Over the last decade an increasing number of studies have been published reporting on the inhibitory potency
or selectivity that several types of ligands show against human galectin-3 (hGal-3). The reason for this interest lies in the
many important roles galectins play both in intra and extra-cellular functions. Among galectins, galectin-3 stands out because
it is the only known member of its subfamily in mammals, is small and monomeric but capable of aggregating, and
is known to be involved in a large number of disease processes, from cancer to heart failure. These characteristics and
roles make hGal-3 an ideal target for drugs. Since it binds β-galactosides, like the rest of the galectin family of proteins,
the search and design of potent and at the same time selective inhibitors for it is not an easy task. Herein we discuss the
chemical features of the most potent inhibitors described so far, as well as the structural basis of their exhibited selectivity,
in order to shed light on the rational design of drugs against this target.
Keywords: Lectin, galectin-3, inhibitor, selectivity, galactose-specific receptor.
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