2. Academic Validation
  3. Targeting EZH2 for cancer therapy: From current progress to novel strategies

Targeting EZH2 for cancer therapy: From current progress to novel strategies

  • Eur J Med Chem. 2022 Aug 5:238:114419. doi: 10.1016/j.ejmech.2022.114419.
Jia Zeng 1,  Jifa Zhang 1,  Ying Sun 2,  Jiaxing Wang 3,  Changyu Ren 4,  Souvik Banerjee 5,  Liang Ouyang 1,  Yuxi Wang 6
Affiliations

Affiliations

  • 1 Targeted Tracer Research and Development Laboratory, Institute of Respiratory Health, Frontiers Science Center for Disease-related Molecular Network, Joint Research Institution of Altitude Health, National Clinical Research Center for Geriatrics, West China Hospital, Sichuan University, Chengdu, 610041, Sichuan, China; State Key Laboratory of Biotherapy and Cancer Center, Department of Respiratory and Critical Care Medicine, West China Hospital, Sichuan University, Chengdu, 610041, Sichuan, China.
  • 2 West China School of Pharmacy, Sichuan University, Chengdu, 610041, Sichuan, China.
  • 3 Department of Pharmaceutical Sciences, College of Pharmacy, University of Tennessee Health Science Center, Memphis, 38163, Tennessee, United States.
  • 4 Department of Pharmacy, Chengdu Fifth People's Hospital, Chengdu, 611130, Sichuan, China.
  • 5 Department of Physical Sciences, College of Arts and Sciences, University of Arkansas Fort Smith, Fort Smith, 72913, Arkansas, United States.
  • 6 Targeted Tracer Research and Development Laboratory, Institute of Respiratory Health, Frontiers Science Center for Disease-related Molecular Network, Joint Research Institution of Altitude Health, National Clinical Research Center for Geriatrics, West China Hospital, Sichuan University, Chengdu, 610041, Sichuan, China; State Key Laboratory of Biotherapy and Cancer Center, Department of Respiratory and Critical Care Medicine, West China Hospital, Sichuan University, Chengdu, 610041, Sichuan, China. Electronic address: yuxiwang@scu.edu.cn.
PMID: 35569264 DOI: 10.1016/j.ejmech.2022.114419
Abstract

EZH2, the catalytic subunit of PRC2, catalyzes histone H3 lysine 27 (H3K27) trimethylation to induce the agglutination of chromosomes and in turn represses the transcription of the target genes. Numerous reports indicate that EZH2 is overexpressed in a variety of malignant tumor tissues. Therefore, targeting EZH2 protein is a promising strategy for Cancer treatment. So far, many small molecule EZH2 specific inhibitors have entered clinical trials, but many of them harbored limited clinical efficacy. New technologies and methods are imperative to enhance the Anticancer activity of EZH2. In this review, the structure and biological functions of EZH2 protein will be reviewed. The internal relationship between EZH2 and various diseases will be expounded. The development status of specific inhibitors for EZH2, and the latest progress of new strategies such as drug combination, dual-target inhibitors, targeted protein degradation technology and protein-protein interactions (PPI) inhibitors will be emphatically summarized and analyzed.

Keywords

Drug combination; Dual-target inhibitors; EZH2; Novel strategies.

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