Borghouts Corina, Kunz Christian, Groner Bernd
Georg-Speyer-Haus Institute for Biomedical Research, Paul-Ehrlich-Strasse 42-44, D-60596 Frankfurt am Main, Germany.
Expert Opin Biol Ther. 2005 Jun;5(6):783-97. doi: 10.1517/14712598.5.6.783.
During the past two decades, our understanding of oncogenesis has advanced considerably and many new signalling pathways have been identified. Differences in signalling events that distinguish normal cells from tumour cells provide new targets for the development of anticancer agents. Peptide aptamers are small peptide sequences that have been selected to recognise a predetermined target protein domain and are potentially able to interfere with its function. They represent useful molecules for manipulating protein function in vivo. The isolation and use of specific peptide aptamers as inhibitors of individual signalling components, essential in cancer development and progression, provides a new challenge for drug development. Although peptides make up only a small fraction of current therapeutics, their potential is being enhanced by new developments affecting their modification, stability, delivery and their successful application in preclinical settings. This review summarises the methods that can be used for the isolation and delivery of peptide aptamers, as well as the important achievements that have been made using such peptide aptamers in different systems. The applicability of peptide aptamers as novel cancer therapeutics will be discussed.
在过去二十年中,我们对肿瘤发生的理解有了显著进展,并且已经鉴定出许多新的信号通路。区分正常细胞与肿瘤细胞的信号事件差异为抗癌药物的开发提供了新靶点。肽适配体是经过筛选以识别预定靶蛋白结构域的小肽序列,并且有可能干扰其功能。它们是在体内操纵蛋白质功能的有用分子。分离和使用特定肽适配体作为癌症发生和发展中必不可少的单个信号成分的抑制剂,为药物开发带来了新挑战。尽管肽仅占当前治疗药物的一小部分,但影响其修饰、稳定性、递送的新进展以及它们在临床前环境中的成功应用正在增强其潜力。本综述总结了可用于分离和递送肽适配体的方法,以及在不同系统中使用此类肽适配体所取得的重要成果。还将讨论肽适配体作为新型癌症治疗药物的适用性。