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5-Aryl-4-carboxamide-1,3-oxazoles: potent and selective GSK-3 inhibitors.
Gentile G, Merlo G, Pozzan A, Bernasconi G, Bax B, Bamborough P, Bridges A, Carter P, Neu M, Yao G, Brough C, Cutler G, Coffin A, Belyanskaya S. Gentile G, et al. Among authors: bridges a. Bioorg Med Chem Lett. 2012 Mar 1;22(5):1989-94. doi: 10.1016/j.bmcl.2012.01.034. Epub 2012 Jan 21. Bioorg Med Chem Lett. 2012. PMID: 22310227
Identification of 2-(4-pyridyl)thienopyridinones as GSK-3β inhibitors.
Gentile G, Bernasconi G, Pozzan A, Merlo G, Marzorati P, Bamborough P, Bax B, Bridges A, Brough C, Carter P, Cutler G, Neu M, Takada M. Gentile G, et al. Among authors: bridges a. Bioorg Med Chem Lett. 2011 Aug 15;21(16):4823-7. doi: 10.1016/j.bmcl.2011.06.050. Epub 2011 Jun 29. Bioorg Med Chem Lett. 2011. PMID: 21764580
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
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. 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
Crystal structures of human RIP2 kinase catalytic domain complexed with ATP-competitive inhibitors: Foundations for understanding inhibitor selectivity.
Charnley AK, Convery MA, Lakdawala Shah A, Jones E, Hardwicke P, Bridges A, Ouellette M, Totoritis R, Schwartz B, King BW, Wisnoski DD, Kang J, Eidam PM, Votta BJ, Gough PJ, Marquis RW, Bertin J, Casillas L. Charnley AK, et al. Among authors: bridges a. Bioorg Med Chem. 2015 Nov 1;23(21):7000-6. doi: 10.1016/j.bmc.2015.09.038. Epub 2015 Sep 25. Bioorg Med Chem. 2015. PMID: 26455654
Crystallizing Membrane Proteins in the Lipidic Mesophase. Experience with Human Prostaglandin E2 Synthase 1 and an Evolving Strategy.
Li D, Howe N, Dukkipati A, Shah ST, Bax BD, Edge C, Bridges A, Hardwicke P, Singh OM, Giblin G, Pautsch A, Pfau R, Schnapp G, Wang M, Olieric V, Caffrey M. Li D, et al. Among authors: bridges a. Cryst Growth Des. 2014 Apr 2;14(4):2034-2047. doi: 10.1021/cg500157x. Epub 2014 Mar 7. Cryst Growth Des. 2014. PMID: 24803849 Free PMC 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: bridges a. 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.
526 results