Activity-Based Protein Profiling: From Enzyme Chemistry to Proteomic Chemistry
Abstract
Genome sequencing projects have provided researchers with a complete inventory of the predicted proteins produced by eukaryotic and prokaryotic organisms. Assignment of functions to these proteins represents one of the principal challenges for the field of proteomics. Activity-based protein profiling (ABPP) has emerged as a powerful chemical proteomic strategy to characterize enzyme function directly in native biological systems on a global scale. Here, we review the basic technology of ABPP, the enzyme classes addressable by this method, and the biological discoveries attributable to its application.
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ABPP was pioneered by Cravatt and Bogyo using active-site-directed chemical probes that covalently target catalytic residues of hydrolases, proteases, and kinases.
“ABPP was pioneered by Cravatt and Bogyo using active-site-directed chemical probes that covalently target catalytic residues of various enzyme classes, including hydrolases, proteases and kinases173,174.”
From Advances in covalent drug discovery (2022) · cites this paper as [173]
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Self-citationDensity Functional Study of the Mechanism of a Tyrosine Phosphatase: I. Intermediate Formation
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Cysteine cathepsins: From structure, function and regulation to new frontiers
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What Is Microbial Community Ecology?
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Activity-Based Profiling of Proteases
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DAGLβ inhibition perturbs a lipid network involved in macrophage inflammatory responses
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How Chemoproteomics Can Enable Drug Discovery and Development
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Ipomoeassin F Binds Sec61α to Inhibit Protein Translocation
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Chemoproteomic profiling and discovery of protein electrophiles in human cells
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IFITM proteins assist cellular uptake of diverse linked chemotypes
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Discovery of Potent and Selective Inhibitors against Protein-Derived Electrophilic Cofactors
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Multidimensional profiling in the investigation of small-molecule-induced cell death
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- Authors
- Cravatt, B. F., Wright, A. T., & Kozarich, J. W.
- Affiliations
- Scripps Research Institute (US)
- Activx Biosciences, La Jolla, California 92037;
- Venue
- Annual Review of Biochemistry
- Publisher
- Annual Reviews
- Published
- 2008-06-01
- Volume
- 77
- Issue
- 1
- Pages
- 383-414
- ISSN
- 0066-4154 (ISSN-L)
- 1545-4509
- OpenAlex
- W2149554987
- Cited by
- 1,270
- References
- 155
- Citations by year
- 2026: 64 · 2025: 71 · 2024: 75 · 2023: 79 · 2022: 82 · 2021: 78 · 2020: 84 · 2019: 82 · 2018: 66 · 2017: 62 · 2016: 68 · 2015: 65 · 2014: 67 · 2013: 66 · 2012: 73
- FWCI
- 5.21
- Type
- journal article
- Language
- en
- Open access
- closed
- Locations
- Annual Review of Biochemistry (publishedVersion)
- PubMed (publishedVersion)
- Funders
- National Institute on Drug Abuse (DA-017259, P01DA017259)
- National Cancer Institute (R33CA118696, CA-087660, CA118696, R01CA087660)
- Topics
- Physical Sciences › Chemistry › Spectroscopy › Advanced Proteomics Techniques and Applications
- Physical Sciences › Chemistry › Organic Chemistry › Click Chemistry and Applications
- Life Sciences › Biochemistry, Genetics and Molecular Biology › Molecular Biology › Advanced Biosensing Techniques and Applications
- Keywords
- activity-based protein profiling, chemoproteomics, enzyme function, enzyme classes, protein annotation
- MeSH terms
- Adenosine Triphosphate, Animals, Biochemistry, Chromatography, Liquid, Cysteine Endopeptidases, Humans, Hydrolases, Models, Biological, Models, Chemical, Proteins, Mass Spectrometry, Genome, Proteome, Proteomics
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