A BODIPY-tagged trivalent glycocluster for receptor-targeting fluorescence imaging of live cells

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.

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Publication Details

Journal
Chemical Science
Published
2025-01-01
DOI
https://doi.org/10.1039/d4sc08472a
Primary Topic
Advanced Fluorescence Microscopy Techniques
Type
article
Field-Weighted Citation Impact
0.00

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article

A BODIPY-tagged trivalent glycocluster for receptor-targeting fluorescence imaging of live cells

Chengyun Wang, Xiao‐Peng He, Fang-Yu Si, Tony D. James et al.
Chemical Science
Advanced Fluorescence Microscopy Techniques
article

A BODIPY-tagged trivalent glycocluster for receptor-targeting fluorescence imaging of live cells

Chengyun Wang, Xiao‐Peng He, Fang-Yu Si, Tony D. James, Chen-Han Wang, Ning Wang, Chen Guo, Jia Li, Xi-Le Hu
article en

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.

Chemical ScienceVol. 16(25)
East China University of Science and Technology (CN), Second Military Medical University (CN), Shanghai Institute of Materia Medica (CN), National Center for Drug Screening (CN), Eastern Hepatobiliary Surgery Hospital (CN), University of Bath (GB), Henan Normal University (CN)
Henan Normal University, University of Bath, National Natural Science Foundation of China, Dalian University of Technology, Science and Technology Commission of Shanghai Municipality, Hunan University, State Key Laboratory of Chemo/Biosensing and Chemometrics, Fundamental Research Funds for the Central Universities
Openalex Percentile: Top 91%
Advanced Fluorescence Microscopy Techniques
DOIOpen Access PDFOpenAlex
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