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Expanding the Chemical Diversity of Fasamycin Via Genome Mining and Biocatalysis

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journal contribution
posted on 2022-03-24, 21:08 authored by Kai Jiang, Xiaoli Yan, Zixin Deng, Chun Lei, Xudong Qu
Genome mining and biocatalytic modification of chemical structures are critical methods to develop new antibiotics. In this study, eight new fasamycins (3, 4, 6, and 812) along with five known analogues (1, 2, 5, 7, and 13) were obtained by the overexpression of two phosphopantetheinyl transferases (PPtases) in Streptomyces kanamyceticus and biocatalytic transformation with two halogenases. These new compounds displayed significant activity against Staphylococcus aureus and Bacillus subtilis, in particular, C-29-methyl and C-2/C-22-halogen derivatives. This study increases the chemical diversity of bioactive fasamycin derivatives and provides useful halogenation tools for engineering their scaffolds.

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