Cyclic Histone Deacetylase Inhibitors HDACs

Histone deacetylase inhibitors, peptides that inhibit histone deacetylases (HDAC). Inhibition of HDAC effects cell-cycle arrest and induces differentiation. Therefore, HDAC is considered a target for new types of pharmaceuticals for treatment of cancers, and several naturally occurring or synthetic peptides have been reported as lead structures. The most prominent family is a series of cyclic tetrapeptides containing the non-proteinogenic amino acid Aoe [(2S,9S)-2-amino-8-oxo-9,10-epoxydecanoic... 

Bugula collected in the US Virgin Islands produces by culture two cyclic tetrapeptides, microsporins A and B, which are potent inhibitors of histone deacetylase (HDAC) and cytotoxic for several human cancer cell lines (Gu et al., 2007). Microsporin A contains two nonribosomal amino acids o-pipecolic add (Pip) and 2(S)-amino-8-oxo-decanoic... 

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