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Probing the breadth of macrolide glycosyltransferases: in vitro remodeling of a polyketide antibiotic creates active bacterial uptake and enhances potency.

Abstract:

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. Su...

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Publication status:
Published

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Publisher copy:
10.1021/ja051482n

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Journal:
Journal of the American Chemical Society
Volume:
127
Issue:
26
Pages:
9336-9337
Publication date:
2005-07-05
DOI:
EISSN:
1520-5126
ISSN:
0002-7863
URN:
uuid:9967aaca-c2c8-4bee-8c1a-a9d92205c718
Source identifiers:
33149
Local pid:
pubs:33149

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