β-D-Galactopyranoside containing disaccharides as inhibitors of Galectin-1: a comparative study.

ANABELA M. CUTINE; M. E. GIORGI; MUCHNIK DE LEDERKREMER, ROSA; D.O. CROCI1; G. A. RABINOVICH; KARINA MARIÑO

Simposio; Primer Simposio Argentino de Glicobiologia GlycoAR; 2014

Galectins are a family of soluble proteins with a conserved carbohydrate recognition domain (CRD) that binds to Nacetyllactosamine residues. There is ample evidence of the role of galectins in cellular apoptosis, homeostasis, immunoregulation and tumor escape. Hence, targeting these proteins specifically with appropriate inhibitors could lead to improvement of therapeutic strategies for a variety of immune disorders. We optimized a solid phase assay to test possible inhibitors of galectin-1. This inhibitory assay is based on galectin interactions with the inhibitor tested and later with immobilized asialofetuin as a well known ligand. Using these data it is possible to calculate the half maximal inhibitory concentration (IC50) for each inhibitor evaluated. In this work we were able to compare the inhibitory ability of different β-Dgalactopyranoside- containing disaccharides (including lactose, lactobionolactone, lactobionic acid, Galβ(1-6)GlcNAc-α-OBn and lactitol), and we showed that this solid phase assay is a reproducible and appropriate method for analyzing possible galectin inhibitors.