Teng Peng, Shi Yan, Sang Peng, Cai Jianfeng
Department of Chemistry, University of South Florida, 4202 E. Fowler Ave, Tampa, FL 33620, USA.
Chemistry. 2016 Apr 11;22(16):5458-66. doi: 10.1002/chem.201504936. Epub 2016 Mar 4.
Sequence-specific peptidomimetics are molecules that mimic the structure and function of peptides and proteins. With new backbones and molecular frameworks, peptidomimetics are of considerable interest in addressing challenges encountered in chemical biology and biomedical sciences. Based on the γ-PNA backbone, a new class of peptidomimetics - "γ-AApeptides" were recently developed. Both linear and cyclic γ-AApeptides can be synthesized with high efficiency. Compared with α-peptides, γ-AApeptides are resistant to enzymatic degradation, and amendable to diversification with a variety of chemical groups. Moreover, they could mimic primary and secondary structure, as well as the function of peptides, and show promise in biological applications, such as the development of new agents combating bacteria, cancer, and Alzheimer's disease. A few research outcomes of γ-AApeptides are highlighted in this Concept article, and a future perspective is also proposed.
序列特异性肽模拟物是一类模仿肽和蛋白质结构与功能的分子。凭借新的骨架和分子框架,肽模拟物在应对化学生物学和生物医学科学中遇到的挑战方面具有相当大的吸引力。基于γ-肽核酸骨架,最近开发了一类新型肽模拟物——“γ-氨基酸肽”。线性和环状γ-氨基酸肽都能高效合成。与α-肽相比,γ-氨基酸肽对酶促降解具有抗性,并且易于用各种化学基团进行多样化修饰。此外,它们能够模拟肽的一级和二级结构以及功能,在生物应用中展现出前景,例如开发对抗细菌、癌症和阿尔茨海默病的新型药物。本概念文章重点介绍了γ-氨基酸肽的一些研究成果,并提出了未来展望。