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

**Authors:** Chen Guo, Fang-Yu Si, Chen-Han Wang, Ning Wang, Xi-Le Hu, Tony D. James, Jia Li, Chengyun Wang, Xiao-Peng He

PMC · DOI: 10.1039/d4sc08472a · Chemical Science · 2025-05-27

## TL;DR

This paper introduces a fluorescent tool to study how a liver cancer cell receptor interacts with sugar-based molecules in real time.

## Contribution

A new fluorescent trivalent galactoside probe for super-resolution imaging of ASGPr dynamics in live cells.

## Key findings

- The BODIPY-tagged galactocluster effectively targets ASGPr-overexpressing liver cancer cells.
- The probe enables super-resolution imaging of ASGPr-mediated endocytosis and lysosomal translocation.
- The tool provides insights into the dynamic interactions of glycoclusters with cell receptors.

## 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.

We synthesized a trivalent galactosyl BODIPY probe for the super-resolution (STED) imaging of the dynamic endocytic action of asialoglycoprotein receptor (ASGPr).

## Linked entities

- **Proteins:** ASGR1 (asialoglycoprotein receptor 1)
- **Chemicals:** BODIPY (PubChem CID 25058173), boron dipyrromethene (PubChem CID 25058173)
- **Diseases:** liver cancer (MONDO:0002691)

## Full-text entities

- **Genes:** ASGR1 (asialoglycoprotein receptor 1) [NCBI Gene 432] {aka ASGPR, ASGPR1, CLEC4H1, HL-1}
- **Diseases:** liver cancer (MESH:D006528)
- **Chemicals:** galactoside (MESH:D005697), boron dipyrromethene (-), BODIPY (MESH:C095489)

## Full text

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## Figures

5 figures with captions in the complete paper: https://tomesphere.com/paper/PMC12109605/full.md

## References

39 references — full list in the complete paper: https://tomesphere.com/paper/PMC12109605/full.md

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Source: https://tomesphere.com/paper/PMC12109605