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01-23-2010
VIP: Lectin-Based Drug Design: Combined Strategy to Identify Lead Compounds using STD NMR Spectroscopy, Solid-Phase Assays, and Cell Binding for a Plant Toxin Model

João P. Ribeiro, Sabine André, F. Javier Cañada, Hans-Joachim Gabius, Anna Paola Butera, Ricardo José Alves, and Jesús Jiménez-Barbero*

Turning sugars into pharmaceuticals: In their Full Paper, Jiménez-Barbero and colleagues demonstrate the validity of lectins—sugar-binding proteins—as targets in drug design. Using a plant toxin model, they tested a series of modified lactosides containing aromatic aglycan groups for the ability to inhibit the cell-surface glycan–lectin binding interaction, thus blocking cellular uptake of the plant toxin. Given the emerging awareness of the sugar code, the biological importance of glycans is becoming increasingly apparent, and this work shows that addressing the challenges of carbohydrate chemistry is becoming ever more important and fruitful in the search for new and improved drugs.

Received November 20, 2009; published online January 21, 2010, DOI: 10.1002/cmdc.200900476.

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