期刊
ACS MEDICINAL CHEMISTRY LETTERS
卷 6, 期 11, 页码 1156-1161出版社
AMER CHEMICAL SOC
DOI: 10.1021/acsmedchemlett.5b00303
关键词
HDAC6-selective inhibitors; mercaptoacetamides; 8-aminoquinoline; 1,2,3,4-tetrahydroquinoline; Treg
资金
- NIH [NS079183, U19MH085195]
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 mu M. To assess possible therapeutic effects, compounds were assayed for their ability to increase T-regulatory (Treg) suppressive function. Some but not all of the compounds increased Treg function, and thereby decreased conventional T cell activation and proliferation in vitro.
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