Histidine(His)bears a uniquely electron-deficient imidazole side chain and plays essential roles in protein interactions and enzyme-catalyzed processes.Modification of His C_(2)position offers a useful method to fine-...Histidine(His)bears a uniquely electron-deficient imidazole side chain and plays essential roles in protein interactions and enzyme-catalyzed processes.Modification of His C_(2)position offers a useful method to fine-tune histidine residues of proteins for their structural and functional study.Due to the moderately nucleophilic imidazole group,the chemoselective modification of histidine in proteins remains particularly challenging.Herein,we report a highly efficient method for the semisynthesis of chitin-binding protein21(CBP21)bearing various groups at the C_(2)position of His28.A combination of modern radical-mediated C-H alkylation and recombinant protein engineering offers a powerful strategy to decipher His functions.展开更多
基金supported by the National Science Fund for National Natural Science Foundation of China(grant nos.92253302,22225701,22077080 and 22477078)the Shanghai Pilot Program for Basic Research-Shanghai Jiao Tong University(grant no.21TQ1400210)+1 种基金the Interdisciplinary Program of Shanghai Jiao Tong University(grant no.20230102)the Shanghai Municipal Science and Technology Major Project and the Department of Human Resources,and Social Security of Sichuan Province,China.
文摘Histidine(His)bears a uniquely electron-deficient imidazole side chain and plays essential roles in protein interactions and enzyme-catalyzed processes.Modification of His C_(2)position offers a useful method to fine-tune histidine residues of proteins for their structural and functional study.Due to the moderately nucleophilic imidazole group,the chemoselective modification of histidine in proteins remains particularly challenging.Herein,we report a highly efficient method for the semisynthesis of chitin-binding protein21(CBP21)bearing various groups at the C_(2)position of His28.A combination of modern radical-mediated C-H alkylation and recombinant protein engineering offers a powerful strategy to decipher His functions.
