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

Bioorganic & medicinal chemistry letters (2012-10-02)
Md Ashraful Hoque, Toru Arai, Norikazu Nishino, Hyun-Jung Kim, Akihiro Ito, Minoru Yoshida
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.

MATERIALS
Product Number
Brand
Product Description

Sigma-Aldrich
Potassium thioacetate, 98%
Sigma-Aldrich
Thioacetic acid, 96%
Sigma-Aldrich
Thioacetic acid, 96%

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