A cell-based high-throughput screen for epidermal growth factor receptor pathway inhibitors

Wen Hsing Lin, Jen Shin Song, Teng Yuan Chang, Chun Yu Chang, Yu Ning Fu, Chi Ling Yeh, Szu Huei Wu, Yu Wen Huang, Ming Yu Fang, Tzu Wen Lien, Hsing Pang Hsieh, Yu Sheng Chao, Shiu Feng Huang, Shih Feng Tsai, Lin Mei Wang, John T.A. Hsu, Yi Rong Chen

Research output: Contribution to journalArticlepeer-review

11 Citations (Scopus)


Epidermal growth factor receptor (EGFR) is a valid drug target for development of target-based therapeutics against non-small-cell lung cancer. In this study, we established a high-throughput cell-based assay to screen for compounds that may inhibit EGFR activation and/or EGFR-mediated downstream signaling pathway. This drug screening platform is based on the characterization of an EGFR-transfected 32D cell line (32D-EGFR). The expression of EGFR in 32D cells allowed cell proliferation in the presence of either epidermal growth factor (EGF) or interleukin 3 (IL-3) and provided a system for both screening and counterscreening of EGFR pathway-inhibitory compounds. After the completion of primary and secondary screenings in which 32D-EGFR cells were grown under the stimulation of either EGF or IL-3, 9 of 20,000 compounds were found to selectively inhibit the EGF-dependent proliferation, but not the IL-3-dependent proliferation, of 32D-EGFR cells. Subsequent analysis showed that 3 compounds of the 9 initial hits directly inhibited the kinase activity of recombinant EGFR in vitro and the phosphorylation of EGFR in H1299 cells transfected with EGFR. Thus, this 32D-EGFR assay system provides a promising approach for identifying novel EGFR and EGFR signaling pathway inhibitors with potential antitumor activity.

Original languageEnglish
Pages (from-to)89-94
Number of pages6
JournalAnalytical Biochemistry
Issue number1
Publication statusPublished - 2008 Jun 1

All Science Journal Classification (ASJC) codes

  • Biophysics
  • Biochemistry
  • Molecular Biology
  • Cell Biology


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