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Updated: Dec 28, 2025

Chemoselective Modification of Viral Surfaces via Bioorthogonal Click Chemistry
Published on: August 19, 2012
Targeting infected host cells in vivo via responsive azido-sugar mediated metabolic cell labeling followed by click
Yang Bo1, Yunjiang Jiang1, Kangmei Chen2
1Department of Materials Science and Engineering, University of Illinois at Urbana-Champaign, Urbana, IL, 61801, United States.
Abstract:
The early in vivo diagnosis of infectious disease foci is largely hindered by invasion and concealment of pathogens in host cells, making it difficult for conventional probes to detect and analyze intracellular pathogens. Taking advantage of the excessively produced reactive oxygen species (ROS) within host cells, herein we report the design of thiol-hemiketal blocked N-azidoacetyl galactosamine (Ac3GalNAzSP), an azido unnatural sugar bearing an unprecedent designed ROS-responsive moiety for targeted labelling of infected host cells. Ac3GalNAzSP showed great stability under physiological conditions, specifically released active unnatural sugar in host cells overproducing ROS, metabolically labeled infected host cells with azido groups, and enabled targeting in vivo infection sites by subsequent Click Chemistry reactions, substantiating an unprecedented approach for targeting infected host cells. This technique could be a powerful tool for early in vivo diagnosis and targeted treatment of infectious disease.
Insights
Researchers developed a novel ROS-responsive unnatural sugar probe for early in vivo diagnosis of infectious diseases. This method targets intracellular pathogens by labeling infected host cells, enabling precise detection and treatment.
Area of Science:
- Biomedical Engineering
- Infectious Disease Diagnostics
- Molecular Imaging
Background:
- Early diagnosis of intracellular infectious disease foci is challenging due to pathogen concealment within host cells.
- Conventional probes struggle to detect and analyze pathogens residing inside host cells.
Purpose of the Study:
- To develop a novel probe for targeted labeling of infected host cells.
- To enable early in vivo diagnosis and treatment of infectious diseases.
Main Methods:
- Design and synthesis of a ROS-responsive unnatural sugar probe (Ac3GalNAzSP).
- Utilizing reactive oxygen species (ROS) overproduction in infected cells to trigger probe activation.
- Metabolic labeling of infected host cells with azido groups.
- Employing Click Chemistry for in vivo targeting of infection sites.
Main Results:
- Ac3GalNAzSP demonstrated stability under physiological conditions.
- The probe specifically released active unnatural sugar in ROS-overproducing host cells.
- Infected host cells were successfully labeled with azido groups.
- In vivo infection sites were targeted using Click Chemistry.
Conclusions:
- The developed probe offers an unprecedented approach for targeting infected host cells.
- This technique facilitates early in vivo diagnosis of infectious diseases.
- The method holds potential for targeted treatment strategies.
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