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10.1021/acsmedchemlett.5b00303

http://scihub22266oqcxt.onion/10.1021/acsmedchemlett.5b00303
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C4645251!4645251!26617971
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suck abstract from ncbi


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pmid26617971      ACS+Med+Chem+Lett 2015 ; 6 (11): 1156-61
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  • Thiol-Based Potent and Selective HDAC6 Inhibitors Promote Tubulin Acetylation and T-Regulatory Cell Suppressive Function #MMPMID26617971
  • Segretti MCF; Vallerini GP; Brochier C; Langley B; Wang L; Hancock WW; Kozikowski AP
  • ACS Med Chem Lett 2015[Nov]; 6 (11): 1156-61 PMID26617971show ga
  • 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 ?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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