Open AccessSesquiterpene binding Gly-Leu-Ser/Lys-“co-adaptation pocket” to inhibit lung cancer cell epithelial-mesenchymal transition
Author(s) -
Xiaoyu Ai,
Heng Zhang,
Shaoyan Gao,
Yuan Qin,
Weilong Zhong,
Ju Gu,
Meng Li,
Kun Qiao,
Qing Tian,
Zhan-Hong Cui,
Jiahuan Yang,
Zhun Bi,
Xiao Tu,
Shuang Chen,
Huijuan Liu,
Honggang Zhou,
Tao Sun,
Cheng Yang
Publication year - 2017
Publication title -
oncotarget
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.373
H-Index - 127
ISSN - 1949-2553
DOI - 10.18632/oncotarget.19599
Subject(s) - epithelial–mesenchymal transition , lung cancer , cancer research , mesenchymal stem cell , medicine , cell , transition (genetics) , lung , biology , microbiology and biotechnology , chemistry , pathology , biochemistry , gene
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.