Design, synthesis and biological evaluation of iminosugar-based glycosyltransferase inhibitors.

Due to their pivotal role in the biosynthesis of oligosaccharides and glycoconjugates, glycosyltransferases represent targets of choice for the development of potent inhibitors and therefore for drug discovery. Since glycosyltransferase reactions are thought to proceed through transition states similar to those of glycosidases, iminosugars and the related compounds have been recently used to design potential inhibitors of this major class of enzymes. The purpose of this review is to stimulate further research in this promising area by providing a description and a biological evaluation of the different types of inhibitors containing an iminosugar. These data in addition to the recent insights into the structural basis of glycosyltransferase catalysis may constitute the first steps toward a rational design of potent glycosyltransferases inhibitors.