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Page 1
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. Among authors: bassil ak. Science. 2020 Apr 24;368(6489):387-394. doi: 10.1126/science.aaz8455. Epub 2020 Mar 19. Science. 2020. PMID: 32193360 Free PMC article.
Template-Hopping Approach Leads to Potent, Selective, and Highly Soluble Bromo and Extraterminal Domain (BET) Second Bromodomain (BD2) Inhibitors.
Aylott HE, Atkinson SJ, Bamborough P, Bassil A, Chung CW, Gordon L, Grandi P, Gray JRJ, Harrison LA, Hayhow TG, Messenger C, Mitchell D, Phillipou A, Preston A, Prinjha RK, Rianjongdee F, Rioja I, Seal JT, Wall ID, Watson RJ, Woolven JM, Demont EH. Aylott HE, et al. J Med Chem. 2021 Mar 25;64(6):3249-3281. doi: 10.1021/acs.jmedchem.0c02156. Epub 2021 Mar 4. J Med Chem. 2021. PMID: 33662213
Identification of a Series of N-Methylpyridine-2-carboxamides as Potent and Selective Inhibitors of the Second Bromodomain (BD2) of the Bromo and Extra Terminal Domain (BET) Proteins.
Harrison LA, Atkinson SJ, Bassil A, Chung CW, Grandi P, Gray JRJ, Levernier E, Lewis A, Lugo D, Messenger C, Michon AM, Mitchell DJ, Preston A, Prinjha RK, Rioja I, Seal JT, Taylor S, Wall ID, Watson RJ, Woolven JM, Demont EH. Harrison LA, et al. J Med Chem. 2021 Aug 12;64(15):10742-10771. doi: 10.1021/acs.jmedchem.0c02155. Epub 2021 Jul 7. J Med Chem. 2021. PMID: 34232650
Fragment-based Scaffold Hopping: Identification of Potent, Selective, and Highly Soluble Bromo and Extra Terminal Domain (BET) Second Bromodomain (BD2) Inhibitors.
Seal JT, Atkinson SJ, Bamborough P, Bassil A, Chung CW, Foley J, Gordon L, Grandi P, Gray JRJ, Harrison LA, Kruger RG, Matteo JJ, McCabe MT, Messenger C, Mitchell D, Phillipou A, Preston A, Prinjha RK, Rianjongdee F, Rioja I, Taylor S, Wall ID, Watson RJ, Woolven JM, Wyce A, Zhang XP, Demont EH. Seal JT, et al. J Med Chem. 2021 Aug 12;64(15):10772-10805. doi: 10.1021/acs.jmedchem.1c00365. Epub 2021 Jul 13. J Med Chem. 2021. PMID: 34255512
Potent antimyeloma activity of the novel bromodomain inhibitors I-BET151 and I-BET762.
Chaidos A, Caputo V, Gouvedenou K, Liu B, Marigo I, Chaudhry MS, Rotolo A, Tough DF, Smithers NN, Bassil AK, Chapman TD, Harker NR, Barbash O, Tummino P, Al-Mahdi N, Haynes AC, Cutler L, Le B, Rahemtulla A, Roberts I, Kleijnen M, Witherington JJ, Parr NJ, Prinjha RK, Karadimitris A. Chaidos A, et al. Among authors: bassil ak. Blood. 2014 Jan 30;123(5):697-705. doi: 10.1182/blood-2013-01-478420. Epub 2013 Dec 13. Blood. 2014. PMID: 24335499 Free article.
Signaling function of PRC2 is essential for TCR-driven T cell responses.
Dobenecker MW, Park JS, Marcello J, McCabe MT, Gregory R, Knight SD, Rioja I, Bassil AK, Prinjha RK, Tarakhovsky A. Dobenecker MW, et al. Among authors: bassil ak. J Exp Med. 2018 Apr 2;215(4):1101-1113. doi: 10.1084/jem.20170084. Epub 2018 Mar 9. J Exp Med. 2018. PMID: 29523590 Free PMC article.
Phase 1 and preclinical profiling of ESM-HDAC391, a myeloid-targeted histone deacetylase inhibitor, shows enhanced pharmacology and monocytopaenia.
Furze RC, Molnar J, Parr NJ, Ahmad F, Henry Y, Howe D, Singh R, Toal M, Bassil AK, Bernard SG, Davis RP, Gibson A, Maller NC, Sharp C, Tough DF, Prinjha RK, Lewis HD. Furze RC, et al. Among authors: bassil ak. Br J Clin Pharmacol. 2022 Dec;88(12):5238-5256. doi: 10.1111/bcp.15428. Epub 2022 Jul 11. Br J Clin Pharmacol. 2022. PMID: 35655123 Free PMC article. Clinical Trial.
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