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Page 1
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. Among authors: furze rc. 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
A Qualified Success: Discovery of a New Series of ATAD2 Bromodomain Inhibitors with a Novel Binding Mode Using High-Throughput Screening and Hit Qualification.
Bamborough P, Chung CW, Demont EH, Bridges AM, Craggs PD, Dixon DP, Francis P, Furze RC, Grandi P, Jones EJ, Karamshi B, Locke K, Lucas SCC, Michon AM, Mitchell DJ, Pogány P, Prinjha RK, Rau C, Roa AM, Roberts AD, Sheppard RJ, Watson RJ. Bamborough P, et al. Among authors: furze rc. J Med Chem. 2019 Aug 22;62(16):7506-7525. doi: 10.1021/acs.jmedchem.9b00673. Epub 2019 Aug 9. J Med Chem. 2019. PMID: 31398032
Structure-Based Optimization of Naphthyridones into Potent ATAD2 Bromodomain Inhibitors.
Bamborough P, Chung CW, Furze RC, Grandi P, Michon AM, Sheppard RJ, Barnett H, Diallo H, Dixon DP, Douault C, Jones EJ, Karamshi B, Mitchell DJ, Prinjha RK, Rau C, Watson RJ, Werner T, Demont EH. Bamborough P, et al. Among authors: furze rc. J Med Chem. 2015 Aug 13;58(15):6151-78. doi: 10.1021/acs.jmedchem.5b00773. Epub 2015 Jul 31. J Med Chem. 2015. PMID: 26230603
A Chemical Probe for the ATAD2 Bromodomain.
Bamborough P, Chung CW, Demont EH, Furze RC, Bannister AJ, Che KH, Diallo H, Douault C, Grandi P, Kouzarides T, Michon AM, Mitchell DJ, Prinjha RK, Rau C, Robson S, Sheppard RJ, Upton R, Watson RJ. Bamborough P, et al. Among authors: furze rc. Angew Chem Int Ed Engl. 2016 Sep 12;55(38):11382-6. doi: 10.1002/anie.201603928. Epub 2016 Aug 17. Angew Chem Int Ed Engl. 2016. PMID: 27530368 Free PMC article.
BET bromodomain inhibitors show anti-papillomavirus activity in vitro and block CRPV wart growth in vivo.
Morse MA, Balogh KK, Brendle SA, Campbell CA, Chen MX, Furze RC, Harada IL, Holyer ID, Kumar U, Lee K, Prinjha RK, Rüdiger M, Seal JT, Taylor S, Witherington J, Christensen ND. Morse MA, et al. Among authors: furze rc. Antiviral Res. 2018 Jun;154:158-165. doi: 10.1016/j.antiviral.2018.03.012. Epub 2018 Apr 11. Antiviral Res. 2018. PMID: 29653131 Free PMC article.
Carboxylesterase-1 Assisted Targeting of HDAC Inhibitors to Mononuclear Myeloid Cells in Inflammatory Bowel Disease.
Elfiky AMI, Ghiboub M, Li Yim AYF, Hageman IL, Verhoeff J, de Krijger M, van Hamersveld PHP, Welting O, Admiraal I, Rahman S, Garcia-Vallejo JJ, Wildenberg ME, Tomlinson L, Gregory R, Rioja I, Prinjha RK, Furze RC, Lewis HD, Mander PK, Heinsbroek SEM, Bell MJ, de Jonge WJ. Elfiky AMI, et al. Among authors: furze rc. J Crohns Colitis. 2022 May 10;16(4):668-681. doi: 10.1093/ecco-jcc/jjab176. J Crohns Colitis. 2022. PMID: 34633041 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. 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.
23 results