The role of H3K27me3 methylation in cancer development

Longjiang Di, Wei-Guo Zhu

Genome Instability & Disease ›› 2024, Vol. 5 ›› Issue (1) : 17-34. DOI: 10.1007/s42764-023-00118-0

The role of H3K27me3 methylation in cancer development

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Abstract

Although the importance of histone methylation in epigenetics was first suggested more than 50 years ago, research into histone modifications conducted in the past decade has led to an exponential increase in our understanding of histone H3 modifications. In particular, the involvement of H3 histone 27 lysine trimethylation in the development of various cancer phenotypes has been demonstrated. Unlike mutations in the DNA sequence, such epigenetic changes are reversible, suggesting that inhibitors of H3 histone 27 amino acid methylation enzymes could be used as anti-cancer agents. Here, we outline the regulatory functions of H3 histone 27 lysine trimethylation carried out by different enzymes, in carcinogenesis. We describe the role of H3 histone 27 lysine trimethylation as an important epigenetic regulatory mechanism in the development of various cancers via effects on inflammation, DNA damage repair, cell proliferation, cell metastasis, regulatory cell death, ferroptosis, and angiogenesis. Finally, we focus specifically on H3 histone 27 lysine trimethylation regulators and their future development as anti-cancer drugs.

Keywords

Cancer / Cancer therapy / DNA damage repair / Epigenetic regulators / H3K27me3 / Histone methylation

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Longjiang Di, Wei-Guo Zhu. The role of H3K27me3 methylation in cancer development. Genome Instability & Disease, 2024, 5(1): 17‒34 https://doi.org/10.1007/s42764-023-00118-0

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National Natural Science Foundation of China(82002986)

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