Three-Component Protein Modification Using Mercaptobenzaldehyde Derivatives
Three-Component Protein Modification Using Mercaptobenzaldehyde Derivatives
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DOI：
10.1021/acs.orglett.9b01294
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发表时间：
2019-05-17
期刊：
影响因子：
5.2
通讯作者：
Zhang, Qiang
中科院分区：
文献类型：
--
作者：
Dai, Yuanwei;Weng, Jiaping;Zhang, Qiang
描述了能够实现三组分一锅法生物缀合的化学选择性伯胺修饰策略。专门设计的基于巯基苯并咪唑的双功能连接体在生物相容性条件下实现了高度选择性和稳健的胺标记。该接头显示出宽的官能团耐受性并且制备简单，这允许容易的有效负载掺入。最后，我们的研究表明，接头的引入不会损害修饰的蛋白质如胰岛素的功能。
A chemoselective primary amine modification strategy that enables the three-component, one-pot bioconjugation is described. The specifically designed, mercaptobenzaldehyde-based bifunctional linker achieves highly selective and robust amine labeling under biocompatible conditions. This linker demonstrates wide functional group tolerance and is simple to prepare, which allowed facile payload incorporation. Finally, our studies have shown that the introduction of linker does not impair the function of modified protein such as insulin.