组蛋白甲基转移酶的双重功能。
Bifaceted functions of histone methyltransferases.
作者信息
Akhtar Jawad, Saloura Vassiliki
机构信息
Thoracic and GI Malignancies Branch, Center for Cancer Research, National Cancer Institute, NIH, Bethesda, MD, USA.
出版信息
Epigenomics. 2025 Sep;17(13):891-896. doi: 10.1080/17501911.2025.2530925. Epub 2025 Jul 13.
Abstract
In this perspective, Akhtar et al provide a brief overview of Enhancer of Zeste Homolog 2 (EZH2) and SET and MYND-domain containing 3 (SMYD3) as histone methyltransferases that function both as activators and repressors of gene transcription in cancer. The importance of deciphering the mechanisms underlying this bifaceted function toward thoughtful pharmacologic interventions is underlined and protein or mRNA degradation are highlighted as the most biologically rational pharmaceutical platforms to target these bifaceted histone methyltransferases.
摘要
从这个角度来看，阿赫塔尔等人简要概述了zeste同源物2增强子（EZH2）和含SET及MYND结构域蛋白3（SMYD3）这两种组蛋白甲基转移酶，它们在癌症中既作为基因转录的激活剂又作为抑制剂发挥作用。文中强调了破解这种双重功能背后机制对于进行周全的药物干预的重要性，并指出蛋白质或mRNA降解是针对这些具有双重功能的组蛋白甲基转移酶最具生物学合理性的药物作用平台。
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本文引用的文献
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EZH2 PROTACs target EZH2- and FOXM1-associated oncogenic nodes, suppressing breast cancer cell growth.EZH2 PROTACs 靶向 EZH2 和 FOXM1 相关的致癌节点，抑制乳腺癌细胞生长。
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