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Updated: Nov 15, 2025

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Published on: October 31, 2016
Targeting Epigenetic Regulators for Endometrial Cancer Therapy: Its Molecular Biology and Potential Clinical
Futaba Inoue1, Kenbun Sone1, Yusuke Toyohara1
1Department of Obstetrics and Gynecology, Faculty of Medicine, The University of Tokyo, 7-3-1 Hongo Bunkyo-ku, Tokyo 113-8655, Japan.
Abstract:
Endometrial cancer is one of the most frequently diagnosed gynecological malignancies worldwide. However, its prognosis in advanced stages is poor, and there are only few available treatment options when it recurs. Epigenetic changes in gene function, such as DNA methylation, histone modification, and non-coding RNA, have been studied for the last two decades. Epigenetic dysregulation is often reported in the development and progression of various cancers. Recently, epigenetic changes in endometrial cancer have also been discussed. In this review, we give the main points of the role of DNA methylation and histone modification in endometrial cancer, the diagnostic tools to determine these modifications, and inhibitors targeting epigenetic regulators that are currently in preclinical studies and clinical trials.
Insights
Epigenetic changes like DNA methylation are key in endometrial cancer development. This review covers their role, diagnostic tools, and emerging epigenetic drugs in trials.
Area of Science:
- Gynecological Oncology
- Epigenetics
- Molecular Biology
Background:
- Endometrial cancer is a common gynecological malignancy with poor prognosis in advanced stages.
- Limited treatment options exist for recurrent endometrial cancer.
- Epigenetic dysregulation, including DNA methylation and histone modification, is implicated in various cancers.
Purpose of the Study:
- To review the role of DNA methylation and histone modification in endometrial cancer.
- To discuss diagnostic tools for these epigenetic modifications.
- To summarize epigenetic inhibitors in preclinical and clinical development for endometrial cancer.
Main Methods:
- Literature review focusing on DNA methylation and histone modification in endometrial cancer.
- Analysis of current diagnostic techniques for epigenetic alterations.
- Survey of ongoing preclinical and clinical trials for epigenetic drugs.
Main Results:
- Epigenetic dysregulation, particularly DNA methylation and histone modification, significantly contributes to endometrial cancer initiation and progression.
- Various diagnostic tools are available to detect these epigenetic changes.
- Several inhibitors targeting epigenetic regulators are under investigation in preclinical and clinical settings.
Conclusions:
- Epigenetic modifications play a crucial role in endometrial cancer.
- Diagnostic advancements aid in understanding these changes.
- Targeting epigenetic regulators offers promising therapeutic strategies for endometrial cancer.
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