The DOI matches its Crossref record; 233 of the 233 references it cites were found in a registry or an index.
Enzyme Inhibitor Discovery by Activity-Based Protein Profiling
Open accessAbstract
Eukaryotic and prokaryotic organisms possess huge numbers of uncharacterized enzymes. Selective inhibitors offer powerful probes for assigning functions to enzymes in native biological systems. Here, we discuss how the chemical proteomic platform activity-based protein profiling (ABPP) can be implemented to discover selective and in vivo–active inhibitors for enzymes. We further describe how these inhibitors have been used to delineate the biochemical and cellular functions of enzymes, leading to the discovery of metabolic and signaling pathways that make important contributions to human physiology and disease. These studies demonstrate the value of selective chemical probes as drivers of biological inquiry.
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Cites
1 retracted
Selective killing of cancer cells by a small molecule targeting the stress response to ROS
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Mutations in LRRK2 Cause Autosomal-Dominant Parkinsonism with Pleomorphic Pathology
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Cited by
Kinase inhibitors: the road ahead
Ferguson, F. M., & Gray, N. S. (2018) · Nature Reviews Drug Discovery · doi:10.1038/nrd.2018.21 · Cited by 1,009
Click Chemistry in Proteomic Investigations
Parker, C. G., & Pratt, M. R. (2020) · Cell · doi:10.1016/j.cell.2020.01.025 · Cited by 380
The emerging role of mass spectrometry-based proteomics in drug discovery
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Activity-based protein profiling reveals off-target proteins of the FAAH inhibitor BIA 10-2474
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Self-citationCovalent inhibitors design and discovery.
De Cesco, S., Kurian, J., Dufresne, C., Mittermaier, A. K., & Moitessier, N. (2017) · European Journal of Medicinal Chemistry · doi:10.1016/j.ejmech.2017.06.019 · Cited by 315
Metadata
- Authors
- Niphakis, M. J., & Cravatt, B. F.
- Venue
- Annual Review of Biochemistry
- Publisher
- Annual Reviews
- Published
- 2014-06-02
- Volume
- 83
- Issue
- 1
- Pages
- 341-377
- ISSN
- 0066-4154 (ISSN-L)
- 1545-4509
- OpenAlex
- W2111385909
- Cited by
- 366
- References
- 233
- FWCI
- 1.04
- Type
- journal article
- Language
- en
- Open access
- bronze
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- Niphakis, M. J., & Cravatt, B. F. (2014). Enzyme Inhibitor Discovery by Activity-Based Protein Profiling. Annual Review of Biochemistry. https://doi.org/10.1146/annurev-biochem-060713-035708
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