Department of Neurosurgery, The First Affiliated Hospital of Medical College of Xi'an Jiaotong University, Xi'an 710061, Shaanxi Province, China.
Peptides. 2012 Dec;38(2):457-62. doi: 10.1016/j.peptides.2012.09.007. Epub 2012 Sep 14.
Anginex, a novel artificial cytokine-like peptide (βpep-25), is designed by using basic folding principles and incorporating short sequences from the β-sheet domains of anti-angiogenic agents, including platelet factor-4 (PF4), interleukin-8 (IL-8), and bactericidal-permeability increasing protein 1 (BP1). Anginex can specially block the adhesion and migration of the angiogenically activated endothelial cells (ECs), leading to apoptosis and ultimately to the inhibition of angiogenesis and tumor growth. In vitro and in vivo studies have proved its inhibitory effects on the formation of new blood vessels and tumor growth even though the mechanism is not clear. The inhibitory effects of anginex can be enhanced when it is applied in combination with other therapies, such as chemotherapy, radiotherapy and other anti-angiogenic agents. The limitations of anginex, including poor stability, short half life, complicated synthesis and low purity, have been conquered by modifying its structure or designing novel compound anginex and recombinant anginex, which makes possible the clinical application of anginex. Here, we summarize the basic and preclinical trials of anginex and discuss the prospects of anginex in clinical application. We come to the conclusion that anginex and compound or recombinant anginex can be used as effective anti-angiogenic agents.
安格宁是一种新型的人工细胞因子样肽（βpep-25），它是利用基本折叠原理设计的，并结合了抗血管生成剂（包括血小板因子-4（PF4）、白细胞介素-8（IL-8）和杀菌通透性增加蛋白 1（BP1）的β-折叠结构域中的短序列。安格宁可以特异性地阻断血管生成激活的内皮细胞（ECs）的黏附和迁移，导致细胞凋亡，最终抑制血管生成和肿瘤生长。体外和体内研究已经证明了它对新血管形成和肿瘤生长的抑制作用，尽管其机制尚不清楚。当与其他治疗方法（如化疗、放疗和其他抗血管生成剂）联合应用时，安格宁的抑制作用可以增强。安格宁的局限性，包括稳定性差、半衰期短、合成复杂和纯度低，已经通过修饰其结构或设计新型的复合安格宁和重组安格宁来克服，这使得安格宁有可能在临床上应用。在这里，我们总结了安格宁的基础和临床前试验，并讨论了安格宁在临床应用中的前景。我们得出结论，安格宁和复合或重组安格宁可以作为有效的抗血管生成剂。
