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Synfacts 2007(8): 0880-0880  
DOI: 10.1055/s-2007-968805
Polymer-Supported Synthesis
© Georg Thieme Verlag Stuttgart · New York

Neoglycopeptide Dendrimer Library for Lectin Binding

Contributor(s): Yasuhiro Uozumi, Yoichi M. A. Yamada
E. Kolomiets, E. M. V. Johansson, O. Renaudet, T. Darbre*, J.-L. Reymond*
Universität Bern, Switzerland and Université Joseph Fourier, Grenoble, France
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Publication History

Publication Date:
24 July 2007 (online)

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Significance

A 15,625-membered peptide dendrimer combinatorial library with α-C-fucosyl residue at the four N-termini was prepared from Tenta­GelTM beads (0.5 g, 0.30 mmol/g, f = 90 mm). The library was assayed for binding to biotinylated Ulex europaeus lectin UEA-I and Pseudomonas aeruginosa lectin PA-IIL, and the lectine binding was measured using an enzyme-linked lectine assay (ELLA). Dendrimer 2a was identified as a potent ligand against UEA-I (IC50 = 11 mM) and PA-IIL (IC50 = 0.14 mM) to exhibit 100-fold higher potency than fucose for binding to UEA-I and PA-IIL.