Targeting protein kinases with selective and semipromiscuous covalent inhibitors

• Published in: Methods in enzymology Vol. 548; p. 93
• Main Authors: Miller, Rand M, Taunton, Jack
• Format: Journal Article
• Language: English
• Published: United States 2014
• Subjects: Animals; Biocatalysis - drug effects; Catalysis; Catalytic Domain; Drug Design; Humans; Lysine - chemistry; Models, Chemical; Protein Conformation; Protein Kinase Inhibitors - chemistry; Protein Kinase Inhibitors - pharmacology; Protein Kinases - chemistry; Protein Kinases - metabolism; Chemoproteomic; T. brucei; Cysteine; Hypothemycin; MSK; Covalent inhibitors; RSK; Kinase inhibitors

Protein kinase inhibitors are an important class of therapeutics. In addition, selective kinase inhibitors can often reveal unexpected biological insights, augmenting genetic approaches and playing a decisive role in preclinical target validation studies. Nevertheless, developing protein kinase inhi...