Assembly/Disassembly of Drug Conjugates Using Imide Ligation

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• 作者：Reda Mhidia ; Nicolas Bzire ; Annick Blanpain ; Nicole Pommery ; Oleg Melnyk
• 刊名：Organic Letters
• 出版年：2010
• 出版时间：September 17, 2010
• 年：2010
• 卷：12
• 期：18
• 页码：3982-3985
• 全文大小：210K
• 年卷期：v.12,no.18(September 17, 2010)
• ISSN：1523-7052

文摘

A strategy is described that allows the easy assembly and controlled disassembly of drug conjugates. Imide ligation, that is, the reaction of a peptide thioacid with an azidoformate, is used for conjugate assembly. The imide bond participates also with an endopeptidase-triggered cyclization-based disassembly mechanism.