南京大学姚祝军团队开发出为多肽、蛋白质和脂类进行特异性生物偶联的新方法。2021年11月26日,《德国应用化学》杂志在线发表了这项成果。
Title: Azaphilones as Activation-Free Primary-Amine-Specific Bioconjugation Reagents for Peptides, Proteins and Lipids
Author: Shandong Yi, Siyuan Wei, Qingsong Wu, Huan Wang, Zhu-Jun Yao
Issue&Volume: 2021-11-26
Abstract: Residue-selective bioconjugation methods for biomolecules are highly sought to expand the scope of their biological and medical applications. Inspired by the generation mechanism of natural vinylogous γ -pyridones (vPDNs), we have developed a novel unique azaphilone-based, activation-free primary amine-selective bioconjugation method for biomolecules. Our strategy allows facile functionalization of primary amine groups in peptides and proteins, including the clinically used therapeutic antibody trastuzumab, by generating a highly stable vPDN linkage. Excellent chemoselectivity toward primary amines also enables the azaphilone derivatives to specifically modify the lipid components of Gram-positive bacteria while bypassing Gram-negative bacteria and mammalian cells. The new method shows significant advantages including chemoselectivity, efficiency, flexibility and biocompatibility, and therefore provides a valuable addition to the current toolbox for biomolecule conjugation.
DOI: 10.1002/anie.202111783
Source: https://onlinelibrary.wiley.com/doi/10.1002/anie.202111783
Angewandte Chemie:《德国应用化学》,创刊于1887年。隶属于德国化学会,最新IF:12.959
官方网址:https://onlinelibrary.wiley.com/journal/15213773
投稿链接:https://www.editorialmanager.com/anie/default.aspx