Probing the Breadth of Macrolide Glycosyltransferases: In Vitro Remodeling of a Polyketide Antibiotic Creates Active Bacterial Uptake and Enhances Potency

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• 作者：Min Yang ; Mark R. Proctor ; David N. Bolam ; James C. Errey ; Robert A. Field ; Harry J. Gilbert ; and Benjamin G. Davis
• 刊名：Journal of the American Chemical Society
• 出版年：2005
• 出版时间：July 6, 2005
• 年：2005
• 卷：127
• 期：26
• 页码：9336 - 9337
• 全文大小：64K
• 年卷期：v.127,no.26(July 6, 2005)
• ISSN：1520-5126

文摘

The glycan portion of macrolide antibiotics modulates their efficacy. High-level expression of three macrolide GTs and kinetic analysis has revealed a highly selective synthetic "tool kit" with such plasticity that 12 glycan-modified macrolide antibiotics have been readily created. One of these (1-Gal) is enhanced over its parent oleandomycin (1) by "glycotargeting", allowing higher uptake through active internalization by virtue of the attachment of a glycan (Gal) not normally found on 1. Subsequent release of the targeting glycan by endogenous galactosidase activity releases 1.