Title of Talk Carbohydrate globules: hexaphenylbenzene-cored ‘snowflake’ dendrimers for presentation of Poly-N-acetylglucosamine (PNAG) polysaccharides.
Abstract The development of synthetic vaccines displaying carbohydrate antigens has been hampered by the complexity, size and difficulty of synthesis of the antigens. We have developed a series of rigid antigen presenting scaffolds (RAPS) designed to allow presentation of components of antigens in a predictable and reproducible relative configuration. The scaffolds also allow for the display of simplified saccharide units in a way that approximates the surface topology of the complete complex carbohydrate antigen. Poly-N-acetylglucosamine (PNAG) saccharides are an important constituent of bacterial biofilms, such as those produced by Staphylococcus aureus. The native polysaccharide is a polymer of up to 130 units of β-(1à6)-glucosamine. In order to facilitate the development of fully synthetic vaccine constructs bearing shorter oligosaccharides we have developed a simple two-step iterative method for the synthesis of β-(1à6)-glucosamine oligosaccharides that are structurally similar to PNAG.1 We illustrate the method with the formation of the di, tri, tetra and pentasaccharide analogues. Twelve copies of these oligosaccharides have been efficiently coupled with the acetylenyl surface groups of the G1-hexaphenyl bezene cored ‘snowflake’-shaped dendrimer via a Huisgen 1,3-dipolar cycloaddition reaction to give a series of multivalent carbohydrate constructs that mimic the globular nodules of polysaccharide intercellular adhesin (PIA) produced by Staphylococcus aureus.2Details of the syntheses of these molecules will be presented.
Figure 1. Iterative synthesis of PNAG oligosaccharides
References: 1. Weaver, Lucy G.; Singh, Yogendra; Blanchfield, Joanne T.; Burn, Paul L. Carbohydrate Research, 2013, 371, 68 2. Weaver, Lucy G.; Singh, Yogendra; Vamvounis, George; Wyatt, Mark F.; Burn, Paul L.; Blanchfield, Joanne T. Polymer Chemistry submitted |
Joanne Blanchfield, Dr, Senior Lecturer
School of Chemistry and Molecular Biosciences, University of Queensland, St. Lucia, QLD 4072, AUSTRALIA e-mail: j.blanchfield@uq.edu.au
Selected Publications 1. Weaver, Lucy G.; Singh, Yogendra; Blanchfield, Joanne T.; Burn, Paul L. Carbohydrate Research, 2013, 371, 68 2. Weaver, Lucy G.; Singh, Yogendra; Vamvounis, George; Wyatt, Mark F.; Burn, Paul L.; Blanchfield, Joanne T. Polymer Chemistry submitted 3. Varamini, P.; Mansfeld, F.M.; Blanchfield, J.T.; Wyse, B.D.; Smith, .T.; Toth, I PLoS One, 2012, 7, e41909 4. Varamini, P.; Mansfeld, F.M.; Blanchfield, J.T.; Wyse, B.D.; Smith, .T.; Toth, I. J. Med. Chem. 2012, 55, 5859 5. Cros, C.D.; Toth, I.; Blanchfield, J.T. Bioorg. Med. Chem.2011, 19, 1528 |