Article
Ibrutinib selectively and irreversibly targets EGFR (L858R, Del19) mutant but is moderately resistant to EGFR (T790M) mutant NSCLC Cells.
Oncotarget - 13 Oct 2015
Wu Hong, Wang Aoli, Zhang Wei, Wang Beilei, Chen Cheng, Wang Wenchao, Hu Chen, Ye Zi, Zhao Zheng, Wang Li, Li Xixiang, Yu Kailin, Liu Juan, Wu Jiaxin, Yan Xiao-E, Zhao Peng, Wang Jinhua, Wang Chu, Weisberg Ellen L, Gray Nathanael S, Yun Cai-Hong, Liu Jing, Chen Liang, Liu Qingsong
Abstract excerpt
Through comprehensive comparison study, we found that ibrutinib, a clinically approved covalent BTK kinase inhibitor, was highly active against EGFR (L858R, del19) mutant driven NSCLC cells, but moderately active to the T790M 'gatekeeper' mutant cells and not active to wild-type EGFR NSCLC cells. Ibrutinib strongly affected EGFR mediated signaling pathways and induced apoptosis and cell cycle arrest (G0/G1) in...
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