D'Andrea Luca D, Del Gatto Annarita, De Rosa Lucia, Romanelli Alessandra, Pedone Carlo
Dipartimento delle Scienze Biologiche, Facoltà di Scienze Biotecnologiche, Università di Napoli Federico II, via Mezzocannone 16, 80134 Napoli, Italy.
Curr Pharm Des. 2009;15(21):2414-29. doi: 10.2174/138161209788682235.
Growth factors (GFs) are extracellular signaling polypeptides regulating cell proliferation, differentiation and survival. They exert a wide spectrum of biological activities selectively binding to and activating specific membrane receptors which then transfer the message to cell interior inducing specific biochemical pathways. GFs are especially involved in the regulation of angiogenesis, a physiological process underlining several pathologies. Molecules able to modulate angiogenesis, interfering with the molecular recognition between a GF and its receptor, have a big pharmacologic interest. Either GF and the receptor are potential drug target. Peptides are useful molecules to develop new lead compounds disrupting protein-protein interface for pharmacological applications. In this review we describe peptides targeting the receptors of the pro-angiogenic growth factors FGF, PDGF and VEGF. The biological function and the structure of each growth factor/receptor system are discussed, as well as the molecular interaction between peptides and the receptors. Finally, we highlight the pharmacological and diagnostic applications of these peptides in angiogenesis related diseases.
生长因子（GFs）是调节细胞增殖、分化和存活的细胞外信号多肽。它们发挥广泛的生物学活性，选择性地结合并激活特定的膜受体，然后将信息传递到细胞内部，诱导特定的生化途径。生长因子尤其参与血管生成的调节，这是一种在多种病理过程中起重要作用的生理过程。能够调节血管生成、干扰生长因子与其受体之间分子识别的分子具有很大的药理学研究价值。生长因子及其受体都是潜在的药物靶点。肽是开发新型先导化合物的有用分子，这些化合物可破坏蛋白质 - 蛋白质界面以用于药理学应用。在本综述中，我们描述了靶向促血管生成生长因子FGF、PDGF和VEGF受体的肽。讨论了每个生长因子/受体系统的生物学功能和结构，以及肽与受体之间的分子相互作用。最后，我们强调了这些肽在血管生成相关疾病中的药理学和诊断应用。
