Small and simple bioorthogonal reactive handles that can be readily encoded by natural processes are important for bioconjugation. A rapid nickel-promoted N–H arylation of pyroglutamate–histidine sequences with 2-nitroarylboronic acids proceeds under mild aqueous conditions. Chemoselective activation of a lactam amide N–H within a peptide or protein provides a new approach to selective conjugation
可以通过自然过程轻松编码的小而简单的
生物正交反应手柄对于
生物缀合非常重要。焦谷
氨酸-组
氨酸序列与2-硝基芳基
硼酸的快速
镍促进NH芳基化反应在温和的
水性条件下进行。肽或蛋白质中内酰胺酰胺N–H的
化学选择性活化为聚酰胺结构的选择性偶联提供了一种新方法。