Transmembrane receptors that can recognize sugars are pervaded on the surface of cells, which, by selective interaction with sugars, can cause a number of pathological events. Therefore, the design and synthesis of glycoside derivatives with high affinity with the receptors may facilitate the development of systems suited for drug delivery and disease diagnosis.

On the basis of previous work as regards the detection of sugar-receptor interactions on the cellular level, researchers from Shanghai Institute of Materia Medica, CAS, and East China University of Science and Technology prepared aminoxy-peptide-based dimeric and tetrameric glycopeptidomimetics. These compounds have potentially good serum stability as they are resistant to trypsin cleavage, and showed low cytotoxicity. Additionally, by using a previously developed glycodye, the antagonist effect between the asialoglycoprotein receptors and the multivalent glycopeptides were monitored by fluorescence microscope. This research offers insights into the direct fluorescence imaging of interactions between transmembrane receptors and their pairing ligands, and also provides new scaffolds for the development of sugar-based vaccines.