State Key Laboratory of Esophageal Cancer Prevention and Treatment, Key Laboratory of Advanced Pharmaceutical Technology, Ministry of Education of China, School of Pharmaceutical Sciences, Zhengzhou University, Zhengzhou 450001, China.
Int J Mol Sci. 2022 Aug 24;23(17):9574. doi: 10.3390/ijms23179574.
Polycomp group (PcG) proteins are members of highly conserved multiprotein complexes, recognized as gene transcriptional repressors during development and shown to play a role in various physiological and pathological processes. PcG proteins consist of two Polycomb repressive complexes (PRCs) with different enzymatic activities: Polycomb repressive complexes 1 (PRC1), a ubiquitin ligase, and Polycomb repressive complexes 2 (PRC2), a histone methyltransferase. Traditionally, PRCs have been described to be associated with transcriptional repression of homeotic genes, as well as gene transcription activating effects. Particularly in cancer, PRCs have been found to misregulate gene expression, not only depending on the function of the whole PRCs, but also through their separate subunits. In this review, we focused especially on the recent findings in the transcriptional regulation of PRCs, the oncogenic and tumor-suppressive roles of PcG proteins, and the research progress of inhibitors targeting PRCs.
多梳蛋白（PcG）家族蛋白是高度保守的多蛋白复合物的成员，在发育过程中被认为是基因转录抑制剂，并且在各种生理和病理过程中发挥作用。PcG 蛋白由具有不同酶活性的两个多梳抑制复合物（PRC）组成：多梳抑制复合物 1（PRC1），一个泛素连接酶，和多梳抑制复合物 2（PRC2），一个组蛋白甲基转移酶。传统上，PRC 被描述为与同源盒基因的转录抑制以及基因转录激活作用有关。特别是在癌症中，已经发现 PRC 错误调节基因表达，不仅取决于整个 PRC 的功能，还取决于它们的单独亚基。在这篇综述中，我们特别关注 PRC 的转录调控、PcG 蛋白的致癌和抑癌作用以及针对 PRC 的抑制剂的研究进展的最新发现。
