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Strategies to expand peptide functionality through hybridisation with a small molecule component
RSC Chemical Biology Pub Date : 2020-12-8 , DOI: 10.1039/d0cb00167h
Yuteng Wu 1, 2 , Jack Williams 1, 2 , Ewen D D Calder 1, 2 , Louise J Walport 1, 2
Affiliation  

Combining different compound classes gives molecular hybrids that can offer access to novel chemical space and unique properties. Peptides provide ideal starting points for such molecular hybrids, which can be easily modified with a variety of molecular entities. The addition of small molecules can improve the potency, stability and cell permeability of therapeutically relevant peptides. Furthermore, they are often applied to create peptide-based tools in chemical biology. In this review, we discuss general methods that allow the discovery of this compound class and highlight key examples of peptide–small molecule hybrids categorised by the application and function of the small molecule entity.

中文翻译:

通过与小分子成分杂交来扩展肽功能的策略

结合不同的化合物类别,可以产生分子杂交,可以提供新的化学空间和独特的特性。肽为此类分子杂交提供了理想的起点,可以很容易地用各种分子实体进行修饰。添加小分子可以提高治疗相关肽的效力、稳定性和细胞渗透性。此外,它们通常用于在化学生物学中创建基于肽的工具。在这篇综述中,我们讨论了发现这类化合物的一般方法,并重点介绍了按小分子实体的应用和功能分类的肽-小分子杂交体的关键例子。
更新日期:2020-12-09
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