Issue 11, 2013

Bacterial toxininhibitors based on multivalent scaffolds

Abstract

Protein toxins released by certain intestinal bacteria are the cause of many diarrhoeal diseases including cholera and travellers' diarrhoea. The toxins enter their target cells by first binding to specific glycolipids in the cell membrane. Inhibition of these proteincarbohydrate interactions has the potential to prevent the toxins from reaching their site of action, and thus avoid the ensuing diarrhoea. Simple oligosaccharides typically have low affinities for the protein toxins, therefore inhibitor design has focussed on exploiting the principles of multivalency: multiple weak interactions acting in concert can enhance the overall binding interaction. The major classes of multivalent inhibitors investigated to date will be discussed; these include glycopolymers, glycodendrimers, tailored glycoclusters and inhibitors exploiting templated assembly.

Graphical abstract: Bacterial toxin inhibitors based on multivalent scaffolds

Article information

Article type
Tutorial Review
Submitted
23 Oct 2012
First published
21 Dec 2012
This article is Open Access

Chem. Soc. Rev., 2013,42, 4613-4622

Bacterial toxin inhibitors based on multivalent scaffolds

T. R. Branson and W. B. Turnbull, Chem. Soc. Rev., 2013, 42, 4613 DOI: 10.1039/C2CS35430F

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