Depsipeptide


A depsipeptide is a peptide in which one or more of its amide, -CNHR-, groups are replaced by the corresponding ester, -COR, Many depsipeptides have both peptide and ester linkages. They are mainly found in marine and microbial natural products.

Depsipeptide natural products

Several depsipeptides have been found to exhibit anti-cancer properties.
A depsipeptide enzyme inhibitor includes romidepsin, a member of the bicyclic peptide class, a known histone deacetylase inhibitors. It was first isolated as a fermentation product from Chromobacterium violaceum by the Fujisawa Pharmaceutical Company.
Etamycin was shown in preliminary data in 2010 to have potent activity against MRSA in a mouse model. Several depsipeptides from Streptomyces exhibit antimicrobial activity. These form a new, potential class of antibiotics known as acyldepsipeptides. ADEPs target and activate the casein lytic protease to initiate uncontrolled peptide and unfolded protein degradation, killing many Gram-positive bacteria.