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Design, synthesis, and biological evaluation of potent and selective class IIa histone deacetylase (HDAC) inhibitors as a potential therapy for Huntington's disease.
Bürli RW, Luckhurst CA, Aziz O, Matthews KL, Yates D, Lyons KA, Beconi M, McAllister G, Breccia P, Stott AJ, Penrose SD, Wall M, Lamers M, Leonard P, Müller I, Richardson CM, Jarvis R, Stones L, Hughes S, Wishart G, Haughan AF, O'Connell C, Mead T, McNeil H, Vann J, Mangette J, Maillard M, Beaumont V, Munoz-Sanjuan I, Dominguez C. Bürli RW, et al. J Med Chem. 2013 Dec 27;56(24):9934-54. doi: 10.1021/jm4011884. Epub 2013 Dec 5. J Med Chem. 2013. PMID: 24261862
A comparative study of fragment screening methods on the p38α kinase: new methods, new insights.
Pollack SJ, Beyer KS, Lock C, Müller I, Sheppard D, Lipkin M, Hardick D, Blurton P, Leonard PM, Hubbard PA, Todd D, Richardson CM, Ahrens T, Baader M, Hafenbradl DO, Hilyard K, Bürli RW. Pollack SJ, et al. Among authors: burli rw. J Comput Aided Mol Des. 2011 Jul;25(7):677-87. doi: 10.1007/s10822-011-9454-9. Epub 2011 Jul 6. J Comput Aided Mol Des. 2011. PMID: 21732248 Free PMC article.
Oral administration of the pimelic diphenylamide HDAC inhibitor HDACi 4b is unsuitable for chronic inhibition of HDAC activity in the CNS in vivo.
Beconi M, Aziz O, Matthews K, Moumné L, O'Connell C, Yates D, Clifton S, Pett H, Vann J, Crowley L, Haughan AF, Smith DL, Woodman B, Bates GP, Brookfield F, Bürli RW, McAllister G, Dominguez C, Munoz-Sanjuan I, Beaumont V. Beconi M, et al. Among authors: burli rw. PLoS One. 2012;7(9):e44498. doi: 10.1371/journal.pone.0044498. Epub 2012 Sep 4. PLoS One. 2012. PMID: 22973455 Free PMC article.
Potent, Selective, and CNS-Penetrant Tetrasubstituted Cyclopropane Class IIa Histone Deacetylase (HDAC) Inhibitors.
Luckhurst CA, Breccia P, Stott AJ, Aziz O, Birch HL, Bürli RW, Hughes SJ, Jarvis RE, Lamers M, Leonard PM, Matthews KL, McAllister G, Pollack S, Saville-Stones E, Wishart G, Yates D, Dominguez C. Luckhurst CA, et al. Among authors: burli rw. ACS Med Chem Lett. 2015 Dec 10;7(1):34-9. doi: 10.1021/acsmedchemlett.5b00302. eCollection 2016 Jan 14. ACS Med Chem Lett. 2015. PMID: 26819662 Free PMC article.
Toward β-Secretase-1 Inhibitors with Improved Isoform Selectivity.
Johansson P, Kaspersson K, Gurrell IK, Bäck E, Eketjäll S, Scott CW, Cebers G, Thorne P, McKenzie MJ, Beaton H, Davey P, Kolmodin K, Holenz J, Duggan ME, Budd Haeberlein S, Bürli RW. Johansson P, et al. Among authors: burli rw. J Med Chem. 2018 Apr 26;61(8):3491-3502. doi: 10.1021/acs.jmedchem.7b01716. Epub 2018 Apr 10. J Med Chem. 2018. PMID: 29617572
Development and characterization of a CNS-penetrant benzhydryl hydroxamic acid class IIa histone deacetylase inhibitor.
Luckhurst CA, Aziz O, Beaumont V, Bürli RW, Breccia P, Maillard MC, Haughan AF, Lamers M, Leonard P, Matthews KL, Raphy G, Stott AJ, Munoz-Sanjuan I, Thomas B, Wall M, Wishart G, Yates D, Dominguez C. Luckhurst CA, et al. Among authors: burli rw. Bioorg Med Chem Lett. 2019 Jan 1;29(1):83-88. doi: 10.1016/j.bmcl.2018.11.009. Epub 2018 Nov 13. Bioorg Med Chem Lett. 2019. PMID: 30463802
50 results