摘要
血管生成与肿瘤的发生发展密切相关,阻断血管生成是靶向治疗肿瘤的重要方法。最重要的血管生成诱导因子之一血管内皮生长因子(vascular endothelial growth factor,VEGF)在人体内主要与其受体酪氨酸激酶VEGFR-2[又称KDR,kinase insertdomain receptor(a type III receptor tyrosine kinase)]结合,激活下游信号通路而导致血管通透性增加以及血管的增生。因此,抑制VEGFR-2磷酸化下游底物来阻断血管的增殖已成为肿瘤治疗中的有效方法。本篇文章主要从化合物结构、活性及其构效关系方面阐述各类VEGFR-2小分子抑制剂的研究现状。
Angiogenesis is closely related to the development of tumors.Blocking angiogenesis is an attractive approach for the treatment of cancer.Vascular endothelial growth factor（VEGF） is one of the most important inducers,which causes vascular proliferation and vascular permeability to increase mainly by interacting with transmembrane tyrosine kinase receptor,VEGFR-2（KDR）,in human bodies.Inhibition of phosphorylation the downstream substrate of VEGFR-2 to block angiogenesis has already become an effective method.In this article we review the recent advances in small molecule VEGFR-2 inhibitors,and focus on the structure-activity relationships of VEGFR-2 inhibitors.
出处
《生命的化学》
CAS
CSCD
2012年第6期519-525,共7页
Chemistry of Life
基金
国家自然科学基金项目(21072115)资助
关键词
血管生成
血管内皮生长因子
血管内皮生长因子受体
酪氨酸激酶抑制剂
angiogenesis
vascular endothelial growth factor
vascular endothelial growth factor receptor tyrosine kinase inhibitor
