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An aldol-based build/couple/pair strategy for the synthesis of medium- and large-sized rings: discovery of macrocyclic histone deacetylase inhibitors.
Marcaurelle LA, Comer E, Dandapani S, Duvall JR, Gerard B, Kesavan S, Lee MD 4th, Liu H, Lowe JT, Marie JC, Mulrooney CA, Pandya BA, Rowley A, Ryba TD, Suh BC, Wei J, Young DW, Akella LB, Ross NT, Zhang YL, Fass DM, Reis SA, Zhao WN, Haggarty SJ, Palmer M, Foley MA. Marcaurelle LA, et al. Among authors: reis sa. J Am Chem Soc. 2010 Dec 1;132(47):16962-76. doi: 10.1021/ja105119r. Epub 2010 Nov 10. J Am Chem Soc. 2010. PMID: 21067169 Free PMC article.
Crebinostat: a novel cognitive enhancer that inhibits histone deacetylase activity and modulates chromatin-mediated neuroplasticity.
Fass DM, Reis SA, Ghosh B, Hennig KM, Joseph NF, Zhao WN, Nieland TJ, Guan JS, Kuhnle CE, Tang W, Barker DD, Mazitschek R, Schreiber SL, Tsai LH, Haggarty SJ. Fass DM, et al. Among authors: reis sa. Neuropharmacology. 2013 Jan;64:81-96. doi: 10.1016/j.neuropharm.2012.06.043. Epub 2012 Jul 4. Neuropharmacology. 2013. PMID: 22771460 Free PMC article.
A selective HDAC 1/2 inhibitor modulates chromatin and gene expression in brain and alters mouse behavior in two mood-related tests.
Schroeder FA, Lewis MC, Fass DM, Wagner FF, Zhang YL, Hennig KM, Gale J, Zhao WN, Reis S, Barker DD, Berry-Scott E, Kim SW, Clore EL, Hooker JM, Holson EB, Haggarty SJ, Petryshen TL. Schroeder FA, et al. PLoS One. 2013 Aug 14;8(8):e71323. doi: 10.1371/journal.pone.0071323. eCollection 2013. PLoS One. 2013. PMID: 23967191 Free PMC article.
PET imaging demonstrates histone deacetylase target engagement and clarifies brain penetrance of known and novel small molecule inhibitors in rat.
Schroeder FA, Wang C, Van de Bittner GC, Neelamegam R, Takakura WR, Karunakaran A, Wey HY, Reis SA, Gale J, Zhang YL, Holson EB, Haggarty SJ, Hooker JM. Schroeder FA, et al. Among authors: reis sa. ACS Chem Neurosci. 2014 Oct 15;5(10):1055-62. doi: 10.1021/cn500162j. Epub 2014 Sep 19. ACS Chem Neurosci. 2014. PMID: 25188794 Free PMC article.
Kinetically Selective Inhibitors of Histone Deacetylase 2 (HDAC2) as Cognition Enhancers.
Wagner FF, Zhang YL, Fass DM, Joseph N, Gale JP, Weïwer M, McCarren P, Fisher SL, Kaya T, Zhao WN, Reis SA, Hennig KM, Thomas M, Lemercier BC, Lewis MC, Guan JS, Moyer MP, Scolnick E, Haggarty SJ, Tsai LH, Holson EB. Wagner FF, et al. Among authors: reis sa. Chem Sci. 2015 Jan 1;6(1):804-815. doi: 10.1039/C4SC02130D. Chem Sci. 2015. PMID: 25642316 Free PMC article.
55 results