中国药科大学学报2025，Vol.56Issue(5)：548-556,9.DOI:10.11665/j.issn.1000-5048.2025021201
第二代蛋白精氨酸甲基转移酶5抑制剂的研究进展
Research progress on second-generation protein arginine methyltransferase 5 inhibitors
摘要
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.关键词
蛋白精氨酸甲基转移酶5/甲硫腺苷磷酸化酶/甲硫腺苷/合成致死Key words
protein arginine methyltransferase 5/methioadenosine phosphorylase/methylthioadenosine/synthetic lethal分类
医药卫生引用本文复制引用
胡浙棋,尹春香,毛慧欢,常艺清,朱启华,徐云根,龚国清,邹毅..第二代蛋白精氨酸甲基转移酶5抑制剂的研究进展[J].中国药科大学学报,2025,56(5):548-556,9.基金项目
This study was supported by the National Innovation and Entrepreneurship Training Program for Undergraduate(202510316012Z) 国家级大学生创新创业训练计划项目(202510316012Z) （202510316012Z）
