血管内皮生长因子受体酪氨酸激酶抑制剂的研究进展  

Advances in the inhibitors of vascular endothelial growth factor receptor tyrosine kinase

作　　者：茆勇军[1] 张佩璇[1] 田广辉 王震[1] 沈敬山[1] 

机构地区：[1]中国科学院上海药物研究所,上海201203 [2]上海特化医药科技有限公司,上海201209

出　　处：《中国新药杂志》2008年第7期544-550,共7页Chinese Journal of New Drugs

摘　　要：血管生成在肿瘤的生长、转移和演进中起着非常重要的作用。文中简要阐述了血管内皮生长因子受体(VEGFR)酪氨酸激酶介导的RAS/Raf/MAPK,PI3K/AKT,PLC-γ及Src信号转导途径,根据结构类型统计和介绍了已经上市或处于临床研究的VEGFR酪氨酸激酶小分子抑制剂,包括吲哚酮类、喹唑啉类、哒嗪类、吲唑类、烟碱类和吡咯并嘧啶类等典型结构,分别阐述了这几类结构中代表性化合物的临床前研究和临床研究的数据。Angiogenesis is critical to the growth, metastasis and progression of solid tumors. In this review, the RAS/Raf/MAPK, PI3K/AKT, PLC-γ and Src signal pathways operated by vascular endothelial growth factor receptor （VEGFR） tyrosine kinases was briefly illuminated, and several small-molecular VEGFR tyrosine kinase inhibitors （TKIs, some of which are approved） were summarized. According to different structures, TKIs inelude indolinones, quinazolines, phthalazines, indazoles, nicotinamides, pyrrolopyrimidines and so on. The preclinical and clinical research data of some representative compounds are depicted in this review.

关 键 词：信号转导 肿瘤血管生成 血管内皮生长因子受体 酪氨酸激酶抑制剂 抗肿瘤药物 

分 类 号：R979.1[医药卫生—药品]