Natural Product-Derived Activity-Based and Affinity-Based Probes: Tools for Mechanism of Action Studies
Zhiming Shi1, Hui Sun1, Yi Jin2
1State Key Laboratory of Natural Medicines, China Pharmaceutical University, Nanjing 211198, China.
Molecules (Basel, Switzerland)
|April 14, 2026
Summary
Labeled natural product probes accelerate drug discovery by enabling efficient target identification and mechanism elucidation. Advanced mass spectrometry and Activity-Based Protein Profiling (ABPP) are key to this progress.
Area of Science:
- Chemical Biology
- Drug Discovery
- Natural Products
Background:
- Natural products are crucial for drug discovery, but mechanistic studies are challenging.
- Traditional methods for target identification are often inefficient and lack sensitivity.
Purpose of the Study:
- To review the applications of labeled natural product probes in drug discovery.
- To provide insights into developing novel probes for chemical biology and drug discovery.
Main Methods:
- Activity-Based Protein Profiling (ABPP) strategies.
- Advanced mass spectrometry techniques.
- Development of labeled probes derived from natural products.
Main Results:
- Labeled probes facilitate efficient target identification and visualization.
- Recent applications of labeled probes across various natural product classes are reviewed.
- Novel photoaffinity groups with improved characteristics are proposed.
Conclusions:
- Labeled natural product probes significantly advance the understanding of mechanisms of action.
- Future probe development should prioritize small size, strong binding affinity, and stability.
- These advancements will expand applications in chemical biology and drug discovery.
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