Guryanov Ivan, Tennikova Tatiana, Urtti Arto
Institute of Chemistry, St. Petersburg State University, Universitetsky pr. 26, Peterhof, 198504 St. Petersburg, Russia.
Division of Pharmaceutical Biosciences, University of Helsinki, Viikinkaari 5 E, 00014 Helsinki, Finland.
Pharmaceutics. 2021 Aug 26;13(9):1337. doi: 10.3390/pharmaceutics13091337.
Vascular endothelial growth factors (VEGFs) are the family of extracellular signaling proteins involved in the processes of angiogenesis. VEGFA overexpression and altered regulation of VEGFA signaling pathways lead to pathological angiogenesis, which contributes to the progression of various diseases, such as age-related macular degeneration and cancer. Monoclonal antibodies and decoy receptors have been extensively used in the anti-angiogenic therapies for the neutralization of VEGFA. However, multiple side effects, solubility and aggregation issues, and the involvement of compensatory VEGFA-independent pro-angiogenic mechanisms limit the use of the existing VEGFA inhibitors. Short chemically synthesized VEGFA binding peptides are a promising alternative to these full-length proteins. In this review, we summarize anti-VEGFA peptides identified so far and discuss the molecular basis of their inhibitory activity to highlight their pharmacological potential as anti-angiogenic drugs.
血管内皮生长因子（VEGFs）是参与血管生成过程的细胞外信号蛋白家族。VEGFA的过表达和VEGFA信号通路调节的改变会导致病理性血管生成，这促进了各种疾病的进展，如年龄相关性黄斑变性和癌症。单克隆抗体和诱饵受体已广泛用于抗血管生成治疗中以中和VEGFA。然而，多种副作用、溶解性和聚集问题以及补偿性VEGFA非依赖性促血管生成机制的参与限制了现有VEGFA抑制剂的使用。化学合成的短VEGFA结合肽是这些全长蛋白的一种有前景的替代物。在本综述中，我们总结了迄今为止鉴定出的抗VEGFA肽，并讨论了它们抑制活性的分子基础，以突出其作为抗血管生成药物的药理学潜力。
