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

Yang, M., Proctor, M.R., Bolam, D.N., Errey, J.C., Field, R.A., Gilbert, H.J. and Davis, B.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. 10.1021/ja051482n .

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DOI: 10.1021/ja051482n

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
Additional Information:Full text available in print and electronically from the School of Pharmacy Library.
Departments, units and centres:Department of Pharmaceutical and Biological Chemistry > Department of Pharmaceutical and Biological Chemistry
ID Code:918
Journal or Publication Title:Journal of the American Chemical Society
Deposited By:Library Staff
Deposited On:14 May 2008 16:17
Last Modified:14 Oct 2011 15:47

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