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Updated: May 30, 2026

Genetically-encoded Molecular Probes to Study G Protein-coupled Receptors

Genetically-encoded Molecular Probes to Study G Protein-coupled Receptors

Published on: September 13, 2013

Targeted pH-dependent fluorescent activity-based cathepsin probes.

Sascha Hoogendoorn¹, Kim L Habets, Solène Passemard

¹Leiden Institute of Chemistry, Leiden University, P.O. Box 9052, 2300 RA Leiden, The Netherlands.

Chemical Communications (Cambridge, England)

|July 20, 2011

Summary

This summary is machine-generated.

New pH-activatable BODIPY dyes in mannose-containing probes target cysteine proteases in dendritic cells. Acidic compartment trafficking triggers fluorescence and cathepsin inhibition, enabling live-cell imaging and drug development.

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Area of Science:

Biochemistry
Chemical Biology
Cell Biology

Background:

Cysteine proteases are crucial in cellular processes.
Targeting proteases in specific cellular compartments requires advanced probe design.
Dendritic cells express mannose receptors involved in cellular uptake.

Purpose of the Study:

To develop novel bifunctional, pH-activatable BODIPY dyes.
To create mannose cluster-containing activity-based probes for cysteine proteases.
To visualize and inhibit cysteine proteases in dendritic cells via receptor-mediated endocytosis.

Main Methods:

Synthesis of pH-activatable BODIPY dyes.
Conjugation of dyes to mannose cluster-based scaffolds.
Preparation of activity-based probes for cysteine proteases.
Live-cell imaging experiments in dendritic cells.
Assessment of cathepsin inhibition.

Main Results:

Successful development of bifunctional, pH-activatable BODIPY dyes.
Incorporation of dyes into mannose-decorated activity-based probes.
Demonstration of mannose receptor-dependent probe uptake in dendritic cells.
Localization of probes within acidic cellular compartments.
Induction of fluorescence upon acidification, enabling live-cell imaging.
Effective inhibition of cathepsin activity.

Conclusions:

The developed probes enable targeted delivery and visualization of cysteine protease activity in dendritic cells.
pH-activatable BODIPY dyes are effective reporters in acidic cellular environments.
These probes represent a promising tool for studying protease function and developing protease inhibitors.