Research progress on second-generation protein arginine methyltransferase 5 inhibitors
10.11665/j.issn.1000-5048.2025021201
- VernacularTitle:第二代蛋白精氨酸甲基转移酶5抑制剂的研究进展
- Author:
Zheqi HU
1
;
Chunxiang YIN
;
Huihuan MAO
;
Yiqing CHANG
;
Qihua ZHU
;
Yungen XU
;
Guoqing GONG
;
Yi ZOU
Author Information
1. 中国药科大学药学院, 南京 211198
- Publication Type:Journal Article 期刊文章
- Keywords:
protein arginine methyltransferase 5;
methioadenosine phosphorylase;
methylthioadenosine;
synthetic lethal
- From:
Journal of China Pharmaceutical University
2025;56(5):548-556
- CountryChina
- Language:Chinese
-
Abstract:
Protein arginine methyltransferase 5 (PRMT5) exhibits elevated expression levels in a variety of cancers and has emerged as a critical target for cancer therapy in recent years. However, first-generation PRMT5 inhibitors have exhibited inadequate selectivity, leading to significant hematological toxicity, thus limiting their clinical utility. The second-generation PRMT5 inhibitors have shown marked improvement in safety and efficacy by selectively targeting MTAP-null tumor cells without impacting normal cells. This review systematically summarizes the biological and functional roles of PRMT5 in MTAP-deficient tumor cells, and comprehensively analyzes the research and development process, molecular binding mechanisms, and the latest advancements in clinical trials of the five second-generation PRMT5 inhibitors currently under investigation, aiming to provide valuable insights for further in-depth studies in this field.
