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靶向子宫内膜癌治疗的表观遗传调节剂:其分子生物学和潜在临床应用。

Targeting Epigenetic Regulators for Endometrial Cancer Therapy: Its Molecular Biology and Potential Clinical Applications.

机构信息

Department of Obstetrics and Gynecology, Faculty of Medicine, The University of Tokyo, 7-3-1 Hongo Bunkyo-ku, Tokyo 113-8655, Japan.

出版信息

Int J Mol Sci. 2021 Feb 25;22(5):2305. doi: 10.3390/ijms22052305.

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.

摘要

子宫内膜癌是全球最常见的妇科恶性肿瘤之一。然而,其晚期预后较差,且复发时可供选择的治疗方法有限。过去二十年,人们一直在研究基因功能的表观遗传变化,如 DNA 甲基化、组蛋白修饰和非编码 RNA。表观遗传失调在各种癌症的发生和发展中经常被报道。最近,子宫内膜癌中的表观遗传变化也被讨论。在这篇综述中,我们给出了 DNA 甲基化和组蛋白修饰在子宫内膜癌中的作用要点、用于确定这些修饰的诊断工具,以及目前处于临床前研究和临床试验阶段的靶向表观遗传调节剂的抑制剂。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/700d/7956745/a3b8c73999bd/ijms-22-02305-g001.jpg

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