2H-Azirines as Potential Bifunctional Chemical Linkers of Cysteine Residues in Bioconjugate Technology
2020
Chen, Yang | Yang, Wenjie | Wu, Jiamin | Sun, Wangbin | Loh, Teck-Peng | Jiang, Yaojia
2H-Azirine-2-caboxamides have been designed to perform as a new type of bifunctional thiol linker under very mild reaction conditions. The cleavage of a C–N double bond of 2H-azirine furnishes an amino amide functional group in situ through a thiol addition and ring-opening process. It works with a broad scope of thiols and 2H-azirines in the absence of any catalysts at room temperature. Cysteine-containing peptides have also been demonstrated to work efficiently in a completely water solution.
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