The DOI matches its Crossref record; 20 of the 20 references it cites were found in a registry or an index.
The Cysteinome of Protein Kinases as a Target in Drug Development
Abstract
Drugs that function through covalent bond formation represent a considerable fraction of our repository of effective medicines but safety concerns and the complexity of developing covalent inhibitors has rendered covalent targeting a less attractive strategy for rational drug design. The recent approval of four covalent kinase inhibitors and the development of highly potent covalent kinase probes with exceptional selectivity has raised significant interest in industry and academic research and validated the concept of covalent kinase targeting for clinical applications. The abundance of cysteines at diverse positions in and around the kinase active site suggests that a large fraction of kinases can be targeted by covalent inhibitors. Herein, we review recent developments of this rapidly growing area in kinase drug development and highlight the unique opportunities and challenges of this strategy.
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Cites
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Cited by
Kinase inhibitors: the road ahead
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Rapid Covalent-Probe Discovery by Electrophile-Fragment Screening
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Reactive-cysteine profiling for drug discovery
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Recent Advances in Selective and Irreversible Covalent Ligand Development and Validation
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Chemoproteomics and Chemical Probes for Target Discovery
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Self-citation
Metadata
- Authors
- Chaikuad, A., Koch, P., Laufer, S. A., & Knapp, S.
- Venue
- Angewandte Chemie International Edition
- Publisher
- Wiley
- Published
- 2018-02-02
- Volume
- 57
- Issue
- 16
- Pages
- 4372-4385
- ISSN
- 1433-7851 (ISSN-L)
- 1521-3773
- OpenAlex
- W2763970918
- Cited by
- 225
- References
- 20
- FWCI
- 8.51
- Type
- journal article
- Language
- en
- Open access
- closed
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