EZH2小分子抑制药抗消化道肿瘤的研究进展

Research Progress in EZH2 Small Molecule Inhibitor in the Treatment of Gastrointestinal Cancer

消化道肿瘤的发病率呈逐年上升趋势,组蛋白H3的27位赖氨酸残基位点的甲基化修饰酶EZH2成为肿瘤发病机制的研究热点之一。EZH2被发现在多种消化道肿瘤组织中过表达,EZH2酶活性抑制药有望成为新的抗消化道肿瘤药物。本文对EZH2在消化道肿瘤的表达情况及近年来EZH2抑制药治疗消化道肿瘤的研究结果进行综述,以期为后续研究及最终的临床应用提供理论参考。

The incidence of gastrointestinal cancer is increasing year by year. Methylase of the 27 th lysine disabled site of histone H3 EZH2 has become one of the hot spots in gastrointestinal cancer pathogenesis. EZH2 has been found to be over-expressed in a variety of gastrointestinal cancer tissues,and EZH2 inhibitor may be a new antitumor drug. The expression of EZH2 in gastrointestinal cancer and the therapeutic effect of EZH2 inhibitors in recent years were reviewed in order to provide theoretical reference for the following studies and clinical application.