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

研究成果: Article査読

27 被引用数 (Scopus)

抄録

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)

本文言語English
ページ(範囲)8574-8581
ページ数8
ジャーナルJournal of Medicinal Chemistry
54
24
DOI
出版ステータスPublished - 2011 12 22

ASJC Scopus subject areas

  • 分子医療
  • 創薬

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