Scutellarin inhibits Hela cell growth and glycolysis by inhibiting the activity of pyruvate kinase M2
Scutellarin inhibits Hela cell growth and glycolysis by inhibiting the activity of pyruvate kinase M2
复制标题
灯盏乙素通过抑制丙酮酸激酶 M2 的活性来抑制 Hela 细胞生长和糖酵解
DOI：
10.1016/j.bmcl.2017.11.011
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发表时间：
2017
影响因子：
2.7
通讯作者：
He Bin
中科院分区：
文献类型：
--
作者：
You Lin;Zhu Hong;Wang Chun;Wang Fang;Li Yongjun;Li Yan;Wang Yonglin;He Bin
Scutellarin, one of natural flavonoids, is widely and clinically used for treating many diseases in China. Recently, scutellarin has demonstrated a broad spectrum of anti-proliferative activities against multiple cancer cell lines. However, the molecular mechanism of action remains to be investigated. We herein report the design and synthesis of biotinylated scutellareins as probes, which can be applied to discover scutellarein interacting proteins. Finally, we show that scutellarin directly targets pyruvate kinase M2 (PKM2) and inhibits its cytosolic activity to decrease glycolytic metabolism; on the other hand, scutellarin may also participate in regulating cell cycle and apoptotic proteins by activating MEK/ERK/PIN1 signaling pathway to promote the nuclear translocation of PKM2.
