Inhibition of glutathione S-Transferase M1 by new gabosine analogues is essential for overcoming cisplatin resistance in lung cancer cells

Chie Hong Wang, Ho T. Wu, Hau M. Cheng, Tien Jui Yen, I. Hsuan Lu, Hui Chuan Chang, Shu Chuan Jao, Tony K.M. Shing, Wen Shan Li

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25 Citations (Scopus)

Abstract

A new class of human GST inhibitors has been identified via rational design approach; we report their discovery, synthesis, inhibitory activity, and synergetic effect in combination with cisplatin against A549 lung cancer cell line. The results of this effort show that the lead 4-O-decyl-gabosine D (24) has optimum synergetic effect in A549 human lung adenocarcinoma epithelial cell and that this activity involves inhibition of glutathione S-transferase M1, apparently consistent with siRNA-mediated knockdown of GSTM1 gene. (Figure presented)

Original languageEnglish
Pages (from-to)8574-8581
Number of pages8
JournalJournal of Medicinal Chemistry
Volume54
Issue number24
DOIs
Publication statusPublished - 2011 Dec 22

ASJC Scopus subject areas

  • Molecular Medicine
  • Drug Discovery

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    Wang, C. H., Wu, H. T., Cheng, H. M., Yen, T. J., Lu, I. H., Chang, H. C., Jao, S. C., Shing, T. K. M., & Li, W. S. (2011). Inhibition of glutathione S-Transferase M1 by new gabosine analogues is essential for overcoming cisplatin resistance in lung cancer cells. Journal of Medicinal Chemistry, 54(24), 8574-8581. https://doi.org/10.1021/jm201131n