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Strategies for Competitive Activity-Based Protein Profiling in Small Molecule Inhibitor Discovery and
He Zhu1,2,3, Mona Sharafi1,4, Wei Pin Teh1,4
1Department of Cancer Biology and the Linde Program, in Cancer Chemical Biology, Dana-Farber Cancer Institute, Boston, MA, USA.
Activity-based protein profiling (ABPP) and its competitive variant (competitive ABPP) are powerful tools for studying enzyme activity. This review introduces competitive ABPP, highlighting its applications in chemical biology and drug discovery.
Area of Science:
- Chemical Biology
- Proteomics
- Drug Discovery
Background:
- Activity-based protein profiling (ABPP) has been a key technology since 1999.
- Competitive ABPP is a variation of ABPP used to study enzyme-target interactions.
- ABPP is utilized across academic, government, and industrial research settings.
Purpose of the Study:
- To review major developments in competitive ABPP.
- To provide an introduction to competitive ABPP for researchers.
- To highlight the utility of competitive ABPP in chemical biology and drug discovery.
Main Methods:
- Review of major developments in competitive ABPP.
- Compare-contrast format to introduce the technology.
- Discussion of creative adaptations of competitive ABPP.
Main Results:
- Competitive ABPP is a powerful approach for characterizing small molecule and drug binding.
- Adaptations of competitive ABPP enhance assay throughput and detection methods.
- Competitive ABPP supports hybrid target-based screening platforms.
Conclusions:
- Competitive ABPP is a flexible and enabling technology.
- The review serves as an introduction for scientists in chemical biology and drug discovery.
- Competitive ABPP has broad applications in understanding the functional proteome.
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