T790M mutation in EGFR kinase causes drug resistance by increasing the affinity for ATP

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...

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Veröffentlicht in:	Proceedings of the National Academy of Sciences - PNAS 2008-02, Vol.105 (6), p.2070-2075
Hauptverfasser:	Yun, Cai-Hong, Mengwasser, Kristen E, Toms, Angela V, Woo, Michele S, Greulich, Heidi, Wong, Kwok-Kin, Meyerson, Matthew, Eck, Michael J
Format:	Artikel
Sprache:	eng
Schlagworte:	Adenocarcinoma Adenosine triphosphatase Adenosine Triphosphate - metabolism AFFINITY Animals ATP AUGMENTATION BASIC BIOLOGICAL SCIENCES Biological Sciences Cell growth CHANNELING Crystal structure Crystallography, X-Ray Crystals Drug resistance Drug Resistance - genetics DRUGS Enzyme Inhibitors - pharmacology Enzymes ErbB Receptors - antagonists & inhibitors ErbB Receptors - chemistry ErbB Receptors - genetics ErbB Receptors - metabolism Gefitinib GENERAL AND MISCELLANEOUS//MATHEMATICS, COMPUTING, AND INFORMATION SCIENCE Genetic mutation Growth factor receptors GROWTH FACTORS Inhibitor drugs Insecta Kinases Kinetics Lung cancer Lung neoplasms LUNGS Molecular structure MOLECULES MUTANTS Mutation MUTATIONS NEOPLASMS PHOSPHOTRANSFERASES Protein Conformation Quinazolines - pharmacology RECEPTORS SPECIFICITY THREONINE TYROSINE
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