Recent design of glycosyltransferase inhibitors

Carbohydrates are implicated in several biological phenomena and play an important role in fecundation, cancer and bacterial or viral infection. The biosynthesis of oligosaccharides displayed at the surface of the cell through glycoproteins or glycolipids is orchestrated by glycosyltransferases and glycosidases creating and hydrolysing glycosidic bonds, respectively. The present review will provide an overview of the past two decades of glycosyltransferase inhibitors development, and will consider not only the design of bioactive molecules but also fundamental studies of the roles of such proteins. Galactosyltransferases will be discussed since this class of enzymes is amongst the most intensively studied. Inhibitors designed against O‐linked N‐acetylglucosaminyl transferase (OGT) will also be reviewed as this enzyme has been recently identified as an important biological target.