Oncotarget

Research Papers:

Sesquiterpene binding Gly-Leu-Ser/Lys-“co-adaptation pocket” to inhibit lung cancer cell epithelial–mesenchymal transition

Xiao-Yu Ai, Heng Zhang, Shao-Yan Gao, Yuan Qin, Wei-Long Zhong, Ju Gu, Meng Li, Kai-Liang Qiao, Qin Tian, Zhan-Hong Cui, Jia-Huan Yang, Zhun Bi, Ting Xiao, Shuang Chen, Hui-Juan Liu, Hong-Gang Zhou, Tao Sun and Cheng Yang _

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Oncotarget. 2017; 8:70192-70203. https://doi.org/10.18632/oncotarget.19599

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Abstract

Xiao-Yu Ai1,*, Heng Zhang1,*, Shao-Yan Gao1,*, Yuan Qin1,2, Wei-Long Zhong1,2, Ju Gu1,2, Meng Li1,2, Kai-Liang Qiao1,2, Qin Tian1,2, Zhan-Hong Cui1,2, Jia-Huan Yang1,2, Zhun Bi1, Ting Xiao1,2, Shuang Chen2, Hui-Juan Liu2, Hong-Gang Zhou1,2, Tao Sun1,2 and Cheng Yang1,2

1State Key Laboratory of Medicinal Chemical Biology and College of Pharmacy, Nankai University, Tianjin, China

2Tianjin Key Laboratory of Molecular Drug Research, Tianjin International Joint Academy of Biomedicine, Tianjin, China

*These authors have contributed equally to this work

Correspondence to:

Cheng Yang, email: [email protected]

Tao Sun, email: [email protected]

Hong-Gang Zhou, email: [email protected]

Keywords: antitumor, EMT, co-adaptation pocket, ERK2, lung cancer

Abbreviations: SL: sesquiterpene lactones; PTL: parthenolide; EMT: epithelial–mesenchymal transition

Received: March 15, 2017     Accepted: June 20, 2017     Published: July 26, 2017

ABSTRACT

Sesquiterpene lactones (SL) have a wide range of applications in anti-tumor and anti-inflammatory therapy. However, the pharmacological mechanism of such substances is not clear. In this study, parthenolide (PTL) was used as an example to explore the anti-tumor effect of natural molecules and their common mechanism. We showed that PTL inhibited the proliferation and migration by reverse EMT via the ERK2/NF-κB/Snail pathway in vivo and in vitro. Interestingly, Multiple potential targets of PTL contain a Gly-Leu-Ser/Lys-“co-adaptation pocket”. This inspiring us analogies of PTL may also bind to these target proteins and play a similar function. Significantly, the Concept of co-adaptation pocket may help to increase the selectivity of drug research and development.


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