期刊
CHEMISTRY-A EUROPEAN JOURNAL
卷 17, 期 7, 页码 2146-2159出版社
WILEY-V C H VERLAG GMBH
DOI: 10.1002/chem.201002635
关键词
calixarenes; carbohydrates; glycoclusters; lectins; multivalency
资金
- Universite Claude Bernard Lyon 1
- Universite Blaise Pascal-Clermont-Ferrand II
- CNRS
- Region Rhone-Alpes
- ANR Glycoasterix
- Czech Ministry of Education [MSM0021622413, ME08008]
- European Community [205872]
The design of multivalent glycoconjugates has been developed over the past decades to obtain high-affinity ligands for lectin receptors. While multivalency frequently increases the affinity of a ligand for its lectin through the so-called glycoside cluster effect, the binding profiles towards different lectins have been much less investigated. We have designed a series of multivalent galactosylated glycoconjugates and studied their binding properties towards two lectins, from plant and bacterial origins, to determine their potential selectivity. The synthesis was achieved through copper(I)-catalysed azide-alkyne cycloaddition (CuAAC) under microwave activation between propargylated multivalent scaffolds and an azido-functionalised carbohydrate derivative. The interactions of two galactose-binding lectins from Pseudomonas aeruginosa (PA-IL) and Erythrina cristagalli (ECA) with the synthesized glycoclusters were studied by hemagglutination inhibition assays (HIA), surface plasmon resonance (SPR) and isothermal titration microcalorimetry (ITC). The results obtained illustrate the influence of the scaffold's geometry on the affinity towards the lectin and also on the relative potency in comparison with a monovalent galactoside reference probe.
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