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摘要
传统的细胞毒性药物缺乏特异性,导致对肿瘤特异性蛋白具有高选择性的抗癌药物的开发。目标结构如EGFR O揭幕HER2允许新疗法的重点发展,并大力推进肿瘤治疗。肿瘤特异性高亲和力配体可通过噬菌体展示技术鉴定。表面、核糖体和mrna显示。这些技术使筛选巨大的库,从而提供了一个有价值的替代合理的药物开发。近年来,miniproteiNS和多环肽已成为这些图书馆的首选配体的表达。由于其良好的药代动力学及其易于合成,肽类配体克服缺点抗体衍生疗法的年龄。结构上由刚性支架定义的肽非常适合于显示技术的使用。这些分子具有很高的稳定性和Excel借给亲和力同时提供机会,随机化部分序列作为结合位点。肽支架的结构可以通过不同的方法实现,其中周期化是一种最常用的。最受青睐的环化策略是基于酰胺或二硫桥和使用人工合成的支架或化学连接。多肽的使用DES允许同时呈现几种不同的绑定循环。半合成的方法使非天然氨基酸的引入,增加产生的肽的多样性电子图书馆。鉴于此,小蛋白支架提供了一个广阔的应用潜力和促进新的高亲和力配体用于精确的诊断和高效的筛选有效的癌症治疗。
关键词: 药物开发,小蛋白支架,靶向治疗,肽库,显示技术性配体。
Current Medicinal Chemistry
Title:Multicyclic Peptides as Scaffolds for the Development of Tumor Targeting Agents
Volume: 24 Issue: 20
关键词: 药物开发,小蛋白支架,靶向治疗,肽库,显示技术性配体。
摘要: The lack of specificity of traditional cytotoxic drugs triggers the development of anticancer agents with high selectivity to tumor-specific proteins. The unveiling of target structures such as EGFR or Her2 allows the focused development of novel therapies and has strongly advanced tumor treatment. Tumor-specific high-affinity ligands can be identified by using display techniques such as phage, yeast surface, ribosome and mRNA display. These techniques enable the screening of huge libraries, consequently providing a valuable alternative to rational drug development. In recent years, miniproteins and multicyclic peptides have become the preferred ligands expressed by these libraries. Due to their favorable pharmacokinetics and the ease of their synthesis, peptidic ligands overcome disadvantages of antibody derived therapeutics. Peptides that are structurally defined by a rigid scaffold are ideally suited for the use in display techniques. These molecules feature high stability and excellent affinities while offering the opportunity to randomize partial sequences to be used as binding sites. Structurization of the peptide scaffold can be achieved by different approaches, of which cyclization is one of the most commonly used. The favored cyclization strategies are based on amide or disulfide bridging and the use of synthetic braces or chemical linkers. The use of multicyclic peptides allows the simultaneous presentation of several different binding loops. Semisynthetic approaches enable the introduction of unnatural amino acids, increasing the diversity of the resulting peptide libraries. Given that, miniprotein scaffolds offer a wide range of potential applications and facilitate efficient screening of novel high-affinity ligands to be used in precise diagnosis and highly efficient cancer therapy.
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Cite this article as:
Multicyclic Peptides as Scaffolds for the Development of Tumor Targeting Agents, Current Medicinal Chemistry 2017; 24 (20) . https://dx.doi.org/10.2174/0929867324666170316120304
DOI https://dx.doi.org/10.2174/0929867324666170316120304 |
Print ISSN 0929-8673 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-533X |
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