Design Syntheses of Inhibitors of Glycoenzymes

The glycoconjugates existing at the cell surface and proteoglycan, an extracellular matrix, are synthesized by the sequential actions of multiple enzymes which hydrolyze or transfer specific glycosidic linkages. The specific inhibitors of such enzymes therefore are considered to play important roles in the functional investigation of oligosaccharides. Alkaloids and nucleotide analogs from natural sources are known to be inhibitors of these enzymes. Recent advances in the three dimensional analysis of glyco-related enzymes, especially the accumulated crystal structures of the glycosidases, have prompted chemists to design and synthesize inhibitors of glycoenzymes. A combined approach with combinatorial chemistry is also a current focus.