Article
Characterization of irreversible kinase inhibitors by directly detecting covalent bond formation: a tool for dissecting kinase drug resistance.
Chembiochem : a European journal of chemical biology - 10 Dec 2010
Klüter Sabine, Simard Jeffrey R, Rode Haridas B, Grütter Christian, Pawar Vijaykumar, Raaijmakers Hans C A, Barf Tjeerd A, Rabiller Matthias, van Otterlo Willem A L, Rauh Daniel
Abstract excerpt
Targeting protein kinases in cancer therapy with irreversible small-molecule inhibitors is moving to the forefront of kinase-inhibitor research and is thought to be an effective means of overcoming mutation-associated drug resistance in epidermal growth factor receptor kinase (EGFR). We generated a detection technique that allows direct measurements of covalent bond formation without relying on kinase activity,...
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