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Int. J. Mol. Sci. 2017, 18(10), 2228;

Coumestrol Epigenetically Suppresses Cancer Cell Proliferation: Coumestrol Is a Natural Haspin Kinase Inhibitor

Research Institute of Biotechnology and Medical Converged Science, Dongguk University-Seoul, Goyang 10326, Korea
The Hormel Institute, University of Minnesota, Minneapolis, MN 55912, USA
Korea Food Research Institute, Iseo-myeon, Wanju-gun, Jeollabuk-do 55365, Korea
Research Institute of Agriculture and Life Sciences, Seoul National University, Seoul 08826, Korea
Department of Agricultural Biotechnology, Seoul National University, Seoul 08826, Korea
Authors to whom correspondence should be addressed.
These authors contributed equally to this work.
Received: 19 October 2017 / Revised: 19 October 2017 / Accepted: 21 October 2017 / Published: 24 October 2017
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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 anti-cancer 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. View Full-Text
Keywords: cancer; coumestrol; haspin kinase; histone H3 cancer; coumestrol; haspin kinase; histone H3

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This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited (CC BY 4.0).

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Kim, J.-E.; Lee, S.-Y.; Jang, M.; Choi, H.-K.; Kim, J.H.; Chen, H.; Lim, T.-G.; Dong, Z.; Lee, K.W. Coumestrol Epigenetically Suppresses Cancer Cell Proliferation: Coumestrol Is a Natural Haspin Kinase Inhibitor. Int. J. Mol. Sci. 2017, 18, 2228.

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