1 research outputs found
Multivalent Glycomimetics with Affinity and Selectivity toward Fucose-Binding Receptors from Emerging Pathogens
Bacterial
and fungal pathogens involved in lung infection in cystic
fibrosis patients utilize a particular family of glycan-binding proteins,
characterized by the presentation of six fucose-binding sites on a
ring-shaped scaffold. These lectins are attractive targets for anti-infectious
compounds that could interfere in the recognition of host tissues
by pathogens. The design of a cyclopeptide-based hexavalent structure
allowed for the presentation of six fucose residues. The synthetic
hexavalent compound displays liable geometry resulting in high-avidity
binding by lectins from <i>Aspergillus fumigatus</i> and <i>Burkholderia ambifaria</i>. Replacing the
fucose residue with a conformationally constrained fucomimetic does
not alter the affinity and provides fine specificity with no binding
to other fucose-specific lectins