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具有化疗潜力的小分子抗真菌肽的研究综述。

Survey of small antifungal peptides with chemotherapeutic potential.

机构信息

Biomedical Sciences Research Complex, University of St Andrews, School of Biology, The North Haugh, St Andrews, Fife KY16 9ST. UK.

出版信息

Curr Pharm Biotechnol. 2011 Aug;12(8):1263-91. doi: 10.2174/138920111796117265.

Abstract

Many cationic peptides with antimicrobial properties have been isolated from bacteria, fungi, plants, and animals. These peptides vary in molecular size, potency and spectra of activities. This report surveyed the literature to highlight the peptides that have antifungal activity and greatest potential for development as new therapeutic agents. Thus, to be included in the evaluation, each peptide had to fulfil the following criteria: (i) potent antifungal activity, (ii) no, or minimal, mammalian cell toxicity, (iii) of ≤25 amino acids in length, which minimises the costs of synthesis, reduces immunogenicity and enhances bioavailability and stability in vivo, (iv) minimal post-translational modifications (also reduces the production costs). The ~80 peptides that satisfied these criteria are discussed with respect to their structures, mechanisms of antimicrobial action and in vitro and in vivo toxicities. Certainly, some of these small peptides warrant further study and have potential for future exploitation as new antifungal agents.

摘要

许多具有抗菌特性的阳离子肽已从细菌、真菌、植物和动物中分离出来。这些肽在分子大小、效力和活性谱方面存在差异。本报告综述了文献,以突出具有抗真菌活性和最大开发潜力的肽,作为新的治疗剂。因此,要包括在评估中,每个肽都必须满足以下标准:(i)具有强大的抗真菌活性,(ii)对哺乳动物细胞无毒性或毒性最小,(iii)长度≤25 个氨基酸,这最大限度地降低了合成成本,降低了免疫原性,并增强了体内的生物利用度和稳定性,(iv)最小的翻译后修饰(也降低了生产成本)。满足这些标准的约 80 种肽讨论了它们的结构、抗菌作用机制以及体外和体内的毒性。当然,其中一些小肽值得进一步研究,并有可能作为新的抗真菌剂进行未来开发。

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