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

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资源类型：
Pubmed体系：
作者：
Zeng Jia[1,2] * ; Zhang Jifa[1,2] * ; Sun Ying[4] ; Wang Jiaxing[5] ; Ren Changyu[3] ; Banerjee Souvik[6] ; Ouyang Liang[1,2] ; Wang Yuxi[1,2,*1] ;
机构： [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 [2]State Key Laboratory of Biotherapy and Cancer Center, Department of Respiratory and Critical Care Medicine, West China Hospital, Sichuan University, Chengdu, 610041, Sichuan, China [3]Department of Pharmacy, Chengdu Fifth People’s Hospital, Chengdu, 611130, Sichuan, China [4]West China School of Pharmacy, Sichuan University, Chengdu, 610041, Sichuan, China [5]Department of Pharmaceutical Sciences, College of Pharmacy, University of Tennessee Health Science Center, Memphis, 38163, Tennessee, United States [6]Department of Physical Sciences, College of Arts and Sciences, University of Arkansas Fort Smith, Fort Smith, 72913, Arkansas, United States
出处：
DOI： 10.1016/j.ejmech.2022.114419
ISSN：

关键词： EZH2 Dual-target inhibitors Drug combination Novel strategies

摘要：
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.Copyright © 2022 Elsevier Masson SAS. All rights reserved.

基金：
Sichuan Science and Technology Program (2019YFS0003), National Natural Science Foundation of China (82073318, 81922064, 81903502), National Major Scientific and Technological Special Project for Significant New Drugs Development (2018ZX09201018-021), Health Commission of Sichuan Province (21PJ149) and Xinglin Foundation of Chengdu University of TCM (YYZX2021043).
语种：
外文
PubmedID：
中科院(CAS)分区：
出版当年[2022]版：
大类 | 1 区 医学
小类 | 1 区 药物化学
最新[2023]版：
大类 | 2 区 医学
小类 | 1 区 药物化学
第一作者：
第一作者机构： [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 [2]State Key Laboratory of Biotherapy and Cancer Center, Department of Respiratory and Critical Care Medicine, West China Hospital, Sichuan University, Chengdu, 610041, Sichuan, China
共同第一作者：
通讯作者：
通讯机构： [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 [2]State Key Laboratory of Biotherapy and Cancer Center, Department of Respiratory and Critical Care Medicine, West China Hospital, Sichuan University, Chengdu, 610041, Sichuan, China [*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
推荐引用方式(GB/T 7714)：
Zeng Jia,Zhang Jifa,Sun Ying,et al.Targeting EZH2 for cancer therapy: From current progress to novel strategies.[J].European journal of medicinal chemistry.2022,238:114419.doi:10.1016/j.ejmech.2022.114419.
APA：
Zeng Jia,Zhang Jifa,Sun Ying,Wang Jiaxing,Ren Changyu...&Wang Yuxi.(2022).Targeting EZH2 for cancer therapy: From current progress to novel strategies..European journal of medicinal chemistry,238,
MLA：
Zeng Jia,et al."Targeting EZH2 for cancer therapy: From current progress to novel strategies.".European journal of medicinal chemistry 238.(2022):114419

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