Discovery of galectin ligands in fully randomized combinatorial one-bead-one-compound (glyco)peptide libraries.
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.
André
Sabine
S
Institute of Physiological Chemistry, Faculty of Veterinary Medicine, Ludwig-Maximilians-University Munich, Veterinärstr. 13, 80539 Munich, Germany.
Maljaars
C Elizabeth P
CE
Halkes
Koen M
KM
Gabius
Hans-Joachim
HJ
Kamerling
Johannis P
JP
D045744:Cell Line, Tumor; D020650:Combinatorial Chemistry Techniques; D037161:Galectins / Q000737:chemistry*; D006020:Glycopeptides / Q000138:chemical synthesis* / Q000494:pharmacology; D006801:Humans; D007202:Indicators and Reagents; D008024:Ligands; D019151:Peptide Library
D037161:Galectins; D006020:Glycopeptides; D007202:Indicators and Reagents; D008024:Ligands; D019151:Peptide Library