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Updated: Sep 13, 2025
Biosensor-based High Throughput Biopanning and Bioinformatics Analysis Strategy for the Global Validation of Drug-protein Interactions
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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.
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Since its introduction by Cravatt and colleagues in 1999, activity-based protein profiling (ABPP) has become widely utilized throughout academia, government, and industry laboratories to study enzymes spanning numerous gene families in a multitude of biological systems. As a variation of ABPP, competitive ABPP provides a powerful approach to characterize the binding behavior of small molecule probes and clinical drugs throughout the functional proteome. The power and flexibility of competitive ABPP are exemplified by a wide range of creative adaptions which increase assay throughput, enable diverse detection schemes, and support the implementation of this approach within a hybrid target-based screening platform. We review major developments in competitive ABPP through a compare-contrast format to provide a useful introduction to this enabling technology for scientists in chemical biology and drug discovery.
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