Effects of linker and liposome anchoring on lactose-functionalized glycomacromolecules as multivalent ligands for binding galectin-3

copper catalyzed 1,3-dipolar cycloaddition. Binding studies with galectin-3 revealed affinities in the micromolar range that increased with increasing carbohydrate valency, and decreased with increasing size and linker flexibility. To further explore their multivalency, selected glycomacromolecules were conjugated to lipids and used in liposomal formulations. Binding studies show a further increase in binding in nanomolar ranges in dependence of both ligand structure and liposomal presentation, demonstrating the power of combining the two approaches.