将转折点肽和环肽转化为小分子靶向蛋白质-蛋白质相互作用的策略

IF 4.2 Q2 BIOCHEMISTRY & MOLECULAR BIOLOGY
Deanne Hayward and Andrew M. Beekman
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引用次数: 0

摘要

开发能与蛋白质相互作用的小分子药物是一项持续的挑战。肽具有更大、更灵活的结构,其结构上的多样性使其能够与蛋白质产生更大的相互作用,这为靶向蛋白质相互作用的药物发现过程提供了一个起点。快速识别强效环肽和转折点肽的技术非常有效,但这种潜力尚未转化为已获批准的候选药物。通过应用肽与蛋白质相互作用的特性,有可能更有效地开发用于药物发现的小分子化合物。在这篇综述中,我们将讨论使肽与蛋白质具有独特结合特性的方法,以及将这些特性转化为强效小分子的方法。
本文章由计算机程序翻译,如有差异,请以英文原文为准。

Strategies for converting turn-motif and cyclic peptides to small molecules for targeting protein–protein interactions

Strategies for converting turn-motif and cyclic peptides to small molecules for targeting protein–protein interactions

Strategies for converting turn-motif and cyclic peptides to small molecules for targeting protein–protein interactions

The development of small molecules that interact with protein–protein interactions is an ongoing challenge. Peptides offer a starting point in the drug discovery process for targeting protein-interactions due to their larger, more flexible structure and the structurally diverse properties that allow for a greater interaction with the protein. The techniques for rapidly identifying potent cyclic peptides and turn-motif peptides are highly effective, but this potential has not yet transferred to approved drug candidates. By applying the properties of the peptide–protein interaction the development of small molecules for drug discovery has the potential to be more efficient. In this review, we discuss the methods that allow for the unique binding properties of peptides to proteins, and the methods deployed to transfer these qualities to potent small molecules.

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来源期刊
CiteScore
6.10
自引率
0.00%
发文量
128
审稿时长
10 weeks
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