Di Stasi Rossella, De Rosa Lucia, D'Andrea Luca Domenico
Istituto di Biostrutture e Bioimmagini, CNR, 80131 Napoli, Italy.
Istituto di Scienze e Tecnologie Chimiche "G. Natta", CNR, 20131 Milano, Italy.
Pharmaceuticals (Basel). 2023 Jun 7;16(6):851. doi: 10.3390/ph16060851.
Vascular endothelial growth factor (VEGF) and its receptors (VEGFRs) play a main role in the regulation of angiogenesis and lymphangiogenesis. Furthermore, they are implicated in the onset of several diseases such as rheumatoid arthritis, degenerative eye conditions, tumor growth, ulcers and ischemia. Therefore, molecules able to target the VEGF and its receptors are of great pharmaceutical interest. Several types of molecules have been reported so far. In this review, we focus on the structure-based design of peptides mimicking VEGF/VEGFR binding epitopes. The binding interface of the complex has been dissected and the different regions challenged for peptide design. All these trials furnished a better understanding of the molecular recognition process and provide us with a wealth of molecules that could be optimized to be exploited for pharmaceutical applications.
血管内皮生长因子（VEGF）及其受体（VEGFRs）在血管生成和淋巴管生成的调节中起主要作用。此外，它们还与多种疾病的发生有关，如类风湿性关节炎、退行性眼部疾病、肿瘤生长、溃疡和缺血。因此，能够靶向VEGF及其受体的分子具有极大的药学研究价值。迄今为止，已报道了几种类型的分子。在本综述中，我们重点关注模拟VEGF/VEGFR结合表位的肽的基于结构的设计。已剖析了复合物的结合界面，并对肽设计的不同区域进行了挑战。所有这些试验都使我们对分子识别过程有了更好的理解，并为我们提供了大量可优化用于药学应用的分子。
