Potent Histone Deacetylase Inhibitory Activity Research Articles

Cyclic tetrapeptides bearing a sulfhydryl group potently inhibit histone deacetylases.

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]