Thiol-based potent and selective HDAC6 inhibitors promote tubulin acetylation and T-regulatory cell suppressive function

…, GP Vallerini, C Brochier, B Langley…

文献索引：Butler, Kyle V.; Kalin, Jay; Brochier, Camille; Vistoli, Guilio; Langley, Brett; Kozikowski, Alan P. Journal of the American Chemical Society, 2010 , vol. 132, # 31 p. 10842 - 10846

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被引用次数: 3

摘要

Several new mercaptoacetamides were synthesized and studied as HDAC6 inhibitors. One compound, 2b, bearing an aminoquinoline cap group, was found to show 1.3 nM potency at HDAC6, with> 3000-fold selectivity over HDAC1. 2b also showed excellent efficacy at increasing tubulin acetylation in rat primary cortical cultures, inducing a 10-fold increase in acetylated tubulin at 1 μM. To assess possible therapeutic effects, compounds were ...