1.Research progress on second-generation protein arginine methyltransferase 5 inhibitors
Zheqi HU ; Chunxiang YIN ; Huihuan MAO ; Yiqing CHANG ; Qihua ZHU ; Yungen XU ; Guoqing GONG ; Yi ZOU
Journal of China Pharmaceutical University 2025;56(5):548-556
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.
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