使用酰亚胺键连接法进行药物偶联物的组装/拆卸。

Assembly/disassembly of drug conjugates using imide ligation.

机构信息

UMR CNRS 8161, Université de Lille Nord de France, IFR 142, Institut Pasteur de Lille, 1 rue du Pr Calmette 59021 Lille, France.

出版信息

Org Lett. 2010 Sep 17;12(18):3982-5. doi: 10.1021/ol101049g.

DOI:10.1021/ol101049g

PMID:20726571

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.

摘要

描述了一种允许药物偶联物轻松组装和控制拆卸的策略。酰亚胺键合，即肽硫酯与叠氮甲酸酯的反应，用于偶联物的组装。该酰亚胺键还参与基于内切蛋白酶触发的环化的拆卸机制。