血管内皮生长因子受体及其小分子抑制剂的研究进展

目前抗血管生成治疗是抗肿瘤研究的热点.血管内皮生长因子(VEGF)是刺激血管生成的重要因子之一,血管内皮生长因子受体(VEGFR)在肿瘤新生血管中高表达,因此成为肿瘤靶向治疗的理想靶点.以VEGF、VEGFR为靶点的抗肿瘤药物除了常见的单克隆抗体药物阿伐斯汀外,小分子抑制剂舒尼替尼、索拉非尼等也已经广泛使用；另外,一些...

Advances in studies on vascular endothelial growth factor receptor and its small-molecule inhibitors

Recently, the anti-angiogenic therapy is a hot focus for antitumor research. The vascular endothelial growth factor (VEGF) is one of the most important angiogenesis stimulators. The vascular endothelial growth factor receptor (VEGFR) is high expressed in the new vessels of tumor tissues, so the antiangiogenic therapy aiming at VEGFR becomes an ideal treatment method. Besides the monoclonal antibody drug Avastin, the small-molecule inhibitors such as sunitinib and sorafenib are already widely used in the antitumor therapy aimed at VEGF and VEGFR. Moreover, it is also worth attention to some clinical drugs with potential market acceptance (vandetanib, cediranib, vatalanib, axtinib, et al). For the drugs on the market and VEGFR-targeted small-molecule inhibitors in clinical study, we roughly divided them into six kinds on structures including quinoline and quinazoline, pyridazine, indazole, imidazole, pyrrolo[2,3-d]pyrimidine, indole, and others. The recent studies of the biologyical function of VEGF and VEGFR and their representative small-molecule inhibitors are reviewed in this paper.