ArticleInternational journal of molecular sciences2017
Coumestrol Epigenetically Suppresses Cancer Cell Proliferation: Coumestrol Is a Natural Haspin Kinase Inhibitor.
Article in International journal of molecular sciences, 2017. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 19 papers.
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Who cites it
19 citing papers in PubMed.
- Oral Ingestion of Bean Sprouts Containing the HASPIN Inhibitor Coumestrol Increased Blood Testosterone Levels in Men.Biology · 2025Article
- Bioinformatics-based drug repositioning and prediction of the main active ingredients and potential mechanisms of action for the efficacy of Dan-Lou tablet.Scientific reports · 2024Article
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- Coumestrol facilitates apoptosis in colorectal cancer cells by interacting with ZIP8 protein via the ferroptosis pathway.Journal of Cancer · 2024Article
- Ingestion of Soybean Sprouts Containing a HASPIN Inhibitor Improves Condition in a Mouse Model of Alzheimer's Disease.Biology · 2023Article
- Article
- Diagnostic value of abnormal chromosome 3p genes in small-cell lung cancer.Oncology letters · 2022Article
- Inhibitory Effect of the HASPIN Inhibitor CHR-6494 on BxPC-3-Luc, A Luciferase-Expressing Pancreatic Cancer Cell Line.Cell journal · 2022Article
- Dietary Phytoestrogens and Their Metabolites as Epigenetic Modulators with Impact on Human Health.Antioxidants (Basel, Switzerland) · 2021Review
- Phosphorylation of H3-Thr3 by Haspin Is Required for Primary Cilia Regulation.International journal of molecular sciences · 2021Article
- Article
- Recent Advances in Heterologous Synthesis Paving Way for Future Green-Modular Bioindustries: A Review With Special Reference to Isoflavonoids.Frontiers in bioengineering and biotechnology · 2021Review
- Design of new disubstituted imidazo[1,2-Journal of enzyme inhibition and medicinal chemistry · 2020Article
- HASPIN kinase inhibitor CHR-6494 suppresses intestinal polyp development, cachexia, and hypogonadism in Apcmin/+ mice.European journal of cancer prevention : the official journal of the European Cancer Prevention Organisation (ECP) · 2020Article
- Knockdown of GSG2 inhibits prostate cancer progression in vitro and in vivo.International journal of oncology · 2020Article
- GSG2 (Haspin) promotes development and progression of bladder cancer through targeting KIF15 (Kinase-12).Aging · 2020Article
- Bioinformatic Analysis Reveals GSG2 as a Potential Target for Breast Cancer Therapy.Open life sciences · 2019Article
- Ripasudil Attenuates Lipopolysaccharide (LPS)-Mediated Apoptosis and Inflammation in Pulmonary Microvascular Endothelial Cells via ROCK2/eNOS Signaling.Medical science monitor : international medical journal of experimental and clinical research · 2018Article
Corrections and comments
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Authors and funding
9 authors.
Funding
No grant is acknowledged in the PubMed record.
Abstract
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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Registered trials
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