A high-throughput cell-based screening for L858R/T790M mutant epidermal growth factor receptor inhibitors

Wen Hsing Lin, Song Jen-Shin, Tzu Wen Lien, Chun Yu Chang, Szu Huei Wu, Yu Wen Huang, Teng Yuan Chang, Ming Yu Fang, Kuei Jung Yen, Chun Hwa Chen, Chang Ying Chu, Hsing Pang Hsieh, Yi Rong Chen, Yu Sheng Chao, John T.A. Hsu

研究成果: Article同行評審

3 引文 斯高帕斯(Scopus)

摘要

A high-throughput 32D(L858R/T790M) cell-based assay to identify inhibitors of the L858R/T790M mutant epidermal growth factor receptor (EGFR) pathway was established. After screening, ten hits from among 60,000 compounds in our in-house compound library were initially identified. In the secondary assays, one hit, 1-[2-(decyloxy)-2-oxoethyl]-3-methyl-2-[(4-methylphenoxy) methyl]-1H-benzimidazol-3-ium, was confirmed to directly inhibit the kinase activity of recombinant L858RIT790M EGFR and the phosphorylation of EGFR-L858R/T790M in gefitinib-resistant H1975 cells. Thus, this high-throughput assay system may be useful for identifying novel inhibitors which suppress mutant EGFR-T790M signalling and for overcoming T790M-mediated acquired resistance for future anticancer drug discovery.

原文English
頁(從 - 到)147-151
頁數5
期刊Anticancer research
32
發行號1
出版狀態Published - 2012 一月

All Science Journal Classification (ASJC) codes

  • 腫瘤科
  • 癌症研究

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