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ID: ALA2157995

Journal: Bioorg Med Chem Lett

Title: Cyclic tetrapeptides with thioacetate tails or intramolecular disulfide bridge as potent inhibitors of histone deacetylases.

Authors: Hoque MA, Arai T, Nishino N, Kim HJ, Ito A, Yoshida M.

Abstract: Two thioacetate tails were introduced to the chlamydocin- and CHAP31-related cyclic tetrapeptides. An intramolecular disulfide bridge could be formed in the CHAP31-related cyclic peptides. Both the thioacetate-tailed and disulfide-bridged peptides were potent histone deacetylase inhibitors in the presence of sulfhydryl compound. Potent p21 promoter inducing activity was also observed in vivo.

CiteXplore: 23021104

DOI: 10.1016/j.bmcl.2012.03.004