带钉肽:在药物开发中瞄准蛋白质与蛋白质之间的相互作用

Qian Zhang, Ziyang Wang, Xiaohan Mei, Quan Chen, Chunqiu Zhang
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引用次数: 0

摘要

蛋白质-蛋白质相互作用(PPIs)在许多生物过程中扮演着重要角色,是许多人类疾病的潜在治疗靶点。钉钉肽作为最有希望干扰PPIs的候选治疗药物,具有更高的α-螺旋度、更强的结合亲和力、更强的抗蛋白酶消化能力、更长的血清半衰期和更强的细胞渗透性,与小分子药物和生物制剂相比具有更高的药理活性。本综述主要从设计原理、结构稳定性、生物活性、细胞渗透性以及在治疗中的潜在应用等方面概述了钉状肽的研究进展,旨在为设计和探索具有更强生物学和药代动力学特性的钉状肽作为针对各种疾病的下一代治疗肽药物提供广泛的参考。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
Stapled peptides: targeting protein-protein interactions in drug development
Protein-protein interactions (PPIs) impersonate a significant role in many biological processes and are potential therapeutic targets in numerous human diseases. Stapled peptides, as the most promising therapeutic candidate for interfering with PPIs, have a higher degree of α-helicity, improved binding affinity, more resistance to proteolytic digestion, longer serum half-life, and enhanced cell permeability, which exhibits higher pharmacological activity compared with small molecule drugs and biologics. This review outlined the continuous progress of stapled peptides mainly concerning the design principle, structural stability, bioactivity, cell permeability, and potential applications in therapeutics, which is aimed at providing a broad reference for the design and exploration of stapled peptides with enhanced biological and pharmacokinetic properties as the next-generation therapeutic peptide drugs targeting various diseases.
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