Innovative peptide architectures: advancements in foldamers and stapled peptides for drug discovery.

IF 6 2区 医学 Q1 PHARMACOLOGY & PHARMACY
Expert Opinion on Drug Discovery Pub Date : 2024-06-01 Epub Date: 2024-05-16 DOI:10.1080/17460441.2024.2350568
Zhou Dongrui, Maho Miyamoto, Hidetomo Yokoo, Yosuke Demizu
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引用次数: 0

Abstract

Introduction: 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.

Areas covered: 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.

Expert opinion: 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.

创新肽结构:折叠肽和钉肽在药物发现方面的进展。
简介:肽折叠体在药物研究和生物医学应用中发挥着至关重要的作用。这篇综述重点介绍了新型折叠器、合成技术及其在药物研究中应用的最新进展(2020 年以后):作者总结了α、β、γ-肽、碳氢叠层肽、脲型折叠剂、磺酸-γ-氨基酸折叠剂、芳香族折叠剂和类佩妥类等多肽折叠剂的结构和应用,这些折叠剂解决了传统多肽药物的难题。在抗菌方面,折叠酰胺在对抗耐药细菌的潜力方面取得了进展。在药物开发方面,多肽折叠物已被用作药物输送系统(DDS)和蛋白质-蛋白质相互作用(PPI)抑制剂:这些结构具有抗酶降解性,有望用于治疗给药,并以特异性、多功能性和稳定性破坏与癌症等疾病相关的关键 PPI,这些都是有用的治疗特性。然而,由于其合成过程复杂、成本高昂,而且必须进行全面的安全性和有效性评估,因此有必要开展广泛的研究和跨部门合作。合成方法、计算建模和靶向递送系统的进步对于充分发挥折叠剂的治疗潜力并将其纳入主流医疗方法至关重要。
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来源期刊
CiteScore
10.20
自引率
1.60%
发文量
78
审稿时长
6-12 weeks
期刊介绍: Expert Opinion on Drug Discovery (ISSN 1746-0441 [print], 1746-045X [electronic]) is a MEDLINE-indexed, peer-reviewed, international journal publishing review articles on novel technologies involved in the drug discovery process, leading to new leads and reduced attrition rates. Each article is structured to incorporate the author’s own expert opinion on the scope for future development. The Editors welcome: Reviews covering chemoinformatics; bioinformatics; assay development; novel screening technologies; in vitro/in vivo models; structure-based drug design; systems biology Drug Case Histories examining the steps involved in the preclinical and clinical development of a particular drug The audience consists of scientists and managers in the healthcare and pharmaceutical industry, academic pharmaceutical scientists and other closely related professionals looking to enhance the success of their drug candidates through optimisation at the preclinical level.
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