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Never Gonna Give You Up – Current Developments in Covalent Protein Kinase Inhibitors

2022; Swiss Chemical Society; Volume: 76; Issue: 5 Linguagem: Inglês

10.2533/chimia.2022.435

2673-2424

Laura Hillebrand, Matthias Gehringer,

Peptidase Inhibition and Analysis

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.