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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 tumorigenesis and development. Blocking angiogenesis is an important method to target tumor therapy. One of the most important angiogenesis-inducing factors is vascular endothelial growth factor (VEGF), which is mainly associated with its receptor tyrosine kinase VEGFR-2 [also known as KDR, a type III receptor tyrosine kinase )], Activating downstream signaling pathways leading to increased vascular permeability and vascular proliferation. Therefore, the inhibition of VEGFR-2 phosphorylation of downstream substrates to block the proliferation of blood vessels has become an effective method of tumor therapy. This article describes the current research status of various inhibitors of VEGFR-2 from the aspects of structure, activity and their structure-activity relationship.