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Curr Opin Chem Biol. 2009 Apr;13(2):189-96. doi: 10.1016/j.cbpa.2009.02.012. Epub 2009 Mar 9.

Diversification of echinomycin molecular structure by way of chemoenzymatic synthesis and heterologous expression of the engineered echinomycin biosynthetic pathway.

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  • 1Division of Chemistry, Graduate School of Science, Hokkaido University, Sapporo 060-0810, Japan.


Echinomycin, a bis-intercalator antitumor cyclic peptide, is biosynthesized by a unique nonribosomal peptide synthetase (NRPS). Successful heterologous expression of the whole gene cluster of echinomycin in Escherichia coli let us to investigate a further application of echinomycin NRPS. To construct a cyclic peptide library, our approach through both chemoenzymatic and rational genetic engineering has been successfully demonstrated. These achievements provided the further support that E. coli-based system can serve as a flexible yet robust platform for producing complex natural products and their analogs.

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