Strength in Numbers

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Science  20 Sep 2002:
Vol. 297, Issue 5589, pp. 1959
DOI: 10.1126/science.297.5589.1959b

Recognition events at cellular membranes frequently involve the simultaneous contact of several oligosaccharide ligands connected to one biomolecule with multiple protein receptors. Such polyvalent interactions serve to increase the strength of the interaction. Thoma et al. report a strategy for creating artificial polyvalent structures based on dendrimers—synthetic macromolecules with a treelike chemical structure—that self-assemble into nanoparticles. The dendrimers carry carbohydrate ligands known to inhibit immunoglobulin binding. The authors show that the nanoparticles inhibit immunoglobulin binding both in vitro and in vivo in cynomolgus monkeys. Only assemblies from second- and third-generation dendrimers were highly potent, indicating that potency correlates with the size of the aggregates. By tuning the aggregate size and the nature of the ligands, it should be possible to adapt the system to a variety of physiological polyvalent interactions. — JFU

Angew. Chem. Int. Ed.41, 3195 (2002).

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