Carcinogenic roles and therapeutic effects of EZH2 in gynecological cancers

Zhong Wan; Huabo Jiang; Li Li; Shuhui Zhu; Jingjing Hou; Yongsheng Yu

doi:10.1016/j.bmc.2020.115379

Carcinogenic roles and therapeutic effects of EZH2 in gynecological cancers

Bioorg Med Chem. 2020 Apr 1;28(7):115379. doi: 10.1016/j.bmc.2020.115379. Epub 2020 Feb 17.

Authors

Zhong Wan¹, Huabo Jiang², Li Li³, Shuhui Zhu⁴, Jingjing Hou⁵, Yongsheng Yu⁶

Affiliations

¹ Urologic Medical Center, Shanghai General Hospital, Shanghai Jiao Tong University School of Medicine, Shanghai, China.
² Clinical and Translational Research Center, Shanghai First Maternity and Infant Hospital, Tongji University School of Medicine, Shanghai, China.
³ Assisted Reproduction Technology Center, Shuguang Hospital Affiliated to Shanghai University of Traditional Chinese Medicine, Shanghai, China.
⁴ Department of Food and Drug Engineering, Shandong Vocational Animal Science and Veterinary College, Weifang, Shandong, China.
⁵ Department of Gastrointestinal Surgery, Institute of Gastrointestinal Oncology, Zhongshan Hospital of Xiamen University, Xiamen, Fujian, China. Electronic address: jjhou@xmu.edu.cn.
⁶ Clinical and Translational Research Center, Shanghai First Maternity and Infant Hospital, Tongji University School of Medicine, Shanghai, China. Electronic address: yongshengyu@tongji.edu.cn.

PMID: 32098708
DOI: 10.1016/j.bmc.2020.115379

Abstract

Enhancer of Zeste Homolog 2 (EZH2) is highly expressed in kinds of malignant tumors and related to tumor occurrence, development, and prognosis. EZH2 is the catalytic subunit of the polycomb repressive complex 2 (PRC2), which promotes cell proliferation, migration, and invasion by epigenetic regulation of anti-tumor gene. It can activate numerous tumor-associated signaling pathways and interfere with DNA damage repair. In recent years, large amounts of studies have shown that EZH2 is closely related to gynecologic-related malignancies and can be used as a potential target gene for the treatment of gynecological-related malignancies. This review summarizes the oncogenic function of EZH2 and introduces the recent advances in the development of EZH2 inhibitors. On this basis, future research prospect of EZH2 is proposed.

Keywords: Enhancer of zeste homolog 2 (EZH2); Gynecologic-relate malignancies; Polycomb group; Targeted inhibitors.

Publication types

Research Support, Non-U.S. Gov't
Review

MeSH terms

Antineoplastic Agents / pharmacology*
Enhancer of Zeste Homolog 2 Protein / antagonists & inhibitors
Enhancer of Zeste Homolog 2 Protein / genetics
Enhancer of Zeste Homolog 2 Protein / metabolism*
Female
Gene Expression Regulation, Neoplastic / drug effects*
Genital Neoplasms, Female / drug therapy*
Genital Neoplasms, Female / enzymology*
Humans

Substances

Antineoplastic Agents
EZH2 protein, human
Enhancer of Zeste Homolog 2 Protein