The DOI matches its Crossref record; 8 of the 8 references it cites were found in a registry or an index.
Lysine‐Targeting Covalent Inhibitors
Abstract
Targeted covalent inhibitors have gained widespread attention in drug discovery as a validated method to circumvent acquired resistance in oncology. This strategy exploits small‐molecule/protein crystal structures to design tightly binding ligands with appropriately positioned electrophilic warheads. Whilst most focus has been on targeting binding‐site cysteine residues, targeting nucleophilic lysine residues can also represent a viable approach to irreversible inhibition. However, owing to the basicity of the ϵ ‐amino group in lysine, this strategy generates a number of specific challenges. Herein, we review the key principles for inhibitor design, give historical examples, and present recent developments that demonstrate the potential of lysine targeting for future drug discovery.
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Cites
The resurgence of covalent drugs
Singh, J., Petter, R. C., Baillie, T. A., & Whitty, A. (2011) · Nature Reviews Drug Discovery · doi:10.1038/nrd3410 · Cited by 1,873
Finlay, M. R. V., Anderton, M., Ashton, S., Ballard, P., Bethel, P. A., Box, M. R., Bradbury, R. H., Brown, S. J., Butterworth, S., Campbell, A., et al. (2014) · Journal of Medicinal Chemistry · doi:10.1021/jm500973a · Cited by 636
Targeted Covalent Inhibitors for Drug Design
Baillie, T. A. (2016) · Angewandte Chemie International Edition · doi:10.1002/anie.201601091 · Cited by 578
Bauer, R. A. (2015) · Drug Discovery Today · doi:10.1016/j.drudis.2015.05.005 · Cited by 534
Zhao, Y., Aguilar, A., Bernard, D., & Wang, S. (2015) · Journal of Medicinal Chemistry · doi:10.1021/jm501092z · Cited by 462
Broad-Spectrum Kinase Profiling in Live Cells with Lysine-Targeted Sulfonyl Fluoride Probes
Zhao, Q., Ouyang, X., Wan, X., Gajiwala, K. S., Kath, J. C., Jones, L. H., Burlingame, A. L., & Taunton, J. (2017) · Journal of the American Chemical Society · doi:10.1021/jacs.6b08536 · Cited by 388
Strategies for Discovering and Derisking Covalent, Irreversible Enzyme Inhibitors
Johnson, D. S., Weerapana, E., & Cravatt, B. F. (2010) · Future Medicinal Chemistry · doi:10.4155/fmc.10.21 · Cited by 387
Introduction: historical perspective and development of amoxicillin/clavulanate
Geddes, A. M., Klugman, K. P., & Rolinson, G. N. (2007) · International Journal of Antimicrobial Agents · doi:10.1016/j.ijantimicag.2007.07.015 · Cited by 96
Cited by
Ertl, P., Altmann, E., & McKenna, J. M. (2020) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.0c00754 · Cited by 429
Structure-based design of targeted covalent inhibitors
Lonsdale, R., & Ward, R. A. (2018) · Chemical Society Reviews · doi:10.1039/c7cs00220c · Cited by 344
Advances in covalent kinase inhibitors
Abdeldayem, A., Raouf, Y. S., Constantinescu, S. N., Moriggl, R., & Gunning, P. T. (2020) · Chemical Society Reviews · doi:10.1039/c9cs00720b · Cited by 317
Tamura, T., Ueda, T., Goto, T., Tsukidate, T., Shapira, Y., Nishikawa, Y., Fujisawa, A., & Hamachi, I. (2018) · Nature Communications · doi:10.1038/s41467-018-04343-0 · Cited by 242
Recent Advances in Selective and Irreversible Covalent Ligand Development and Validation
Zhang, T., Hatcher, J. M., Teng, M., Gray, N. S., & Kostic, M. (2019) · Cell Chemical Biology · doi:10.1016/j.chembiol.2019.09.012 · Cited by 178
Metadata
- Authors
- Pettinger, J., Jones, K., & Cheeseman, M. D.
- Venue
- Angewandte Chemie International Edition
- Publisher
- Wiley
- Published
- 2017-10-27
- Volume
- 56
- Issue
- 48
- Pages
- 15200-15209
- ISSN
- 1433-7851 (ISSN-L)
- 1521-3773
- OpenAlex
- W2752520345
- Cited by
- 236
- References
- 8
- FWCI
- 6.30
- Type
- journal article
- Language
- en
- Open access
- closed
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Contains information from the Semantic Scholar Academic Graph Datasets, made available under the ODC Attribution License (ODC-BY 1.0).
Semantic Scholar’s data is described in: Kinney, R., et al. (2023). The Semantic Scholar Open Data Platform. arXiv:2301.10140.
