Never Gonna Give You Up – Current Developments in Covalent Protein Kinase Inhibitors
DOI:
https://doi.org/10.2533/chimia.2022.435Keywords:
Covalent inhibitors, Cysteine targeting, Protein kinasesAbstract
Covalent inhibitors have recently seen a revival in medicinal chemistry. Inhibitors addressing non-catalytic cysteine residues with weakly reactive electrophiles have been very successfully employed to target protein kinases, one of the major druggable protein families. Here we provide an overview of irreversible and reversible covalent protein kinase inhibitors in clinical development and beyond. We further spotlight recent advances in targeting amino acids other than cysteine and the reactive groups utilized in covalent protein kinase inhibitors.
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Published
2022-05-25
How to Cite
[1]
L. Hillebrand, M. Gehringer, Chimia 2022, 76, 435, DOI: 10.2533/chimia.2022.435.
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Scientific Articles
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Copyright (c) 2022 Laura Hillebrand, Matthias Gehringer

This work is licensed under a Creative Commons Attribution 4.0 International License.