani L, Chung CW, Craggs PD, Demont EH, Humphreys PG, Mitchell DJ, Phillipou A, Rioja I, Shah RR, Wellaway CR, Prinjha RK, Palmer DS, Kerr WJ, Reid M, Wall ID, Cookson R. Bradley E, et al. Among authors: wellaway cr. J Med Chem. 2023 Dec 14;66(23):15728-15749. doi: 10.1021/acs.jmedchem.3c00906. Epub 2023 Nov 15. J Med Chem. 2023. PMID: 37967462 Free PMC article.
12 results