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Published on: March 22, 2012
A BODIPY-tagged trivalent glycocluster for receptor-targeting fluorescence imaging of live cells
Chen Guo1,2, Fang-Yu Si1, Chen-Han Wang1,3
1Key Laboratory for Advanced Materials and Joint International Research Laboratory of Precision Chemistry and Molecular Engineering, Feringa Nobel Prize Scientist Joint, Research Center, School of Chemistry and Molecular Engineering, East China University of Science and Technology 130 Meilong Rd Shanghai 200237 China xphe@ecust.edu.cn cywang@ecust.edu.cn.
Abstract:
Multivalent glycoclusters have been extensively used as a targeting agent for drug delivery. However, tools capable of investigating their dynamic interactions with a target receptor remain elusive. Here, we synthesized fluorescently-tagged galactoclusters for the fluorescence imaging of cells that overly express the asialoglycoprotein receptor (ASGPr). A trivalent galactoside was synthesized, to which a boron dipyrromethene (BODIPY) dye was conjugated. The resulting fluorescent glycocluster was used for the targeted fluorescence imaging of liver cancer cells with a high ASGPr expression level. The trivalent probe was also demonstrated to be applicable for super-resolution imaging of ASGPr-mediated ligand endocytosis and the dynamic intracellular translocation to the lysosomes. As such, this study provides a suitable chemical tool for the study of receptor dynamics using fluorescently tagged glycoclusters.
