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10.3390/ijms18102228

http://scihub22266oqcxt.onion/10.3390/ijms18102228
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C5666907!5666907!29064398
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suck abstract from ncbi


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pmid29064398      Int+J+Mol+Sci 2017 ; 18 (10): ä
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  • Coumestrol Epigenetically Suppresses Cancer Cell Proliferation: Coumestrol Is a Natural Haspin Kinase Inhibitor #MMPMID29064398
  • Kim JE; Lee SY; Jang M; Choi HK; Kim JH; Chen H; Lim TG; Dong Z; Lee KW
  • Int J Mol Sci 2017[Oct]; 18 (10): ä PMID29064398show ga
  • 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.
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