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Título: | 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. |
Autor: | Ribeiro, João P. CSIC ORCID; André, Sabine; Cañada, F. Javier ; Gabius, Hans-Joachim; Butera, Anna Paola; Alves, Ricardo José; Jiménez-Barbero, Jesús CSIC ORCID | Palabras clave: | Antitumor agents Drug design Lectins Molecular recognition NMR Glycoproteins Lactose Ribosome inactivating proteins Viscum album viscumin |
Fecha de publicación: | 1-mar-2010 | Editor: | Wiley-VCH ChemPubSoc Europe |
Citación: | ChemMedChem, 5(3): 415–419 (2010) | Resumen: | The growing awareness of the sugar code—i.e. the biological functionality of glycans—is leading to increased interest in lectins as drug targets. The aim of this study was to establish a strategic combination of screening procedures with increased biorelevance. As a model, we used a potent plant toxin (viscumin) and lactosides synthetically modified at the C6/C6′ positions and the reducing end aglycan. Changes in the saturation transfer difference (STD) in NMR spectroscopy, applied in inhibition assays, yielded evidence for ligand activity and affinity differences. Inhibitory potency was confirmed by the blocking of lectin binding to a glycoprotein-bearing matrix. In cell-based assays, iodo/azido-substituted lactose derivatives were comparatively active. Interestingly, cell-type dependence was observed, indicating the potential of synthetic carbohydrate derivative to interact with lectins in a cell-type (glycan profile)-specific manner. These results are relevant to research into human lectins, glycosciences, and beyond. | Descripción: | Detailed facts of importance to specialist readers are published as ”Supporting Information” at Wiley OnlineLibrary with the filename: cmdc_200900476_sm_miscellaneous_information.pdf | Versión del editor: | http://dx.doi.org/10.1002/cmdc.200900476 | URI: | http://hdl.handle.net/10261/41834 | DOI: | 10.1002/cmdc.200900476 | E-ISSN: | 1860-7187 |
Aparece en las colecciones: | (CIB) Artículos |
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