Nanomolar cholera toxin inhibitors based on symmetrical pentavalent ganglioside GM1os-sym-corannulenes
Eight symmetric and pentavalent corannulene derivatives were functionalized with galactose and the ganglioside GM1-oligosaccharide (GM1os) via copper-catalyzed alkyne-azide cycloaddition (CuAAC) reactions. The compounds were evaluated for their ability to inhibit the binding of the pentavalent cholera toxin to its natural ligand, ganglioside GM1. In this assay, all ganglioside GM1os-sym-corannulenes proved to be highly potent nanomolar inhibitors of cholera toxin.
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| Main Authors: | , , , , |
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| Format: | Article/Letter to editor biblioteca |
| Language: | English |
| Subjects: | corannulene, dendrimers, derivatives, design, gm1 mimics, heat-labile enterotoxin, multivalent ligands, receptor-binding, subunit, |
| Online Access: | https://research.wur.nl/en/publications/nanomolar-cholera-toxin-inhibitors-based-on-symmetrical-pentavale |
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| Summary: | Eight symmetric and pentavalent corannulene derivatives were functionalized with galactose and the ganglioside GM1-oligosaccharide (GM1os) via copper-catalyzed alkyne-azide cycloaddition (CuAAC) reactions. The compounds were evaluated for their ability to inhibit the binding of the pentavalent cholera toxin to its natural ligand, ganglioside GM1. In this assay, all ganglioside GM1os-sym-corannulenes proved to be highly potent nanomolar inhibitors of cholera toxin. |
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