关键词: N-methylation cyclization d-amino acid peptides peptoid stability

Mesh : Humans Peptides / pharmacology therapeutic use chemistry

来  源:   DOI:10.1016/j.tips.2023.04.003   PDF(Pubmed)

Abstract:
Peptides have unique characteristics that make them highly desirable as therapeutic agents. The physicochemical and proteolytic stability profiles determine the therapeutic potential of peptides. Multiple strategies to enhance the therapeutic profile of peptides have emerged. They include chemical modifications, such as cyclization, substitution with d-amino acids, peptoid formation, N-methylation, and side-chain halogenation, and incorporation in delivery systems. There have been recent advances in approaches to discover peptides having these modifications to attain desirable therapeutic properties. We critically review these recent advancements in therapeutic peptide development.
摘要:
肽具有独特的特性,使得它们作为治疗剂是非常理想的。物理化学和蛋白水解稳定性谱决定了肽的治疗潜力。已经出现了增强肽的治疗概况的多种策略。它们包括化学修饰,如环化,用d-氨基酸取代,类肽形成,N-甲基化,和侧链卤化,并纳入交付系统。最近在发现具有这些修饰的肽以获得期望的治疗性质的方法方面取得了进展。我们批判性地回顾了这些治疗性肽开发的最新进展。
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