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Updated: May 1, 2026
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Genetically-encoded Molecular Probes to Study G Protein-coupled Receptors
Published on: September 13, 2013
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A perspective on cysteine-reactive activity-based probes
Constantin M Nuber1, Max A Schwab2,3, David B Konrad1,2,3
1Department of Pharmacy, Ludwig-Maximilians-Universität München, Butenandtstr. 5-13, 81377 Munich, Germany. david.konrad@cup.lmu.de.
Organic & Biomolecular Chemistry
|October 31, 2025
Summary
Activity-based protein profiling (ABPP) uses chemical probes to study protein function and drug mechanisms. This perspective reviews the design and application of covalent cysteine-targeted probes for mass spectrometry-based chemoproteomics.
Area of Science:
- Chemical Biology
- Proteomics
- Drug Discovery
Background:
- Activity-based protein profiling (ABPP) is a key chemical biology technique.
- It enables the investigation of protein function, target identification, and mechanism-of-action studies for chemical probes and drugs.
Purpose of the Study:
- To provide an overview of covalent cysteine-targeted activity-based probes (ABPs).
- To discuss the design, application, and future potential of ABPP in chemical biology and pharmaceutical research.
Main Methods:
- Overview of ABP design, including reactive elements (chemotypes/warheads) and functional handles.
- Description of mass spectrometry-based chemoproteomics analysis using ABPs.
- Strategies for developing advanced ABPs for live-cell applications and post-translational modification studies.
Main Results:
- Covalent cysteine-targeted ABPs are versatile tools for chemical proteomics.
- Advanced ABPs facilitate live-cell chemoproteomics and the study of post-translational modifications.
- ABPP holds significant potential for the pharmaceutical industry.
Conclusions:
- ABPP is a powerful approach for understanding protein function and drug mechanisms.
- The design and application of advanced ABPs are expanding the reach of chemoproteomics.
- Further development of ABPP has substantial implications for drug discovery and development.
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