Møller Delphine Nørgaard, Kofoed Christian, Thygesen Mikkel Boas, Jensen Knud J
Department of Chemistry, University of Copenhagen, Frederiksberg C, Denmark.
J Pept Sci. 2025 Nov;31(11):e70058. doi: 10.1002/psc.70058.
Bioconjugation chemistry is an important tool for studying proteins, developing pharmaceutical agents, and for many other applications. Conventional methods for protein functionalization rely on chemoselective reactions but often have poor regioselectivity. Peptide tags facilitating site-selective chemical covalent modification of proteins are of great value in the synthesis of protein conjugates. Ideally, a protein would only have to be minimally mutated prior to chemical modification to avoid interfering with native protein folding, trafficking, and function. This short review summarizes the advances in the developments and applications of peptide tags for covalent modifications that proceed without enzymatic assistance.
生物共轭化学是研究蛋白质、开发药物制剂以及许多其他应用的重要工具。蛋白质功能化的传统方法依赖于化学选择性反应，但区域选择性往往较差。促进蛋白质位点选择性化学共价修饰的肽标签在蛋白质缀合物的合成中具有重要价值。理想情况下，蛋白质在化学修饰之前只需进行最小程度的突变，以避免干扰天然蛋白质的折叠、运输和功能。这篇简短的综述总结了在无酶辅助下进行共价修饰的肽标签的开发和应用进展。
