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

doi:10.1021/jm201131n

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

Department of Chemistry

Research output: Contribution to journal › Article › peer-review

30 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 language	English
Pages (from-to)	8574-8581
Number of pages	8
Journal	Journal of Medicinal Chemistry
Volume	54
Issue number	24
DOIs	https://doi.org/10.1021/jm201131n
Publication status	Published - 2011 Dec 22

ASJC Scopus subject areas

Molecular Medicine
Drug Discovery

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10.1021/jm201131n

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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)",

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AU - Wang, Chie Hong

AU - Wu, Ho T.

AU - Cheng, Hau M.

AU - Yen, Tien Jui

AU - Lu, I. Hsuan

AU - Chang, Hui Chuan

AU - Jao, Shu Chuan

AU - Shing, Tony K.M.

AU - Li, Wen Shan

PY - 2011/12/22

Y1 - 2011/12/22

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

Abstract

ASJC Scopus subject areas

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