Chetverina D A, Lomaev D V, Erokhin M M
Institute of Gene Biology, Russian Academy of Sciences, Moscow, 119334 Russia.
Acta Naturae. 2020 Oct-Dec;12(4):66-85. doi: 10.32607/actanaturae.11090.
Polycomb group (PcG) and Trithorax group (TrxG) proteins are evolutionarily conserved factors responsible for the repression and activation of the transcription of multiple genes in and mammals. Disruption of the PcG/TrxG expression is associated with many pathological conditions, including cancer, which makes them suitable targets for diagnosis and therapy in medicine. In this review, we focus on the major PcG and TrxG complexes, the mechanisms of PcG/TrxG action, and their recruitment to chromatin. We discuss the alterations associated with the dysfunction of a number of factors of these groups in oncology and the current strategies used to develop drugs based on small-molecule inhibitors.
多梳蛋白家族（PcG）和三胸蛋白家族（TrxG）蛋白是进化上保守的因子，负责果蝇和哺乳动物中多个基因转录的抑制和激活。PcG/TrxG表达的破坏与许多病理状况相关，包括癌症，这使得它们成为医学诊断和治疗的合适靶点。在本综述中，我们重点关注主要的PcG和TrxG复合物、PcG/TrxG的作用机制及其在染色质上的募集。我们讨论了这些蛋白家族中一些因子功能障碍在肿瘤学中的相关改变，以及目前基于小分子抑制剂开发药物所采用的策略。
