BIOCEV, First Faculty of Medicine, Charles University, Průmyslová 595, 252 50 Vestec, Czech Republic; Department of Paediatrics and Inherited Metabolic Disorders, First Faculty of Medicine, Charles University and General University Hospital in Prague, Ke Karlovu 455/2, 128 08 Prague, Czech Republic.
1st Department of Surgery-Department of Abdominal, Thoracic Surgery and Traumatology, First Faculty of Medicine, Charles University and General University Hospital, U Nemocnice 2, 121 08 Prague, Czech Republic.
Biomed Pharmacother. 2023 Oct;166:115324. doi: 10.1016/j.biopha.2023.115324. Epub 2023 Aug 18.
TET proteins (methylcytosine dioxygenases) play an important role in the regulation of gene expression. Dysregulation of their activity is associated with many serious pathogenic states such as oncological diseases. Regulation of their activity by specific inhibitors could represent a promising therapeutic strategy. Therefore, this review describes various types of TET protein inhibitors in terms of their inhibitory mechanism and possible applicability. The potential and possible limitations of this approach are thoroughly discussed in the context of TET protein functionality in living systems. Furthermore, possible therapeutic strategies based on the inhibition of TET proteins are presented and evaluated, especially in the field of oncological diseases.
TET 蛋白（甲基胞嘧啶双加氧酶）在基因表达调控中发挥着重要作用。其活性失调与许多严重的病理状态有关，如肿瘤疾病。通过特异性抑制剂来调节其活性可能代表一种有前途的治疗策略。因此，本综述从抑制机制和可能的适用性方面描述了各种类型的 TET 蛋白抑制剂。在活系统中 TET 蛋白功能的背景下，深入讨论了这种方法的潜力和可能的局限性。此外，还提出并评估了基于 TET 蛋白抑制的可能治疗策略，特别是在肿瘤疾病领域。
