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, 21 (12), 1467-9

Antibiotic Optimization via in Vitro Glycorandomization

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Antibiotic Optimization via in Vitro Glycorandomization

Xun Fu et al. Nat Biotechnol.

Abstract

In nature, the attachment of sugars to small molecules is often used to mediate targeting, mechanism of action and/or pharmacology. As an alternative to pathway engineering or total synthesis, we report a useful method, in vitro glycorandomization (IVG), to diversify the glycosylation patterns of complex natural products. We have used flexible glycosyltransferases on nucleotide diphosphosugar (NDP-sugar) libraries to generate glycorandomized natural products and then applied chemoselective ligation to produce monoglycosylated vancomycins that rival vancomycin.

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