Identification of a potent kinase inhibitor targeting EML4-ALK fusion protein in non-small cell lung cancer,RSC Medicinal Chemistry

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Identification of a potent kinase inhibitor targeting EML4-ALK fusion protein in non-small cell lung cancer
RSC Medicinal Chemistry ( IF 4.1 ) Pub Date : 2017-08-25 00:00:00 , DOI: 10.1039/c7md00305f
Lian-Xiang Luo _{1,

2,

3,

4} , Ying Li _{1,

2,

3,

4} , Yu-Zhen Niu _{4,

5,

6,

7} , Yu-Wei Wang _{1,

2,

3,

4} , Qian-Qian Wang _{1,

2,

3,

4} , Xing-Xing Fan _{1,

2,

3,

4} , Jia-Hui Xu _{1,

2,

3,

4} , Liang Liu _{1,

2,

3,

4} , Elaine Lai-Han Leung _{1,

2,

3,

4} , Xiao-Jun Yao _{1,

2,

3,

4,

5}

Affiliation

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.

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