期刊
NATURE CHEMICAL BIOLOGY
卷 3, 期 10, 页码 657-662出版社
NATURE PUBLISHING GROUP
DOI: 10.1038/nchembio.2007.28
关键词
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资金
- NCI NIH HHS [U19 CA113297] Funding Source: Medline
- NIAID NIH HHS [AI52218] Funding Source: Medline
Natural products, many of which are decorated with essential sugar residues, continue to serve as a key platform for drug development(1). Adding or changing sugars attached to such natural products can improve the parent compound's pharmacological properties, specificity at multiple levels(2), and/ or even the molecular mechanism of action(3). Though some natural-product glycosyltransferases ( GTs) are sufficiently promiscuous for use in altering these glycosylation patterns, the stringent specificity of others remains a limiting factor in natural-product diversification and highlights a need for general GT engineering and evolution platforms. Herein we report the use of a simple high-throughput screen based on a fluorescent surrogate acceptor substrate to expand the promiscuity of a natural-product GT via directed evolution. Cumulatively, this study presents variant GTs for the glycorandomization of a range of therapeutically important acceptors, including aminocoumarins, flavonoids and macrolides, and a potential template for engineering other natural-product GTs.
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