The modification of biomolecules, particularly peptides, has garnered considerable attention from researchers, effectively serving as a connection between chemistry and biology. The modification of peptides can facilitate, among others, the generation of peptide drugs, antibody–drug conjugates, and probes for molecular imaging. Herein, we have carefully curated reactions and chemical transformations of bioactive peptide sequences equipped with histidine amino acids that are conducive for biological applications. This Account also highlights strategies for the chemical modification of histidine that might capture the imagination of both peptide researchers and synthetic chemists.

1 Introduction

2 Histidine Modification in Bioactive Peptides and Proteins

3 Remote Bioactive Peptides and Protein Modification Adjacent to Histidine

4 Conclusions and Future Directions

生物分子（特别是肽）的修饰引起了研究人员的广泛关注，有效地充当了化学和生物学之间的联系。肽的修饰可以促进肽药物、抗体药物缀合物和分子成像探针的产生。在这里，我们精心策划了配备组氨酸氨基酸的生物活性肽序列的反应和化学转化，这有利于生物应用。本报告还重点介绍了组氨酸的化学修饰策略，这可能会激发肽研究人员和合成化学家的想象力。

 1 简介

2 生物活性肽和蛋白质中的组氨酸修饰

3 与组氨酸相邻的远程生物活性肽和蛋白质修饰

4 结论和未来方向