EZH2: a novel target for cancer treatment

被引：579
作者：
Duan, Ran [1 ,2 ]
Du, Wenfang [3 ]
Guo, Weijian [1 ,2 ]
机构：
[1] Fudan Univ, Dept Med Oncol, Shanghai Canc Ctr, Shanghai 200032, Peoples R China
[2] Fudan Univ, Shanghai Med Coll, Dept Oncol, Shanghai 200032, Peoples R China
[3] Fudan Univ, Shanghai Med Coll, Shanghai 200032, Peoples R China
来源：
JOURNAL OF HEMATOLOGY & ONCOLOGY | 2020年 / 13卷 / 01期
关键词：
EZH2; Cancer; inhibitor; HOMOLOG; 2; EZH2; EPITHELIAL-MESENCHYMAL TRANSITION; GROUP PROTEIN EZH2; SELECTIVE-INHIBITION; HISTONE METHYLTRANSFERASE; BREAST-CANCER; POLYCOMB; METHYLATION; CELLS; PROSTATE;
D O I：
10.1186/s13045-020-00937-8
中图分类号：
R73 [肿瘤学];
学科分类号：
100214 ;
摘要：
Enhancer of zeste homolog 2 (EZH2) is enzymatic catalytic subunit of polycomb repressive complex 2 (PRC2) that can alter downstream target genes expression by trimethylation of Lys-27 in histone 3 (H3K27me3). EZH2 could also regulate gene expression in ways besides H3K27me3. Functions of EZH2 in cells proliferation, apoptosis, and senescence have been identified. Its important roles in the pathophysiology of cancer are now widely concerned. Therefore, targeting EZH2 for cancer therapy is a hot research topic now and different types of EZH2 inhibitors have been developed. In this review, we summarize the structure and action modes of EZH2, focusing on up-to-date findings regarding the role of EZH2 in cancer initiation, progression, metastasis, metabolism, drug resistance, and immunity regulation. Furtherly, we highlight the advance of targeting EZH2 therapies in experiments and clinical studies.
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页数：12
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