Antibiotic optimization via in vitro glycorandomization
摘要：
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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关键词：
ANTIBIOTICS PHARMACOLOGY SUGAR in the body GLYCOSYLATION LIGATURE (Surgery) SUGAR phosphates VANCOMYCIN
DOI：
10.1038/nbt909
被引量：
年份：
2004
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