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Updated: Jun 12, 2026
Deep Proteome Profiling by Isobaric Labeling, Extensive Liquid Chromatography, Mass Spectrometry, and Software-assisted Quantification
Published on: November 15, 2017
Recent advances in proteome-wide label-free target deconvolution for bioactive small molecules
Jichao Sun1,2, Nayana Prabhu3, Jun Tang1,4
1Department of Urology, Shenzhen People's Hospital (The Second Clinical Medical College, Jinan University; The First Affiliated Hospital, Southern University of Science and Technology), Shenzhen Urology Minimally Invasive Engineering Center, Shenzhen, Guangdong, China.
Label-free chemical proteomics methods systematically identify drug targets. These techniques are crucial for understanding drug mechanisms and developing more effective therapeutics.
Area of Science:
- Chemical proteomics
- Drug discovery
- Molecular pharmacology
Background:
- Small-molecule drugs interact with target proteins to modulate biological processes.
- Understanding drug-target engagement is vital for elucidating drug mechanisms and side effects.
- Systematic assessment of drug-target engagement has historically been challenging.
Purpose of the Study:
- To provide an overview of label-free chemical proteomics approaches for drug target deconvolution.
- To discuss the principles and applications of various label-free methods.
- To explore the technical implications and future outlook of these techniques.
Main Methods:
- Overview of label-free chemical proteomics techniques.
- Discussion of methods including cellular thermal shift assay, pulse proteolysis, and drug affinity responsive target stability.
- Exploration of chemical denaturant and protein precipitation methods.
Main Results:
- Label-free approaches offer a non-intrusive way to identify drug targets.
- Various methods like CETSA, limited proteolysis, and protein precipitation are effective.
- These techniques are advancing the field of drug target deconvolution.
Conclusions:
- Label-free chemical proteomics methods are essential for drug discovery and development.
- Continued advancements in mass spectrometry are enhancing these techniques.
- Future outlook suggests broader applications in understanding drug action.
