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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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.
|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|
|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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