Assembly/disassembly of drug conjugates using imide ligation

R Mhidia, N Bézière, A Blanpain, N Pommery…

Index: Mhidia, Reda; Beziere, Nicolas; Blanpain, Annick; Pommery, Nicole; Melnyk, Oleg Organic Letters, 2010 , vol. 12, # 18 p. 3982 - 3985

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Citation Number: 13

Abstract

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.

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