Hydrolytically Stable Multivalent Glycoclusters as inhibitors of Galectin-1 and Galectin-3: a comparative study.

ALEJANDRO JAVIER CAGNONI; ANABELA M. CUTINE; MARÍA EMILIA CANO; D.O. CROCI; JOSÉ KOVENSKY; MARÍA LAURA UHRIG; GABRIEL RABINOVICH; KARINA V. MARIÑO

Mar del Plata

Congreso; LIX Reunión Científica Anual de la Sociedad Argentina de Investigación Clínica; 2014

Sociedad Argentina de Investigación Clínica

In this work, we were able to compare the inhibitory ability of the different synthesized glycoclusters with both human Gal-1 and Gal-3, and we showed that this solid phase assay is a useful, robust, reproducible and appropriate method for analyzing galectin ligands. We have tested different families of glycoclusters bearing residues of N- and S- linked β-galactose moieties as inhibitors of human Gal-1 and Gal-3. Using a competitive solid phase assay, we have shown that an increment in the valency of the ligand produces a higher affinity for these hydrolytically stable glycoclusters, reflected by a decrease in their maximal inhibitory concentration (IC50) . Thus, these multivalent inhibitors may be promising chemotherapeutics in galectin-mediated biological processes.