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ID: ALA1138414

Journal: Bioorg Med Chem Lett

Title: Discovery of galectin ligands in fully randomized combinatorial one-bead-one-compound (glyco)peptide libraries.

Authors: André S, Maljaars CE, Halkes KM, Gabius HJ, Kamerling JP.

Abstract: The involvement of human lectins (galectins) in disease progression accounts for the interest to design potent inhibitors. Three fully randomized hexa(glyco)peptide libraries were prepared using the portion mixing method combined with ladder synthesis. On-bead screening with fluorescently labelled galectin-1 and -3 yielded a series of lead structures, whose inhibitory activity on carbohydrate-dependent galectin binding was tested in solution by solid-phase and cell assays. The various data obtained define the library approach as a facile route for the discovery of selective (glyco)peptide-based galectin inhibitors.

CiteXplore: 17095217

DOI: 10.1016/j.bmcl.2006.10.067