Coumestrol epigenetically suppresses cancer cell proliferation: Coumestrol is a natural haspin kinase inhibitor

Jong Eun Kim, Sung Young Lee, Mi Jang, Hyo Kyung Choi, Jong Hun Kim, Hanyong Chen, Tae Gyu Lim, Zigang Dong, Ki Won Lee

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30 Scopus citations


Targeting epigenetic changes in gene expression in cancer cells may offer new strategies for the development of selective cancer therapies. In the present study, we investigated coumestrol, a natural compound exhibiting broad anti-cancer effects against skin melanoma, lung cancer and colon cancer cell growth. Haspin kinase was identified as a direct target protein of coumestrol using kinase profiling analysis. Histone H3 is a direct substrate of haspin kinase. We observed haspin kinase overexpression as well as greater phosphorylation of histone H3 at threonine 3 (Thr-3) in the cancer cells compared to normal cells. Computer modeling using the Schrödinger Suite program identified the binding interface within the ATP binding site. These findings suggest that the anticancer effect of coumestrol is due to the direct targeting of haspin kinase. Coumestrol has considerable potential for further development as a novel anti-cancer agent.

Original languageEnglish (US)
Article number2228
JournalInternational journal of molecular sciences
Issue number10
StatePublished - Oct 24 2017

Bibliographical note

Funding Information:
Acknowledgments: This work was supported by the “Cooperative Research Program for Agriculture Science and Technology Development (Project No. PJ01133403 to KWL)” from Rural Development Administration, the Korea Food Research Institute (E0164700-02) and the National Research Foundation of Korea (NRF) grant funded by the Korea government (Ministry of Science, ICT & Future Planning) (NO. 2015R1A2A1A10053567 to KWL and NO. NRF-2017R1C1B5017109 to JEK).

Publisher Copyright:
© 2017 by the authors. Licensee MDPI, Basel, Switzerland.


  • Cancer
  • Coumestrol
  • Haspin kinase
  • Histone H3


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