Group Ⅱ p21-activated kinases as therapeutic targets in gastrointestinal cancer  

作　　者：Yang-Guang Shao Ke Ning Feng Li 

机构地区：[1]Department of Cell Biology,Key Laboratory of Cell Biology,Ministry of Public Health and Key Laboratory of Medical Cell Biology,Ministry of Education,China Medical University

出　　处：《World Journal of Gastroenterology》2016年第3期1224-1235,共12页世界胃肠病学杂志（英文版）

基　　金：Supported by National Natural Science Foundation of China;No.90813038;No.31271389;No.31371424;No.31171360 and No.81230077

摘　　要：P21-activated kinases(PAKs) are central players in various oncogenic signaling pathways. The six PAK family members are classified into group Ⅰ(PAK1-3) and group Ⅱ(PAK4-6). Focus is currently shifting from group Ⅰ PAKs to group Ⅱ PAKs. Group Ⅱ PAKs play important roles in many fundamental cellular processes, some of which have particular significance in the development and progression of cancer. Because of their important functions, group Ⅱ PAKs have become popular potential drug target candidates. However, few group Ⅱ PAKs inhibitors have been reported, and most do not exhibit satisfactory kinase selectivity and "drug-like" properties. Isoform- and kinase-selective PAK inhibitors remain to be developed. This review describes the biological activities of group Ⅱ PAKs, the importance of group Ⅱ PAKs in the development and progression of gastrointestinal cancer, and smallmolecule inhibitors of group Ⅱ PAKs for the treatment of cancer.P21-activated kinases(PAKs) are central players in various oncogenic signaling pathways. The six PAK family members are classified into group Ⅰ(PAK1-3) and group Ⅱ(PAK4-6). Focus is currently shifting from group Ⅰ PAKs to group Ⅱ PAKs. Group Ⅱ PAKs play important roles in many fundamental cellular processes, some of which have particular significance in the development and progression of cancer. Because of their important functions, group Ⅱ PAKs have become popular potential drug target candidates. However, few group Ⅱ PAKs inhibitors have been reported, and most do not exhibit satisfactory kinase selectivity and 'drug-like' properties. Isoform- and kinase-selective PAK inhibitors remain to be developed. This review describes the biological activities of group Ⅱ PAKs, the importance of group Ⅱ PAKs in the development and progression of gastrointestinal cancer, and smallmolecule inhibitors of group Ⅱ PAKs for the treatment of cancer.

关 键 词：GROUP Ⅱ p21-activated KINASES SIGNALINGPATHWAY GASTROINTESTINAL cancer PAK4 INHIBITOR Drugtarget 

分 类 号：R735[医药卫生—肿瘤]