RSK2在肿瘤发生发展中作用及其抑制剂的研究进展  

Recent advances in role of RSK2 in tumorigenesis and its inhibitors

作　　者：李海啸 艾元宝 刘森 LI Haixiao;AI Yuanbao;LIU Sen(Cooperative Innovation Center of Industrial Fermentation(Ministry of Education&Hubei Province),School of Life and Health Sciences,School of Life and Health Sciences,Key Laboratory of Fermentation Engineering(Ministry of Education),School of Life and Health Sciences,Hubei Provincial Key Laboratory of Industrial Microbiology,School of Life and Health Sciences,Innovation Base for Cell Regulation and Molecular Pharmacology(111 Program),School of Life and Health Sciences,Hubei University of Technology,Wuhan 430068,China;Hubei WEL-SAFE Biotechnology Co.,Ltd.,Ezhou 436006,China)

机构地区：[1]湖北工业大学生命科学与健康工程学院,工业发酵省部共建协同创新中心,发酵工程教育部重点实验室,工业微生物湖北省重点实验室,国家细胞调控与分子药物学科创新引智基地(“111计划”),湖北武汉430068 [2]湖北微生元生物科技有限公司,湖北鄂州436006

出　　处：《中国病理生理杂志》2025年第4期775-782,共8页Chinese Journal of Pathophysiology

基　　金：国家自然科学基金资助项目(No.31971150);湖北省创新群体项目(No.2024AFA014);湖北省杰出青年基金资助项目(No.2019CFA069)。

摘　　要：核糖体S6激酶2(RSK2)作为RSK家族的重要成员,参与细胞增殖、转化、凋亡等活动。RSK2在多种癌症发生发展中起重要作用,已成为抗癌药物开发的潜在靶标,目前缺少有效抑制剂,仅有PMD-026一款抑制剂进入临床阶段。以往研究表明RSK2仅受MAPK信号通路调控,而最新研究显示AKT1也可激活RSK2。本文就RSK2蛋白的结构功能及其信号转导过程、RSK2与肿瘤发生发展关系、以及作用于RSK2不同位点抑制剂的研究现状和面临的挑战进行综述,旨在为RSK2抑制剂的开发提供参考。Ribosomal S6 kinase 2(RSK2),an important member of the RSK family,is involved in cell proliferation,transformation,apoptosis,and the cell cycle.It plays a pivotal role in the development and progression of various tumors,making it a promising target for anticancer drug development.To date,there is a notable paucity of effective inhibitors,with only one compound,PMD-026,having advanced to the clinical stage of testing.Earlier studies have suggested that RSK2 was regulated exclusively by MAPK,however recent research has shown that AKT1 also activates RSK2.This article provides an in-depth review of the structural and functional characteristics of the RSK2 protein,its signal transduction pathways,and the relationship between RSK2 and tumor development and progression.We also reviews the status of current research and the challenges associated with developing inhibitors that target different sites of RSK2.The objective was to provide valuable insights for the advancement of RSK2 inhibitors.

关 键 词：核糖体S6激酶2 信号通路 肿瘤 抑制剂 

分 类 号：R363[医药卫生—病理学] R730.23[医药卫生—基础医学] R393