Inhibition of vascular endothelial growth factor (VEGF) or its corresponding receptor (VEGFR) has been validated as an efficacious antiangiogenetic approach for cancer treatment. More recently, neuropilins (NRPs), the essential coreceptors for VEGF, have also been shown to have a significant role in VEGF signaling. Given the multifaceted effects of VEGF–NRP interactions on tumor initiation and progression, the exploration of new chemical entities that selectively block these interactions has recently attracted considerable interest as a novel antitumor strategy. Here, we summarize the biological functions of VEGF–NRP interactions in tumor biology, analyze the structural basis for these interactions, and present a detailed discussion of the development of the NRP antagonists reported so far.

抑制血管内皮生长因子（VEGF）或其相应的受体（VEGFR）已被证实是一种有效的抗血管生成方法，可用于治疗癌症。最近，神经纤维蛋白（NRP），即VEGF的必需共受体，也已显示在VEGF信号传导中具有重要作用。考虑到VEGF-NRP相互作用对肿瘤发生和发展的多方面影响，作为一种新型的抗肿瘤策略，对选择性阻断这些相互作用的新化学实体的探索最近引起了极大的兴趣。在这里，我们总结了VEGF-NRP相互作用在肿瘤生物学中的生物学功能，分析了这些相互作用的结构基础，并提出了迄今为止报道的NRP拮抗剂发展的详细讨论。