Treating human cancer by targeting EZH2  

作　　者：Mengfei Xu Chunyan Xu Rui Wang Qing Tang Qichun Zhou Wanyin Wu Xinliang Wan Handan Mo Jun Pan Sumei Wang 

机构地区：[1]The Second Clinical Medical College,Guangzhou University of Chinese Medicine,Guangzhou,Guangdong 510120,China [2]Department of Oncology,Clinical and Basic Research Team of TCM Prevention and Treatment of NSCLC,Guangdong Provincial Hospital of Chinese Medicine,The Second Clinical College of Guangzhou University of Chinese Medicine,Guangdong Provincial Key Laboratory of Clinical Research on Traditional Chinese Medicine Syndrome,State Key Laboratory of Dampness Syndrome of Chinese Medicine,Guangzhou,Guangdong 510120,China [3]Department of Urology,The Second Affiliated Hospital of Guangzhou University of Chinese Medicine,Guangzhou,Guangdong 510120,China

出　　处：《Genes & Diseases》2025年第3期205-218,共14页基因与疾病(英文)

基　　金：supported by grants from the Research Fund for Bajian Talents of Guangdong Provincial Hospital of Chinese Medicine(China)(No.BJ2022KY13);the National Natural Science Foundation of China(No.82274602);the Foundation for Basic and Applied Research of Guangdong Province,China(No.2021A1515220023,2017B030314166);the Chinese Medicine Science and Technology Research Project of Guangdong Provincial Hospital of Chinese Medicine(China)(No.YN2019QJ06);the Guangzhou Science and Technology Plan Project(Guangdong,China)(No.2024A03J0548,202201020349);the Key Project of State Key Laboratory of Dampness Syndrome of Chinese Medicine Jointly Built by Province and Ministry(China)(No.SZ2021ZZ38);Guangdong Provincial Key Laboratory of Chinese Medicine for Prevention and Treatment of Refractory Chronic Diseases(China)(No.YN2023MB09);the Guangdong Traditional Chinese Medicine Project(China)(No.20231094,20241135).

摘　　要：Enhancer of zeste homolog 2 (EZH2), an epigenetic regulator that primarily inhibitsdownstream gene expression by tri-methylating histone H3, which is usually overexpressed intumors and participates in many processes such as tumor occurrence and development, invasion, migration, drug resistance, and anti-tumor immunity as an oncogene, making it an important biomarker in cancer therapy. Collectively, several transcription factors and RNAscooperate to facilitate the elevated expression of EZH2 in cancer. Although the significanceof blocking EZH2 in cancer for inhibiting cancer progression is widely recognized, the clinicalapplication of EZH2 inhibitors continues to encounter numerous challenges. In this review,drawing upon our comprehensive understanding of the factual underpinnings of EZH2’s rolein cancer, we aim to clarify the crucial importance of targeting EZH2 in cancer treatment.Furthermore, we summarize the current research landscape surrounding targeted EZH2 inhibitors and offer insights into potential future applications of these inhibitors.

关 键 词：CANCER Epigenetic modification EZH2 EZH2 inhibitor H3K27me3 

分 类 号：R730.5[医药卫生—肿瘤]