Cyclic tetrapeptides bearing a sulfhydryl group potently inhibit histone deacetylases.

Org Lett

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

Published: December 2003

New inhibitors of histone deacetylase (HDAC) containing a sulfhydryl group were designed on the basis of the corresponding hydroxamic acid (CHAP31) and FK228. Their disulfide dimers and hybrids exhibited potent HDAC inhibitory activity in vivo with potential as anticancer prodrugs. [structure: see text]

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Source
http://dx.doi.org/10.1021/ol036098eDOI Listing

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