Article
L1198F Mutation Resensitizes Crizotinib to ALK by Altering the Conformation of Inhibitor and ATP Binding Sites.
International journal of molecular sciences - 24 Feb 2017
Li Jian, Sun Rong, Wu Yuehong, Song Mingzhu, Li Jia, Yang Qianye, Chen Xiaoyi, Bao Jinku, Zhao Qi
Abstract excerpt
The efficacy of anaplastic lymphoma kinase (ALK) positive non-small-cell lung cancer (NSCLC) treatment with small molecule inhibitors is greatly challenged by acquired resistance. A recent study reported the newest generation inhibitor resistant mutation L1198F led to the resensitization to crizotinib, which is the first Food and Drug Administration (FDA) approved drug for the treatment of ALK-positive NSCLC. It...
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