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Review | Special issue | Vol 99, No. 1, 2019, pp.73-82
Published online, 20th November, 2018
DOI: 10.3987/REV-18-SR(F)3
Renovation of Glycomolecules for Molecular Imaging Studies: Low-Affinity Glycan Ligands can be Used for Selective Cell Imaging?

Shogo Nomura and Katsunori Tanaka*

*Biofunctional Synthetic Chemistry Laboratory, Cluster for Pioneering Research, RIKEN, 2-1 Hirosawa, Wako, Saitama 351-0198, Japan


Since the interaction of single molecule of glycans is very weak to the lectins, in most cases they have been formed into clusters for binding studies. Then, a glycan molecule cannot be used for efficient cell imaging or targeting? We established a new strategy to selectively image the cells by using synergistic interaction of peptide and glycan ligands on cell surface. Namely, the peptide ligand with high affinity to the target surface receptor was pretargeted, and then the low-affinity glycan ligand with fluorescent label was interacted to the same cell; Bioorthogonal reaction between them can anchor the label on the target cells when both receptors are expressed and close in space on the surface. When the lectin is not expressed on the target or two receptors are separated, the weakly interacting glycan ligands are washed away the cells, hence the target cells are selectively imaged. While new idea and proof-of-concept data were exemplified based on our previous research, using this strategy, we would like to report the new data to visualize cell surface dynamics in response to the treatment with bioactive compounds.