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Improve Stability of Bioactive Peptides by Enzymatic Modular Synthesis of Peptides with O-Linked Sialyl Lewis x
ACS Catalysis ( IF 11.3 ) Pub Date : 2021-06-17 , DOI: 10.1021/acscatal.1c00955
Xiaoju Zheng 1 , Lin Zhu 1 , Tianlu Li 2 , Wenjia Xu 1 , Dongke Liu 1 , Juzheng Sheng 1 , Hongzhi Cao 2 , Yikang Shi 2 , Fengshan Wang 1, 2, 3
Affiliation  

Glycosylation is an effective solution for peptide drug modification to overcome limitations such as instability under physiological conditions and lack of receptor selectivity. Disclosed herein is a facile enzymatic modular assembly strategy for the (semi)preparative-scale synthesis of active glycopeptides. Sialyl Lewis x (sLex) oligosaccharides with E-selectin-targeting activity can be conjugated with peptides through multistep enzymatic reactions. The antiangiogenic peptide ES2 and anticancer peptide citropin 1.1 were successfully modified without loss of their biological activities. The half-lives of the glycopeptides were approximately 64-fold (ES2-sLex) and 28-fold (citropin-sLex) higher than that of the unmodified peptides in human serum.

中文翻译:

通过酶促模块化合成肽与O-连接的唾液酸路易斯 x提高生物活性肽的稳定性

糖基化是多肽药物修饰的有效解决方案,可以克服生理条件下的不稳定性和受体选择性缺乏等局限性。本文公开了一种用于活性糖肽的(半)制备规模合成的简便酶促模块化组装策略。具有 E-选择素靶向活性的唾液酸路易斯 x (sLe x ) 寡糖可以通过多步酶促反应与肽结合。抗血管生成肽 ES2 和抗癌肽 Citropin 1.1 被成功修饰而没有丧失其生物活性。糖肽的半衰期比人血清中未修饰肽的半衰期高约 64 倍 (ES2-sLe x ) 和 28 倍 (citropin-sLe x )。
更新日期:2021-07-02
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