在非小细胞肺癌中鉴定一种靶向EML4-ALK融合蛋白的强效激酶抑制剂。
Identification of a potent kinase inhibitor targeting EML4-ALK fusion protein in non-small cell lung cancer.
作者信息
Luo Lian-Xiang, Li Ying, Niu Yu-Zhen, Wang Yu-Wei, Wang Qian-Qian, Fan Xing-Xing, Xu Jia-Hui, Liu Liang, Leung Elaine Lai-Han, Yao Xiao-Jun
机构信息
State Key Laboratory of Quality Research in Chinese Medicine/Macau Institute For Applied Research in Medicine and Health , Macau University of Science and Technology , Macau SAR , China . Email:
State Key Laboratory of Applied Organic Chemistry and Department of Chemistry , Lanzhou University , Lanzhou 730000 , China.
出版信息
Medchemcomm. 2017 Aug 25;8(10):1914-1918. doi: 10.1039/c7md00305f. eCollection 2017 Oct 1.
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.
摘要
ALK融合蛋白在约5%的非小细胞肺癌发生发展中起重要作用。在此，我们鉴定出化合物5067 - 0952为一种有效的ALK抑制剂，它可抑制细胞生长、诱导细胞凋亡，并抑制ALK的磷酸化，进而阻断其下游信号通路。
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