Article
The T790M mutation in EGFR kinase causes drug resistance by increasing the affinity for ATP.
Proceedings of the National Academy of Sciences of the United States of America - 12 Feb 2008
Yun Cai-Hong, Mengwasser Kristen E, Toms Angela V, Woo Michele S, Greulich Heidi, Wong Kwok-Kin, Meyerson Matthew, Eck Michael J
Abstract excerpt
Lung cancers caused by activating mutations in the epidermal growth factor receptor (EGFR) are initially responsive to small molecule tyrosine kinase inhibitors (TKIs), but the efficacy of these agents is often limited because of the emergence of drug resistance conferred by a second mutation, T790M. Threonine 790 is the "gatekeeper" residue, an important determinant of inhibitor specificity in the ATP binding...
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