OBCR Group, Dept. of Organic and Macromolecular Chemistry, Ghent University, Krijgslaan 281 S4, Ghent, 9000, Belgium.
Nanobody Lab, Dept. of Biochemistry, Faculty of Medicine and Health Sciences, Ghent University, Ghent, 9000, Belgium.
Chem Commun (Camb). 2018 Oct 28;54(84):11929-11932. doi: 10.1039/c8cc06684a. Epub 2018 Oct 4.
Methodologies to conjugate proteins to property-enhancing entities are highly sought after. We report a remarkably simple strategy for conjugating proteins bearing accessible cysteines to unprotected peptides containing a Cys(Scm) protecting group, which is introduced on-resin via a Cys(Acm) building block. The peptides employed for this proof of principle study are highly varied and structurally diverse, and undergo multiple on-resin decoration steps prior to conjugation. The methodology was applied to three different proteins, and proved to be efficient and site-selective. This twist on protecting group chemistry has led to a novel and generally applicable strategy for crossed-disulfide formation between proteins and peptides.
人们强烈追求将蛋白质与增强性能的实体结合的方法。我们报告了一种非常简单的策略，用于将带有可及半胱氨酸的蛋白质与含有 Cys(Scm)保护基团的未保护肽结合，该保护基团通过 Cys(Acm)砌块在树脂上原位引入。在此原理验证研究中使用的肽具有高度的多样性和结构多样性，并在偶联之前经历多次树脂上的修饰步骤。该方法适用于三种不同的蛋白质，并且被证明是高效和选择性的。这种保护基化学的变化导致了蛋白质和肽之间形成交叉二硫键的新颖且通用的策略。
