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Title 

2′-hydroxycinnamaldehyde inhibits cancer cell proliferation and tumor growth by targeting the pyruvate kinase M2

 

하드록시 신남알데하이드에 의한 PKM2 활성화와 항암효과

Authors 

Yae Jin YoonYoung Hwan KimYena JinSeung-Wook ChiJeong Hee MoonDong Cho HanByoung-Mog Kwon

Publisher 

Elsevier

Issue Date 

2018

Citation 

Cancer Letters

Keywords 

Anti-tumorCancer metabolismExtracellular vesiclePyruvate kinase M2Traditional medicine

Abstract 

It is reported that 2'-hydroxycinnamaldehyde (HCA), isolated from cinnamon, has anti-tumor effects through the modulation of multi-target molecules. In this study, we identified pyruvate kinase M2 (PKM2) as a direct target of HCA by use of biochemical methods including affinity chromatography, drug affinity responsive target stability, and cellular thermal shift assay. PKM2 is up-regulated in multiple cancer types and is considered as a potential target for cancer therapy. HCA binds directly to PKM2 and selectively decreases the phosphorylation of PKM2 at Tyr105, indicating a potential anti-proliferative effect on prostate cancer cells. As a PKM2 activator, HCA increases pyruvate kinase activity by promoting the tetrameric state of PKM2. However, HCA suppresses protein kinase activity of PKM2 by decreasing the phosphorylation at Tyr105. Moreover, this leads to a decrease of PKM2-mediated STAT3 phosphorylation at Tyr705 and a down-regulation of target genes, including MEK5 and cyclin D1. Furthermore, HCA suppresses tumor growth and the release of tumor extracellular vesicles in vivo by inhibiting the phosphorylation of PKM2. Collectively, our results suggest that HCA may be a potential anticancer agent targeting PKM2 in cancer progression.

ISSN 

0304-3835

Link 

http://dx.doi.org/10.1016/j.canlet.2018.07.015

Appears in Collections

1. Journal Articles > Journal Articles

Registered Date

2019-05-02


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