小分子酪氨酸激酶抑制剂在癌症靶向治疗的研究进展  

Advances in Research of Small Molecule Tyrosine Kinase Inhibitors for Targeted Cancer Therapy

作　　者：宋艳宁 张赫然[2] 尹东东[2] 宋丽明[2] 王杏林[2] 张艺卓[1,2] 陈永超[1] 

机构地区：[1]河南大学药学院,河南开封475001 [2]天津药物研究院有限公司,释药技术与药代动力学国家重点实验室,天津300193

出　　处：《中国药学杂志》2016年第3期165-171,共7页Chinese Pharmaceutical Journal

基　　金：国家“十二五重大新药创制”科技重大专项课题资助项目(2014ZX09507005-002)

摘　　要：查阅国内外相关文献,根据不同作用靶点及相关癌症将已经成功上市和处于研发阶段的酪氨酸激酶抑制剂进行分类整理与总结,综述小分子酪氨酸激酶抑制剂的研究进展。小分子酪氨酸激酶抑制剂通过特异性地与胞内酪氨酸激酶催化区结合,抑制其催化活性,阻断细胞增殖信号,一些已应用在癌症治疗或处于临床开发的各个阶段,具有良好的应用前景。To review the research progress of small molecule tyrosine kinase inhibitors （TKIs）. Literatures on tyrosine kinase inhibitors which have already been successfully marketed or are in development were sorted and summarized according to the targets and related cancers. Through binding to catalytic domain of intracellular tyrosine kinase, small molecule TKIs inhibit the catalytic activity specifically and block cell proliferation signals, and some of them have already been used in cancer therapy or are in different stages of clinical development, showing good prospects.

关 键 词：癌症 酪氨酸激酶抑制剂(TKI) 小分子抑制剂 靶点 

分 类 号：R946[医药卫生—药剂学]