Article
Discovery and characterization of a novel irreversible EGFR mutants selective and potent kinase inhibitor CHMFL-EGFR-26 with a distinct binding mode.
Oncotarget - 14 Mar 2017
Hu Chen, Wang Aoli, Wu Hong, Qi Ziping, Li Xixiang, Yan Xiao-E, Chen Cheng, Yu Kailin, Zou Fengming, Wang Wenchao, Wang Wei, Wu Jiaxin, Liu Juan, Wang Beilei, Wang Li, Ren Tao, Zhang Shanchun, Yun Cai-Hong, Liu Jing, Liu Qingsong
Abstract excerpt
EGFR T790M mutation accounts for about 40-55% drug resistance for the first generation EGFR kinase inhibitors in the NSCLC. Starting from ibrutinib, a highly potent irreversible BTK kinase inhibitor, which was also found to be moderately active to EGFR T790M mutant, we discovered a highly potent irreversible EGFR inhibitor CHMFL-EGFR-26, which is selectively potent against EGFR mutants including L858R, del19, and...
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