Article
Site-Selective Phosphoglycerate Mutase 1 Acetylation by a Small Molecule.
ACS chemical biology - 20 Mar 2020
Zhang Xiaodan, Jiang Lulu, Huang Ke, Fang Chuantao, Li Jian, Yang Jintong, Li Huiti, Ruan Xiaoxue, Wang Penghui, Mo Mingguang, Wu Ping, Xu Yanhui, Peng Chao, Uesugi Motonari, Ye Deyong, Yu Fa-Xing, Zhou Lu
Abstract excerpt
Post-translational modifications play vital roles in fine-tuning a myriad of physiological processes, and one of the most important modifications is acetylation. Here, we report a ligand-directed site-selective acetylation using KHAc, a derivative of a phosphoglycerate mutase 1 (PGAM1) inhibitor. KHAc binds to PGAM1 and transfers its acetyl group to the ε-NH2 of Lys100 to inactivate the enzyme. The acetyl...
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