Synthesis and Biological Applications of Glycoconjugates


Olivier Renaudet, Nicolas Spinelli

DOI: 10.2174/97816080527761110101
eISBN: 978-1-60805-277-6, 2011
ISBN: 978-1-60805-537-1

Indexed in: Chemical Abstracts, Scopus, EBSCO.

The interactions between carbohydrates and proteins have been extensively explored in a wide range of physiological and pathological p...[view complete introduction]
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Monovalent and Multivalent Inhibitors of Bacterial Toxins

- Pp. 78-91 (14)

Edward D. Hayes and W. Bruce Turnbull


<p>Cholera and travellers' diarrhoea are caused by AB5 protein toxins that bind to ganglioside GM1 at the surface of the cells lining the intestine. Inhibition of this protein-carbohydrate interaction would prevent the toxin from entering the cells, and thus prevents toxin-induced diarrhoea. In this review we will describe the structures of the cholera and E. coli heat-labile toxins, and summarize the main strategies that have led to the development of monovalent and multivalent inhibitors of these toxins. A number of key design concepts emerge from these studies including the importance of pre-organization of the sugar residues within the monovalent ligands, and also the pre-organization of monovalent ligand groups within larger multivalent ligands. The importance of chelation and protein aggregation as mechanisms of multivalent inhibition is also discussed.</p>

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