Pini Alessandro, Falciani Chiara, Bracci Luisa
Dipartimento di Biologia Molecolare, Università degli Studi di Siena, Via Fiorentina 1, Siena, Italy.
Curr Protein Pept Sci. 2008 Oct;9(5):468-77. doi: 10.2174/138920308785915227.
The concept of 'magic bullet', initially ascribed to immunoglobulins by Paul Ehrlich at the beginning of the 20th century and strengthened by the hybridoma technology of Kohler and Milstein in the mid 70s, can nowadays be attributed to different target-specific molecules, such as peptides. This attribution is increasingly valid in light of the explosion of new technologies for peptide library construction and screening, not to mention improvements in peptide synthesis and conjugation and in-vivo peptide stability, which make peptide molecules specific bullets for targeting pathological markers and pathogens. Today, hundreds of peptides are being developed and dozens are in clinical trials for a variety of diseases, demonstrating that the general reluctance towards peptide drugs that existed a decade ago has now been overcome. In spite of this progress, the development of new peptide drugs has largely been limited by their short half-life. Branched peptides such as Multiple Antigen Peptides (MAPs) were invented in the 80s by Tam [Tam, J.P., (1998) Proc. Natl. Acad. Sci. USA, 85, 5409] and have been extensively tested to reproduce single epitopes to stimulate the immune system for new vaccine discovery. In our lab we discovered that MAP molecules acquire strong resistance to proteases and peptidases. This resistance renders MAPs very stable and thus suitable for drug development. Here we report our experience with several MAP molecules in different biotechnological applications ranging from antimicrobial and anti toxin peptides to peptides for tumor targeting.
“神奇子弹”的概念最初在20世纪初由保罗·埃尔利希归因于免疫球蛋白,并在70年代中期由科勒和米尔斯坦的杂交瘤技术得到强化,如今可归因于不同的靶向特异性分子,如肽。鉴于肽库构建和筛选新技术的爆炸式发展,这种归因越来越合理,更不用说肽合成与偶联以及体内肽稳定性方面的改进了,这些使得肽分子成为靶向病理标志物和病原体的特异性子弹。如今,数百种肽正在研发中,数十种肽正处于针对各种疾病的临床试验阶段,这表明十年前对肽类药物普遍存在的抵触情绪现已被克服。尽管取得了这一进展,但新肽类药物的开发在很大程度上受到其半衰期短的限制。诸如多抗原肽(MAPs)之类的分支肽是由谭(Tam, J.P., (1998) Proc. Natl. Acad. Sci. USA, 85, 5409)在8阗年代发明的,并已被广泛测试以重现单个表位,从而刺激免疫系统以发现新疫苗。在我们实验室,我们发现MAP分子对蛋白酶和肽酶具有很强的抗性。这种抗性使MAPs非常稳定,因此适合用于药物开发。在此,我们报告我们在不同生物技术应用中使用几种MAP分子的经验,这些应用范围从抗菌和抗毒素肽到肿瘤靶向肽。