Article
Ibrutinib targets mutant-EGFR kinase with a distinct binding conformation.
Oncotarget - 25 Oct 2016
Wang Aoli, Yan Xiao-E, Wu Hong, Wang Wenchao, Hu Chen, Chen Cheng, Zhao Zheng, Zhao Peng, Li Xixiang, Wang Li, Wang Beilei, Ye Zi, Wang Jinhua, Wang Chu, Zhang Wei, Gray Nathanael S, Weisberg Ellen L, Chen Liang, Liu Jing, Yun Cai-Hong, Liu Qingsong
Abstract excerpt
Ibrutinib, a clinically approved irreversible BTK kinase inhibitor for Mantle Cell Lymphoma (MCL) and Chronic Lymphocytic Leukemia (CLL) etc, has been reported to be potent against EGFR mutant kinase and currently being evaluated in clinic for Non Small Cell Lung Cancer (NSCLC). Through EGFR wt/mutant engineered isogenic BaF3 cell lines we confirmed the irreversible binding mode of Ibrutinib with EGFR wt/mutant...
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