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

M. Yang, M.R. Proctor, D.N. Bolam, J.C. Errey, R.A. Field, H.J. Gilbert, B.G. Davis

Research output: Contribution to journalArticlepeer-review

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.
Original languageUndefined
Pages (from-to) 9336-9337
Number of pages2
JournalJournal of the American Chemical Society
Volume127
Issue number26
DOIs
Publication statusPublished - 11 Jun 2005

Research Beacons, Institutes and Platforms

  • Manchester Institute of Biotechnology

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