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Identification of a potent kinase inhibitor targeting EML4-ALK fusion protein in non-small cell lung cancer.


ABSTRACT: ALK-fusion proteins play a fundamental role in the development of about 5% of non-small cell lung cancers. Herein, we identified the compound 5067-0952 as a potent ALK inhibitor, which inhibited cell growth, induced apoptosis, and suppressed the phosphorylation of ALK, subsequently blocking its downstream signaling pathway.

SUBMITTER: Luo LX 

PROVIDER: S-EPMC6071718 | biostudies-literature | 2017 Oct

REPOSITORIES: biostudies-literature

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Identification of a potent kinase inhibitor targeting EML4-ALK fusion protein in non-small cell lung cancer.

Luo Lian-Xiang LX   Li Ying Y   Niu Yu-Zhen YZ   Wang Yu-Wei YW   Wang Qian-Qian QQ   Fan Xing-Xing XX   Xu Jia-Hui JH   Liu Liang L   Leung Elaine Lai-Han EL   Yao Xiao-Jun XJ  

MedChemComm 20170825 10


ALK-fusion proteins play a fundamental role in the development of about 5% of non-small cell lung cancers. Herein, we identified the compound 5067-0952 as a potent ALK inhibitor, which inhibited cell growth, induced apoptosis, and suppressed the phosphorylation of ALK, subsequently blocking its downstream signaling pathway. ...[more]

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