PMID- 32098708 OWN - NLM STAT- MEDLINE DCOM- 20210507 LR - 20210507 IS - 1464-3391 (Electronic) IS - 0968-0896 (Linking) VI - 28 IP - 7 DP - 2020 Apr 1 TI - Carcinogenic roles and therapeutic effects of EZH2 in gynecological cancers. PG - 115379 LID - S0968-0896(20)30175-9 [pii] LID - 10.1016/j.bmc.2020.115379 [doi] AB - 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. CI - Copyright (c) 2020 Elsevier Ltd. All rights reserved. FAU - Wan, Zhong AU - Wan Z AD - Urologic Medical Center, Shanghai General Hospital, Shanghai Jiao Tong University School of Medicine, Shanghai, China. FAU - Jiang, Huabo AU - Jiang H AD - Clinical and Translational Research Center, Shanghai First Maternity and Infant Hospital, Tongji University School of Medicine, Shanghai, China. FAU - Li, Li AU - Li L AD - Assisted Reproduction Technology Center, Shuguang Hospital Affiliated to Shanghai University of Traditional Chinese Medicine, Shanghai, China. FAU - Zhu, Shuhui AU - Zhu S AD - Department of Food and Drug Engineering, Shandong Vocational Animal Science and Veterinary College, Weifang, Shandong, China. FAU - Hou, Jingjing AU - Hou J AD - Department of Gastrointestinal Surgery, Institute of Gastrointestinal Oncology, Zhongshan Hospital of Xiamen University, Xiamen, Fujian, China. Electronic address: jjhou@xmu.edu.cn. FAU - Yu, Yongsheng AU - Yu Y AD - Clinical and Translational Research Center, Shanghai First Maternity and Infant Hospital, Tongji University School of Medicine, Shanghai, China. Electronic address: yongshengyu@tongji.edu.cn. LA - eng PT - Journal Article PT - Research Support, Non-U.S. Gov't PT - Review DEP - 20200217 PL - England TA - Bioorg Med Chem JT - Bioorganic & medicinal chemistry JID - 9413298 RN - 0 (Antineoplastic Agents) RN - EC 2.1.1.43 (EZH2 protein, human) RN - EC 2.1.1.43 (Enhancer of Zeste Homolog 2 Protein) SB - IM MH - Antineoplastic Agents/*pharmacology MH - Enhancer of Zeste Homolog 2 Protein/antagonists & inhibitors/genetics/*metabolism MH - Female MH - Gene Expression Regulation, Neoplastic/*drug effects MH - Genital Neoplasms, Female/*drug therapy/*enzymology MH - Humans OTO - NOTNLM OT - Enhancer of zeste homolog 2 (EZH2) OT - Gynecologic-relate malignancies OT - Polycomb group OT - Targeted inhibitors COIS- Declaration of Competing Interest The authors declared that there is no conflict of interest. EDAT- 2020/02/27 06:00 MHDA- 2021/05/08 06:00 CRDT- 2020/02/27 06:00 PHST- 2019/11/20 00:00 [received] PHST- 2020/02/10 00:00 [revised] PHST- 2020/02/12 00:00 [accepted] PHST- 2020/02/27 06:00 [pubmed] PHST- 2021/05/08 06:00 [medline] PHST- 2020/02/27 06:00 [entrez] AID - S0968-0896(20)30175-9 [pii] AID - 10.1016/j.bmc.2020.115379 [doi] PST - ppublish SO - Bioorg Med Chem. 2020 Apr 1;28(7):115379. doi: 10.1016/j.bmc.2020.115379. Epub 2020 Feb 17.