Sesquiterpene Binding Gly-Leu-Ser/Lys-"Co-Adaptation Pocket" To Inhibit Lung Cancer Cell Epithelial-Mesenchymal Transition

ONCOTARGET(2017)

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摘要
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-kappa B/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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关键词
antitumor, EMT, co-adaptation pocket, ERK2, lung cancer
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