肽折叠体在药物研究和生物医学应用中起着至关重要的作用。这篇评论强调了新型文件夹的最新(2020年后)进展,合成技术,及其在药物研究中的应用。
■作者总结了诸如α,β,γ-肽,碳氢化合物束缚肽,尿素型折叠器,磺酸-γ-氨基酸折叠剂,芳香折叠器,和拟肽,解决传统多肽药物的挑战。关于抗菌药物的使用,foldamers在对抗耐药细菌的潜力方面已经显示出进展。在药物开发中,肽折叠剂已被用作药物递送系统(DDS)和蛋白质-蛋白质相互作用(PPI)抑制剂。
■这些结构表现出对酶降解的抗性,有希望用于治疗性输送,并破坏与癌症等疾病相关的关键PPI,多功能性,和稳定性,这是有用的治疗特性。然而,它们合成的复杂性和成本,以及全面的安全性和有效性评估的必要性,需要广泛的研究和跨部门合作。合成方法的进展,计算建模,和靶向递送系统对于充分实现foldamers的治疗潜力并将其整合到主流医学治疗中至关重要。
UNASSIGNED: Peptide foldamers play a critical role in pharmaceutical research and biomedical applications. This review highlights recent (post-2020) advancements in novel foldamers, synthetic techniques, and their applications in pharmaceutical research.
UNASSIGNED: The authors summarize the structures and applications of peptide foldamers such as α, β, γ-peptides, hydrocarbon-stapled peptides, urea-type foldamers, sulfonic-γ-amino acid foldamers, aromatic foldamers, and peptoids, which tackle the challenges of traditional peptide drugs. Regarding antimicrobial use, foldamers have shown progress in their potential against drug-resistant bacteria. In drug development, peptide foldamers have been used as drug delivery systems (DDS) and protein-protein interaction (PPI) inhibitors.
UNASSIGNED: These structures exhibit resistance to enzymatic degradation, are promising for therapeutic delivery, and disrupt crucial PPIs associated with diseases such as cancer with specificity, versatility, and stability, which are useful therapeutic properties. However, the complexity and cost of their synthesis, along with the necessity for thorough safety and efficacy assessments, necessitate extensive research and cross-sector collaboration. Advances in synthesis methods, computational modeling, and targeted delivery systems are essential for fully realizing the therapeutic potential of foldamers and integrating them into mainstream medical treatments.