Peptide macrocyclization is typically associated with the development of higher affinity and more protease stable protein ligands, and, as such, is an important tool in peptide drug discovery. Yet, within the context of a diverse library, does cyclization give inherent advantages over linear peptides? Here, we used mRNA display to create a peptide library of diverse ring sizes and topologies (monocyclic, bicyclic, and linear). Several rounds of in vitro selection against streptavidin were performed and the winning peptide sequences were analyzed for their binding affinities and overall topologies. The effect of adding a protease challenge on the enrichment of various peptides was also investigated. Taken together, the selection output yields insights about the relative abundance of binders of various topologies within a structurally diverse library.

中文翻译：

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使用mRNA显示直接，竞争性比较线性，单环和双环库。

肽大环化通常与更高亲和力和更蛋白酶稳定的蛋白质配体的发展有关，因此，它是肽药物发现中的重要工具。但是，在多样化文库的背景下，环化是否比线性肽具有固有优势？在这里，我们使用mRNA展示来创建具有不同环大小和拓扑结构（单环，双环和线性）的肽库。进行了几轮针对链霉亲和素的体外选择，分析了获胜的肽序列的结合亲和力和整体拓扑。还研究了添加蛋白酶挑战对各种肽的富集的影响。在一起