Identification of a potent kinase inhibitor targeting EML4-ALK fusion protein in non-small cell lung cancer. Issue 10 (12th September 2017)

• Record Type: Journal Article
• Authors: 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
• Is Part Of: MedChemComm. Volume 8:Issue 10(2017)
• Page Start: 1914
• Page End: 1918
• Publication Date: 2017-09-12
• Subjects: Pharmaceutical chemistry -- Periodicals; 615.19
• DOI: 10.1039/c7md00305f
• Languages: English
• ISSNs: 2040-2503

Abstract

Abstract : Herein, we reported 5067-0952, a potent ALK inhibitor with pharmacological efficacy in non-small cell lung cancers harboring the ALK fusion oncogene. 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.