C-4 Modified Sialosides Enhance Binding to Siglec-2 (CD22): Towards Potent Siglec Inhibitors for Immunoglycotherapy


  • We gratefully acknowledge the financial support of the Volkswagenstiftung (S.K.), Deutsche Forschungsgemeinschaft (S.K.), Tönjes-Vagt-Stiftung (S.K.), and the Australian Research Council (T.H., M.v.I.). S.K. is thankful for the Sir Allan Sewell Fellowship awarded by Griffith University. We thank Mary Murphy (Reichert Inc, Depew, NY (USA)) for the SPR analysis.


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Two changes for the better: A novel class of sialic acid derivatives is prepared by modifying both the C-4 and C-9 positions of Neu5Aα2Me (see structure). This approach gives a lead compound that has sub-micromolar affinity for Siglec-2 and may provide a pathway for immunoglycotherapy strategies for autoimmune diseases and B cell derived non-Hodgkin's lymphoma.