Ⅱ型p21激活激酶在肿瘤中的调节作用及其抑制剂研究进展  

Research Progress of Regulatory Role of GroupⅡp21-Activated Kinases in Cancer and the Development of the Inhibitors

作　　者：牟杰 李龙宝 孟思寒 裴冬生 MOU Jie;LI Longbao;MENG Sihan;PEI Dongsheng(Xuzhou Medical University,School of Pharmacy,Xuzhou 221004,China;Xuzhou Medical University,Jiangsu Key Laboratory of New drug and Clinical Pharmacy,Xuzhou 221004,China;Xuzhou Medical University,Department of Pathology,Xuzhou 221004,China)

机构地区：[1]徐州医科大学,药学院,江苏徐州221004 [2]徐州医科大学,江苏省新药研究与临床药学重点实验室,江苏徐州221004 [3]徐州医科大学,病理学教研室,江苏徐州221004

出　　处：《中国现代应用药学》2021年第20期2608-2615,共8页Chinese Journal of Modern Applied Pharmacy

基　　金：国家自然科学基金项目(81872080,81572349);江苏省自然科学基金项目(BK20181148);徐州市推动科技创新项目(KC20245);江苏省研究生科研创新计划(KYCX20_2510);江苏省高等学校大学生实践创新训练计划(201910313073Y,201910313098H)。

摘　　要：p21激活激酶(p21-activated kinases,PAKs)是小GTP酶Rho家族的成员Rac和Cdc42的下游靶蛋白,参与调节细胞骨架重构和细胞运动等多种生物功能。PAKs家族分为Ⅰ型PAKs(PAK1~3)和Ⅱ型PAKs(PAK4~6),其中Ⅱ型PAKs在多种肿瘤中高表达,并与肿瘤的发生和预后密切相关。Ⅱ型PAKs对肿瘤的增殖、凋亡、侵袭和转移起到重要的调控作用,成为有研发前途的抗肿瘤靶点。本文从Ⅱ型PAKs在肿瘤领域的研究进展及其抑制剂在肿瘤中的作用进行综述,期望为开发选择性Ⅱ型PAKs抑制剂提供参考。p21-activated kinases(PAKs)are important downstream effector molecules of the small G protein RHO family Rac and Cdc42 which involved in regulating various biological functions such as cytoskeletal remodeling and cell movement.The human PAKs family can be divided into two types:typeⅠPAKs(PAK1-3)and typeⅡPAKs(PAK4-6),in which typeⅡPAKs are highly expressed in various tumors and are closely related to the occurrence and prognosis of tumors.TypeⅡPAKs play the vital role in the regulation of tumor proliferation,apoptosis,invasion and metastasis,and become a promising anti-tumor target.Herein,the research progress of typeⅡPAKs in oncology and the roles of their inhibitors in cancer were reviewed,expecting to develop selective typeⅡPAKs inhibitors.

关 键 词：Ⅱ型p21激活激酶 肿瘤 抑制剂 亚型选择性 

分 类 号：R966[医药卫生—药理学]