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

• DOI: 10.18632/oncotarget.19599
• Publication Date: 2017-07-27T00:32:16Z
• Authors: 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
• Keywords: 0303 health sciences; 03 medical and health sciences; Research Paper; 3. Good health

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.