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How Chemoproteomics Can Enable Drug Discovery and Development
Open accessAbstract
Creating first-in-class medications to treat human disease is an extremely challenging endeavor. While genome sequencing and genetics are making direct connections between mutations and human disorders at an unprecedented rate, matching molecular targets with a suitable therapeutic indication must ultimately be achieved by pharmacology. Here, we discuss how the integration of chemical proteomic platforms (such as activity-based protein profiling) into the earliest stages of the drug discovery process has the potential to greatly expand the scope of proteins that can be pharmacologically evaluated in living systems, and, through doing so, promote the identification and prioritization of new therapeutic targets.
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“In addition, some analytical techniques such as click chemistry, activity probes, and mass spectrometry-based proteomics to evaluate binding activity and selectivity in vitro and in vivo are only available for covalent compounds [120–124].”
From The design and development of covalent protein-protein interaction inhibitors for cancer treatment (2020) · cites this paper as [120]
In the citing paper
“This ‘electrophile-first’ approach is partly facilitated by the development of chemoproteomic platforms that enable rapid target identification and selectivity profiling of covalent ligands14–18.”
From Advances in covalent drug discovery (2022) · cites this paper as [17]
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Cites
1 retracted
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Cited by
Sorted by citations
Advances in covalent drug discovery
Boike, L., Henning, N. J., & Nomura, D. K. (2022) · Nature Reviews Drug Discovery · doi:10.1038/s41573-022-00542-z · Cited by 823
Targeted Covalent Inhibitors for Drug Design
Baillie, T. A. (2016) · Angewandte Chemie International Edition · doi:10.1002/anie.201601091 · Cited by 578
Sulfonyl fluorides as privileged warheads in chemical biology
Narayanan, A., & Jones, L. H. (2015) · Chemical Science · doi:10.1039/c5sc00408j · Cited by 557
Chemical proteomics approaches for identifying the cellular targets of natural products
Wright, M. H., & Sieber, S. A. (2016) · Natural Product Reports · doi:10.1039/c6np00001k · Cited by 400
Enzyme Inhibitor Discovery by Activity-Based Protein Profiling
Niphakis, M. J., & Cravatt, B. F. (2014) · Annual Review of Biochemistry · doi:10.1146/annurev-biochem-060713-035708 · Cited by 374
Self-citation
Metadata
- Authors
- Moellering, R. E., & Cravatt, B. F.
- Affiliations
- Scripps Research Institute (US)
- Corresponding author
- Cravatt, Benjamin F.
- Venue
- Chemistry & Biology
- Publisher
- Elsevier BV
- Published
- 2012-01
- Volume
- 19
- Issue
- 1
- Pages
- 11-22
- ISSN
- 1074-5521 (ISSN-L)
- PMC
- PMC3312051
- OpenAlex
- W2030953184
- Cited by
- 182
- References
- 96
- Citations by year
- 2026: 9 · 2025: 12 · 2024: 22 · 2023: 7 · 2022: 5 · 2021: 11 · 2020: 16 · 2019: 21 · 2018: 9 · 2017: 10 · 2016: 16 · 2015: 15 · 2014: 7 · 2013: 14 · 2012: 7
- FWCI
- 6.47
- Type
- journal article
- Language
- en
- Open access
- bronze
- doi.org
- Licence
- Locations
- Chemistry & Biology (publishedVersion)
- PubMed (publishedVersion)
- Europe PMC (PubMed Central) (acceptedVersion)
- PubMed Central (acceptedVersion)
- Funders
- Howard Hughes Medical Institute
- Cancer Research Institute
- Damon Runyon Cancer Research Foundation
- National Institutes of Health
- National Institute on Drug Abuse (DA025285, R01DA025285)
- National Cancer Institute (R01CA132630, CA-087660, R37CA087660, R01CA087660, CA132630)
- Topics
- Physical Sciences › Chemistry › Organic Chemistry › Click Chemistry and Applications
- Life Sciences › Pharmacology, Toxicology and Pharmaceutics › Drug Discovery › Computational Drug Discovery Methods
- Physical Sciences › Chemistry › Spectroscopy › Advanced Proteomics Techniques and Applications
- Keywords
- chemoproteomics, drug discovery, drug development, activity-based protein profiling, drug target identification, target prioritization, first-in-class drugs
- MeSH terms
- Enzymes, Humans, Serine Proteinase Inhibitors, Genome, Human, Proteomics, Metabolic Networks and Pathways, Small Molecule Libraries, Drug Discovery
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