果蝇Zeste基因增强子人类同源物2(Drosophila zeste gene enhancer of human homolog 2,EZH2)是一种参与基因负性表观遗传调控的甲基转移酶。研究发现,EZH2在多种肿瘤组织中高表达,并与肿瘤的发生发展和侵袭转移密切相关,由此成为抗肿瘤治疗新的分子靶点。目前已研发出多种EZH2抑制剂用于肿瘤的基础和临床治疗研究,并取得令人鼓舞的结果。本文将对EZH2小分子抑制剂的研究进展做简要综述。 Drosophila zeste gene enhancer of human homolog 2 (EZH2) is a methyltransferase involved in the negative epigenetic regulation of genes. The study found that EZH2 is highly expressed in many tumor tissues and is closely related to tumorigenesis and invasion and metastasis, thus becoming a new molecular target of antitumor therapy. A number of EZH2 inhibitors have been developed for the study of basic and clinical treatment of tumors and encouraging results have been obtained. This article will briefly review the research progress of EZH2 small molecule inhibitors.