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 s...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.展开更多
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)+5 种基金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).
文摘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.
