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ERK2/NF-κB/Snail通路
Oncotarget · 2017 · IF 5.168

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,Cheng Yang

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.

CAS / MDL: 20554-84-1
研究领域: 药理学 · 肿瘤学 · 分子生物学
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