Abstract

The construction of targeted and activatable materials can largely improve the precision of disease diagnosis and therapy. However, the currently developed systems either target a transmembrane antigen or are activatable to release imaging and/or therapeutic reagents intracellularly. Here, we develop a simple thin-layer glycomaterial through the self-assembly between fluorescent glycoprobes, in which the carbohydrate-targeting reagent and the fluorophore are linked to each other by polyethylene glycol with a suitable chain length, and thin-layer manganese dioxide. The fluorogenic material developed is both capable of targeting a transmembrane glycoprotein receptor and fluorescently activatable by intracellular biothiols. The shell thickness of the material was determined to be important for achieving the biothiol-induced activation of fluorescence. This research might provide insight into the development of precision-enhanced self-assembled materials for disease theranostics.

Highlights

  • Carbohydrate–protein interactions are responsible for the activation of many biological and disease-relevant signaling pathways (Lee and Lee, 1995)

  • While previous studies mainly focused on the development of materials that can target a transmembrane antigen or are activatable for controlled release of imaging and therapeutic agents, here we develop a thin-layer glycomaterial for both targeted and activatable imaging of cells

  • We envision that while the material composite formed between DCM-Gal and thin-layer MnO2 might dissociate directly after interaction with the asialoglycoprotein receptor (ASGPr) that selectively recognizes galactoconjugates, that formed between DCMPEG6-Gal and thin-layer MnO2 could be more stable during receptor-mediated endocytosis for stimuli-activated fluorescence imaging (Figure 2B)

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Summary

Introduction

Carbohydrate–protein interactions are responsible for the activation of many biological and disease-relevant signaling pathways (Lee and Lee, 1995). The fluorogenic material developed is both capable of targeting a transmembrane glycoprotein receptor and fluorescently activatable by intracellular biothiols. Zang Y (2019) Self-Assembled Thin-Layer Glycomaterials With a Proper Shell Thickness for Targeted and Activatable Cell Imaging.

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