Changjun Yu, Guangjun Bao, Wangsheng Sun
In recent years, chemical modification techniques based on dehydroalanine (Dha) have become a prominent area in the functionalization of peptides and proteins due to their high efficiency and site selectivity. This article reviews the recent advancements in the modification of Dha-containing peptides and proteins. Focusing on the chemical properties of Dha, the advantages of nucleophilic addition reactions, free radical chemistry, metal-catalyzed cross-coupling reactions, and cycloaddition reactions in peptide and protein modification are discussed, as well as their applicability in the development of novel biocompatible methods. Additionally, the article explores the current limitations of these techniques and highlights future challenges that need to be addressed.