Department of Medical Oncology of Shaanxi Provincial People's Hospital, Xi'an, Shaanxi, China.
Xi'an Medical University, Xi'an, Shaanxi, China.
Cell Cycle. 2023 Feb;22(3):269-275. doi: 10.1080/15384101.2022.2122257. Epub 2022 Sep 13.
SET domain containing lysine methyltransferase 7 (SETD7) belongs to the protein lysine methyltransferase family and can catalyze the monomethylation of histone H3K4, which plays a vital role in the regulation of cell cycle, cell differentiation, DNA damage response and chromatin remodeling through K/R-S/T-K (K is lysine residue) sites and the recognition of substrates mediated by SET, i-SET, and -SET domains and electrostatic action. SETD7 also can regulate the transcription of several genes including β-catenin, Cullin l and lin-28 homolog A (LIN28A), etc. In addition, the abnormal expression of SETD7 can promote the proliferation, migration, invasion of tumor cells, predict the poor prognosis of tumor patients, and may be a potential target for tumor therapy. This paper reviews the structure of SETD7, its role in tumor genesis and development, and the current research progress of relevant targeted drugs to explore its regulatory mechanism in tumor genesis and development and the prospect of targeted therapy.
赖氨酸甲基转移酶 7（SET domain containing lysine methyltransferase 7，SETD7）属于蛋白赖氨酸甲基转移酶家族，能够催化组蛋白 H3K4 的单甲基化，通过 K/R-S/T-K（K 为赖氨酸残基）位点和 SET、i-SET、-SET 结构域介导的底物识别以及静电作用，在细胞周期、细胞分化、DNA 损伤反应和染色质重塑中发挥重要作用。SETD7 还可以调节包括 β-连环蛋白、Cullin l 和 lin-28 同源物 A（lin-28 homolog A，LIN28A）等在内的几个基因的转录。此外，SETD7 的异常表达可以促进肿瘤细胞的增殖、迁移和侵袭，预测肿瘤患者的不良预后，可能是肿瘤治疗的潜在靶点。本文综述了 SETD7 的结构、在肿瘤发生发展中的作用以及相关靶向药物的研究进展，探讨其在肿瘤发生发展中的调控机制和靶向治疗的前景。
