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

Yang, Min, Proctor, Mark R., Bolam, David N., Errey, James C., Field, Robert A. ORCID: https://orcid.org/0000-0001-8574-0275, Gilbert, Harry J. and Davis, Benjamin G. (2005) Probing the breadth of macrolide glycosyltransferases: in vitro remodeling of a polyketide antibiotic creates active bacterial uptake and enhances potency. Journal of the American Chemical Society, 127 (26). pp. 9336-9337. ISSN 0002-7863

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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. Subsequent release of the targeting glycan by endogenous galactosidase activity releases 1.

Item Type:	Article
Uncontrolled Keywords:	catalysis,general chemistry,biochemistry,colloid and surface chemistry ,/dk/atira/pure/subjectarea/asjc/1500/1503
Faculty \ School:	Faculty of Science > School of Chemistry, Pharmacy and Pharmacology
Related URLs:	https://www.scopus.com/pages/publication...
Depositing User:	LivePure Connector
Date Deposited:	10 Sep 2024 12:30
Last Modified:	18 Jun 2026 20:21
URI:	https://ueaeprints.uea.ac.uk/id/eprint/96642
DOI:	10.1021/ja051482n

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