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Sesquiterpene binding Gly-Leu-Ser/Lys-"co-adaptation pocket" to inhibit lung cancer cell epithelial-mesenchymal transition.


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-?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.

SUBMITTER: Ai XY 

PROVIDER: S-EPMC5642546 | biostudies-literature | 2017 Sep

REPOSITORIES: biostudies-literature

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Sesquiterpene binding Gly-Leu-Ser/Lys-"co-adaptation pocket" to inhibit lung cancer cell epithelial-mesenchymal transition.

Ai Xiao-Yu XY   Zhang Heng H   Gao Shao-Yan SY   Qin Yuan Y   Zhong Wei-Long WL   Gu Ju J   Li Meng M   Qiao Kai-Liang KL   Tian Qin Q   Cui Zhan-Hong ZH   Yang Jia-Huan JH   Bi Zhun Z   Xiao Ting T   Chen Shuang S   Liu Hui-Juan HJ   Zhou Hong-Gang HG   Sun Tao T   Yang Cheng C  

Oncotarget 20170726 41


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 <i>in vivo</i> and <i>in vitro</i>. Interestingly, Multiple potential tar  ...[more]

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