2. Academic Validation
  3. EZH2: a novel target for cancer treatment

EZH2: a novel target for cancer treatment

  • J Hematol Oncol. 2020 Jul 28;13(1):104. doi: 10.1186/s13045-020-00937-8.
Ran Duan 1 2,  Wenfang Du 3,  Weijian Guo 4 5
Affiliations

Affiliations

  • 1 Department of Medical Oncology, Fudan University Shanghai Cancer Center, Shanghai, 200032, People's Republic of China.
  • 2 Department of Oncology, Shanghai Medical College, Fudan University, Shanghai, 200032, People's Republic of China.
  • 3 Shanghai Medical College, Fudan University, Shanghai, 200032, People's Republic of China.
  • 4 Department of Medical Oncology, Fudan University Shanghai Cancer Center, Shanghai, 200032, People's Republic of China. [email protected].
  • 5 Department of Oncology, Shanghai Medical College, Fudan University, Shanghai, 200032, People's Republic of China. [email protected].
PMID: 32723346 DOI: 10.1186/s13045-020-00937-8
Abstract

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.

Keywords

Cancer; EZH2; EZH2 inhibitor; H3K27me3.

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