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

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

  • Medchemcomm. 2017 Aug 25;8(10):1914-1918. doi: 10.1039/c7md00305f.
Lian-Xiang Luo 1,  Ying Li 1,  Yu-Zhen Niu 2,  Yu-Wei Wang 1,  Qian-Qian Wang 1,  Xing-Xing Fan 1,  Jia-Hui Xu 1,  Liang Liu 1,  Elaine Lai-Han Leung 1,  Xiao-Jun Yao 1 2
Affiliations

Affiliations

  • 1 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: lliu@must.edu.mo ; Email: lhleung@must.edu.mo ; Email: xjyao@must.edu.mo ; ; Tel: +853 8897 2409.
  • 2 State Key Laboratory of Applied Organic Chemistry and Department of Chemistry , Lanzhou University , Lanzhou 730000 , China.
PMID: 30108712 DOI: 10.1039/c7md00305f
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.

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