How Chemoproteomics Can Enable Drug Discovery and Development
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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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Some analytical techniques (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.
“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]
Chemoproteomic platforms enable rapid target identification and selectivity profiling of covalent ligands.
“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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Yanagi, K., Komatsu, T., Ogihara, S., Okabe, T., Kojima, H., Nagano, T., Ueno, T., Hanaoka, K., & Urano, Y. (2021) · Cell Reports · doi:10.1016/j.celrep.2021.109311 · Cited by 13 · see citing works
The Age of Omics‐Driven Precision Medicine
McColl, E. R., Asthana, R., Paine, M. F., & Piquette‐Miller, M. (2019) · Clinical Pharmacology & Therapeutics · doi:10.1002/cpt.1532 · Cited by 13 · see citing works
Single-cell chemoproteomics identifies metastatic activity signatures in breast cancer
Pillai, K. S., Laxton, O. C., Li, G., Lin, J., Karginova, O. A., Nanda, R., Olopade, O. I., Tay, S., & Moellering, R. E. (2024) · Science Advances · doi:10.1126/sciadv.adp2622 · Cited by 12 · see citing works
Self-citationCompetitive ABPP of Serine Hydrolases: A Case Study on DAGL-Alpha
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Quantitative proteomics and applications in covalent ligand discovery
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Large-scale characterization of drug mechanism of action using proteome-wide thermal shift assays
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Interaction profiling methods to map protein and pathway targets of bioactive ligands
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Self-citationEmerging opportunities for intact and native protein analysis using chemical proteomics
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- 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
- Physical Sciences › Computer Science › Computational Theory and Mathematics › 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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