Article
Insight into resistance mechanism of anaplastic lymphoma kinase to alectinib and JH-VIII-157-02 caused by G1202R solvent front mutation.
Drug design, development and therapy - 1 Jan 2018
Wang Han, Wang Yao, Guo Wentao, Du Bin, Huang Xiaobing, Wu Riping, Yang Baoyu, Lin Xiaoyan, Wu Yilan
Abstract excerpt
BACKGROUND: Mutated anaplastic lymphoma kinase (ALK) drives the development of advanced non-small cell lung cancer (NSCLC). Most reported small-molecule inhibitors targeting the ALK domain do not display good inhibition of the G1202R solvent front mutation. The solvent front mutation was assumed to hinder drug binding. However, a different fact could be uncovered by the simulations reported in this study through...
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