Department of Biological Sciences, Center for Cancer Research and Therapeutic Development, Clark Atlanta University, Atlanta, GA 30314,United States.
Chemical Biology Program, Department of Pharmacology and Toxicology, University of Texas Medical Branch, Galveston, TX 77555,United States.
Curr Top Med Chem. 2021;21(31):2771-2777. doi: 10.2174/1568026621666210920154942.
The polycomb repressive complex 2 (PRC2) can methylate at lysine 27 of histone H3 at the trimethylation level (H3K27me3). This leads to gene silencing and is known to be dysregulated in many cancers. PRC2 is made up of three core subunits: EZH2, SUZ12, and EED. EED is essential for the regulation of PRC2 function by binding to H3K27me3. Targeting the allosteric site within EED offers new strategies to disrupt the PRC2 activity. In this minireview, we summarize some of the recent developments in small molecules that target EED and its interaction with other core proteins in the PRC2 complex.
多梳抑制复合物 2（PRC2）可以在组蛋白 H3 的赖氨酸 27 位进行三甲基化修饰（H3K27me3）。这导致基因沉默，并且已知在许多癌症中失调。PRC2 由三个核心亚基组成：EZH2、SUZ12 和 EED。EED 通过与 H3K27me3 结合对于 PRC2 功能的调节是必不可少的。靶向 EED 的变构位点为破坏 PRC2 活性提供了新的策略。在这篇简评中，我们总结了一些针对 EED 及其与 PRC2 复合物中其他核心蛋白相互作用的小分子的最新进展。
