Journal
BIOORGANIC & MEDICINAL CHEMISTRY
Volume 28, Issue 7, Pages -Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmc.2020.115379
Keywords
Enhancer of zeste homolog 2 (EZH2); Polycomb group; Targeted inhibitors; Gynecologic-relate malignancies
Funding
- National Natural Science Foundation of China [81902622]
- Shanghai Pujiang Program (China) [18PJ1409400]
- Fundamental Research Funds for the Central Universities (China) [22120170210]
- Scientific Research Foundation of Shanghai Municipal Commission of Health and Family Planning (China) [20174Y0218]
- Program for Young Excellent Talents in Tongji University (China) [1515219033]
- Foundation of Fujian Provincial Department of Science and Technology (China) [2019J01556, 2018-ZQN-87, 2018-2-66]
- Foundation of Xiamen Municipal Bureau of Science and Technology (China) [3502Z20174080, 3502Z20184038]
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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.
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