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Bioorg Med Chem Lett. 2012 Nov 1;22(21):6770-2. doi: 10.1016/j.bmcl.2012.03.004. Epub 2012 Mar 8.

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

Author information

1
Graduate School of Life Science and Systems Engineering, Kyushu Institute of Technology, Kitakyushu 808-0196, Japan.

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.

PMID:
23021104
DOI:
10.1016/j.bmcl.2012.03.004
[Indexed for MEDLINE]

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