Kinetically selective inhibitors of histone deacetylase 2 (HDAC2) as cognition enhancers

作者：Florence F. Wagner, Yarong Zhang, Daniel M. Fass, Naima T. Joseph, Jennifer P. Gale, Michel Weïwer, Patrick R. McCarren, Stewart L. Fisher, Taner Kaya, Wen‐Ning Zhao, Surya A. Reis, Krista M. Hennig, Melvin Edward Thomas, Bérénice C. Lemercier, Michael C. Lewis, Ji‐Song Guan, M. P. Moyer, Edward M. Scolnick, Stephen J. Haggarty, Li‐Huei Tsai, Edward B. Holson · 发表于：Chemical Science · 年份：2014 · DOI：10.1039/c4sc02130d · 被引用次数：102 · 研究领域：Histone Deacetylase Inhibitors Research、Cholinesterase and Neurodegenerative Diseases、Protein Degradation and Inhibitors

) increased H4K12 and H3K9 histone acetylation in primary mouse neuronal cell culture assays, in the hippocampus of CK-p25 mice, a model of neurodegenerative disease, and rescued the associated memory deficits of these mice in a cognition behavioural model. These studies demonstrate for the first time that selective pharmacological inhibition of HDAC2 is feasible and that inhibition of the catalytic activity of this enzyme may serve as a therapeutic approach towards enhancing the learning and memory processes that are affected in many neurological and psychiatric disorders.