Thiodigalactoside-BSA-Conjugates as High-Potency Inhibitors of Ga-lectin-3: An Outstanding Example of Multivalent Presentation of Small Molecule Inhibitors.
Bioconjug Chem 2018 Feb 23. Epub 2018 Feb 23.
Galectin inhibitors are urgently needed to understand the mode of action and druggability of different galectins, but potent and selective agents still eludes researchers to date. Small-sized inhibitors based on thiodigalactoside (TDG) have shown their potential while modifications at their C3 position indicated a strategy to improve selectivity and potency. Considering the role of galectins as a glycoprotein traffic police, involved in multivalent bridging interac-tions, we aimed to create multivalent versions of the potent TDG inhibitors. Read More