黏着斑激酶及其小分子抑制剂作为抗肿瘤药物的研究进展  

Research Progress on Focal Adhesion Kinase and Its Small Molecule Inhibitors as Antitumor Agents

作　　者：杨超[1] 陈颖[1] 田巍[1] 朱驹[1] 

机构地区：[1]第二军医大学药学院药物化学教研室,上海200433

出　　处：《药学进展》2014年第9期649-655,共7页Progress in Pharmaceutical Sciences

摘　　要：抗黏着斑激酶是一种非受体型酪氨酸蛋白激酶,在许多肿瘤的发生和发展过程中均有过表达。研究表明,作为细胞内重要的骨架蛋白和调节多种细胞信号通路的关键分子,黏着斑激酶在肿瘤发生、发展、迁移和侵袭的各个阶段都起着重要作用。因此,以黏着斑激酶作为抗肿瘤靶点开发其抑制剂的研究受到广泛关注。综述黏着斑激酶的结构与功能、它与肿瘤的关联及其小分子抑制剂的研究与开发。Focal adhesion kinase（FAK） is a non-receptor tyrosine kinase overexpressed in the development and progression of many tumors. It has been suggested that as an important intracellular cytoskeletal protein and a key molecule in a variety of cell signal transduction pathways,FAK plays a signifi cant role in tumor cell survival,development,migration and invasion. Therefore,the researches on the development of FAK inhibitors as antitumor agents have attracted an extensive attention. The structure and function of FAK,its association with tumor and research and development of its small molecule inhibitors were reviewed.

关 键 词：黏着斑激酶 细胞信号通路 靶点 黏着斑激酶小分子抑制剂 抗肿瘤活性 

分 类 号：R96[医药卫生—药理学]