Lysine methylation of transcription factors in cancer.,Cell Death & Disease

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Lysine methylation of transcription factors in cancer.
Cell Death & Disease ( IF 8.1 ) Pub Date : 2019-03-29 , DOI: 10.1038/s41419-019-1524-2
Dong Han ₁ , Mengxi Huang ₂ , Ting Wang ₂ , Zhiping Li ₁ , Yanyan Chen ₂ , Chao Liu ₃ , Zengjie Lei _{1,

2} , Xiaoyuan Chu _{1,

2}

Affiliation

Protein lysine methylation is a critical and dynamic post-translational modification that can regulate protein stability and function. This post-translational modification is regulated by lysine methyltransferases and lysine demethylases. Recent studies using mass-spectrometric techniques have revealed that in addition to histones, a great number of transcription factors are also methylated, often at multiple sites and to different degrees (mono-, di-, trimethyl lysine). The biomedical significance of transcription factor methylation in human diseases, including cancer, has been explored recently. Some studies have demonstrated that interfering with transcription factor lysine methylation both in vitro and in vivo can inhibit cancer cell proliferation, thereby reversing tumor progression. The inhibitors targeting lysine methyltransferases and lysine demethylases have been under development for the past two decades, and may be used as potential anticancer agents in the clinic. In this review, we focus on the current findings of transcription factor lysine methylation, and the effects on both transcriptional activity and target gene expression. We outlined the biological significance of transcription factor lysine methylation on tumor progression and highlighted its clinical value in cancer therapy.

中文翻译：

癌症中转录因子的赖氨酸甲基化。

蛋白质赖氨酸甲基化是关键且动态的翻译后修饰，可调节蛋白质的稳定性和功能。该翻译后修饰受赖氨酸甲基转移酶和赖氨酸脱甲基酶的调节。最近使用质谱技术进行的研究表明，除组蛋白外，许多转录因子也被甲基化，常常在多个位点以不同程度被甲基化（单，二，三甲基赖氨酸）。最近已经探索了转录因子甲基化在包括癌症在内的人类疾病中的生物医学意义。一些研究表明，在体外和体内干扰转录因子赖氨酸甲基化均可抑制癌细胞的增殖，从而逆转肿瘤的进展。在过去的二十年中，针对赖氨酸甲基转移酶和赖氨酸脱甲基酶的抑制剂一直在开发中，并且可以在临床中用作潜在的抗癌药。在这篇综述中，我们重点研究转录因子赖氨酸甲基化的最新发现，以及对转录活性和靶基因表达的影响。我们概述了转录因子赖氨酸甲基化对肿瘤进展的生物学意义，并突出了其在癌症治疗中的临床价值。

更新日期：2019-04-01

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