PDF(Pubmed)
Abstract：
Late-stage specific and selective diversifications of peptides and proteins performed at target residues under ambient conditions are recognized to be the most facile route to various and abundant conjugates. Herein, we report an orthogonal modification of cysteine residues using alkyl thianthreium salts, which proceeds with excellent chemoselectivity and compatibility under mild conditions, introducing a diverse array of functional structures. Crucially, multifaceted bioconjugation is achieved through clickable handles to incorporate structurally diverse functional molecules. This \"two steps, one pot\" bioconjugation method is successfully applied to label bovine serum albumin. Therefore, our technique is a versatile and powerful tool for late-stage orthogonal bioconjugation.
摘要：
在环境条件下在靶残基处进行的肽和蛋白质的后期特异性和选择性多样化被认为是获得各种和丰富缀合物的最容易的途径。在这里，我们报告了使用烷基硫烷盐对半胱氨酸残基的正交修饰，在温和条件下具有优异的化学选择性和相容性，引入各种各样的功能结构。至关重要的是，多方面的生物缀合是通过可点击的手柄实现的，以结合结构上不同的功能分子。这两个步骤，一锅生物缀合法成功应用于标记牛血清白蛋白。因此,我们的技术是后期正交生物缀合的通用且强大的工具。
