TY - JOUR AU - Hillebrand, Laura AU - Gehringer, Matthias PY - 2022/05/25 Y2 - 2024/03/19 TI - Never Gonna Give You Up – Current Developments in Covalent Protein Kinase Inhibitors JF - CHIMIA JA - Chimia VL - 76 IS - 5 SE - Scientific Articles DO - 10.2533/chimia.2022.435 UR - https://www.chimia.ch/chimia/article/view/2022_435 SP - 435-447 AB - <p>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.</p> ER -