Staff Publications

Staff Publications

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    'Staff publications' is the digital repository of Wageningen University & Research

    'Staff publications' contains references to publications authored by Wageningen University staff from 1976 onward.

    Publications authored by the staff of the Research Institutes are available from 1995 onwards.

    Full text documents are added when available. The database is updated daily and currently holds about 240,000 items, of which 72,000 in open access.

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Record number 440114
Title Picomolar inhibition of cholera toxin by a pentavalent ganglioside GM1os-calix[5]arene
Author(s) Garcia-Hartjes, J.; Bernardi, S.; Weijers, C.A.G.M.; Wennekes, T.; Gilbert, M.; Sansone, F.; Casnati, A.; Zuilhof, H.
Source Organic & Biomolecular Chemistry 11 (2013). - ISSN 1477-0520 - p. 4340 - 4349.
DOI https://doi.org/10.1039/c3ob40515j
Department(s) Laboratory for Organic Chemistry
VLAG
Publication type Refereed Article in a scientific journal
Publication year 2013
Keyword(s) heat-labile enterotoxin - gm1 mimics - binding - ligand - hexamethylenetetramine - oligosaccharide - recognition - affinity - crystal - design
Abstract Cholera toxin (CT), the causative agent of cholera, displays a pentavalent binding domain that targets the oligosaccharide of ganglioside GM1 (GM1os) on the periphery of human abdominal epithelial cells. Here, we report the first GM1os-based CT inhibitor that matches the valency of the CT binding domain (CTB). This pentavalent inhibitor contains five GM1os moieties linked to a calix[5]arene scaffold. When evaluated by an inhibition assay, it achieved a picomolar inhibition potency (IC50 = 450 pM) for CTB. This represents a significant multivalency effect, with a relative inhibitory potency of 100000 compared to a monovalent GM1os derivative, making GM1os-calix[5]arene one of the most potent known CTB inhibitors.
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