Galectins are a protein family defined by their affinity for β-galactosides and consensus sequences. They are pleiotropic regulators involved in a multitude of functions, both in and out of the cell. Extracellularly, they have the potential to bind to various surface receptors on a variety of cell types as well as extracellular matrix (ECM) proteins, thus causing cell activation or apoptosis, modulating cell adhesion and inducing cell migration. Intracellularly, they can regulate cell growth, apoptosis and cell cycle progression. Galectins are either pro-inflammatory or anti-inflammatory. Some, such as galectin-1, may be employed as anti-inflammatory agents, while others, such as galectin-3, are evidently suitable targets for anti-inflammatory drugs. The extracellular functions of galectins involve their lectin–carbohydrate interactions and thus their carbohydrate ligands or mimetics would be suitable inhibitors. While the intracellular functions of galectins do not appear to engage lectin–carbohydrate interactions, the carbohydrate-binding sites of these proteins may still be involved. Therefore, the same inhibitors may be used regardless of whether intracellular or extracellular galectins are to be targeted.