State Key Laboratory of Chemical Oncogenomics, School of Chemical Biology and Biotechnology, Peking University Shenzhen Graduate School, Shenzhen 518055, P. R. China.
Pingshan Translational Medicine Center, Shenzhen Bay Laboratory, Shenzhen 518118, P. R. China.
Org Lett. 2022 Jan 21;24(2):581-586. doi: 10.1021/acs.orglett.1c04017. Epub 2021 Dec 30.
A novel amidation strategy using electrophilic sulfonium, which is soluble and stable in aqueous conditions, was developed. The sulfoniums could activate thioacid and carboxyl acid to efficiently react with amines to afford amides. This method enables applications in amidation in both aqueous media and solid-phase peptide synthesis, peptide/protein modifications, and reactive lysines of a proteome at pH 10 with activity-based protein profiling. A peptide ligand-directed labeling of the USP7-UBL2 domain was also performed using this method.
开发了一种新颖的酰胺化策略，使用在水相条件下可溶且稳定的亲电锍盐。该锍盐可以激活硫代酸和羧酸，与胺高效反应，生成酰胺。该方法可用于水相和固相肽合成中的酰胺化、肽/蛋白质修饰以及在 pH 值为 10 时对蛋白质组中反应性赖氨酸的活性蛋白质谱分析。还使用该方法对 USP7-UBL2 结构域进行了肽配体导向标记。
