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Development of a series of aryl pyrimidine kynurenine monooxygenase inhibitors as potential therapeutic agents for the treatment of Huntington's disease.
Toledo-Sherman LM, Prime ME, Mrzljak L, Beconi MG, Beresford A, Brookfield FA, Brown CJ, Cardaun I, Courtney SM, Dijkman U, Hamelin-Flegg E, Johnson PD, Kempf V, Lyons K, Matthews K, Mitchell WL, O'Connell C, Pena P, Powell K, Rassoulpour A, Reed L, Reindl W, Selvaratnam S, Friley WW, Weddell DA, Went NE, Wheelan P, Winkler C, Winkler D, Wityak J, Yarnold CJ, Yates D, Munoz-Sanjuan I, Dominguez C. Toledo-Sherman LM, et al. J Med Chem. 2015 Feb 12;58(3):1159-83. doi: 10.1021/jm501350y. Epub 2015 Jan 23. J Med Chem. 2015. PMID: 25590515
Exploiting differences in caspase-2 and -3 S₂ subsites for selectivity: structure-based design, solid-phase synthesis and in vitro activity of novel substrate-based caspase-2 inhibitors.
Maillard MC, Brookfield FA, Courtney SM, Eustache FM, Gemkow MJ, Handel RK, Johnson LC, Johnson PD, Kerry MA, Krieger F, Meniconi M, Muñoz-Sanjuán I, Palfrey JJ, Park H, Schaertl S, Taylor MG, Weddell D, Dominguez C. Maillard MC, et al. Bioorg Med Chem. 2011 Oct 1;19(19):5833-51. doi: 10.1016/j.bmc.2011.08.020. Epub 2011 Aug 16. Bioorg Med Chem. 2011. PMID: 21903398
Discovery and structure-activity relationship of potent and selective covalent inhibitors of transglutaminase 2 for Huntington's disease.
Prime ME, Andersen OA, Barker JJ, Brooks MA, Cheng RK, Toogood-Johnson I, Courtney SM, Brookfield FA, Yarnold CJ, Marston RW, Johnson PD, Johnsen SF, Palfrey JJ, Vaidya D, Erfan S, Ichihara O, Felicetti B, Palan S, Pedret-Dunn A, Schaertl S, Sternberger I, Ebneth A, Scheel A, Winkler D, Toledo-Sherman L, Beconi M, Macdonald D, Muñoz-Sanjuan I, Dominguez C, Wityak J. Prime ME, et al. J Med Chem. 2012 Feb 9;55(3):1021-46. doi: 10.1021/jm201310y. Epub 2012 Jan 27. J Med Chem. 2012. PMID: 22224594
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. PLoS One. 2012;7(9):e44498. doi: 10.1371/journal.pone.0044498. Epub 2012 Sep 4. PLoS One. 2012. PMID: 22973455 Free PMC article.
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
102 results