It is well established that protein- and lipid-bound saccharides play essential roles in many molecular processes impacting eukaryotic biology and disease. Progress in glycobiology is, however, hampered by the inaccessibility of well-defined oligosaccharides and glycoconjugates for biological and biomedical studies. The Boons group is addressing these issues by developing chemical and chemoenzymatic methods and strategies for complex oligosaccharide and glycoconjugate synthesis. In particular, methods were developed that employ a small number of monosaccharide building blocks for the assembly of a large number of complex compounds involving a minimal number of chemical steps. Furthermore, we devised new approaches for controlling anomeric selectivities of glycosylations, which has been one of the most important stumbling blocks in oligosaccharide assembly.
The new methodologies have been applied for synthesis of biological important oligosaccharides such as N– and O-glycans, ganglio-oligosaccharides, heparan sulfates, tumor-associated antigens, and capsular polysaccharides of pathogenic bacteria. A hallmark of our program is to employ synthesized target molecules for biological and biomedical explorations. Particularly, we have made contributions to the understanding of infectious, immunological and inflammatory processes mediated by complex oligosaccharides and glycoconjugates at a molecular level. This information, in turn, is being exploited for the design of fully synthetic immuno-modulators, vaccines and anti-inflammatory and cancer drugs. A highlight of such program was the design, chemical synthesis, and immunological examination of three-component vaccine candidates that offer a prospect to be employed as a therapeutic vaccine for many types of epithelial cancer. Synthetic glycans have been used for microarray development and screening efforts have identified lead compounds that are being developed as glycomimetics for the treatment of various diseases. The Boons group has also made substantial contributions to the development of methods for visualizing glycoconjugates of living cells.