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Issue 11, 2013
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Bacterial toxin inhibitors based on multivalent scaffolds

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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

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Publication details

The article was received on 23 Oct 2012 and first published on 21 Dec 2012


Article type: Tutorial Review
DOI: 10.1039/C2CS35430F
Chem. Soc. Rev., 2013,42, 4613-4622
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    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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