Discovery and characterization of novel potent non-covalent small molecule inhibitors targeting papain-like protease from SARS-CoV-2  

作　　者：Miao Zheng Bo Feng Yumin Zhang Xin Liu NaZhao Hui Liu Zichao Xu Xinheng He Zhiyan Qu ShizhaoChen Zhidong Jiang Xi Cheng Hong Liu Yi Zang Linxiang Zhao Jie Zheng Leike Zhang Jia Li Yu Zhou 

机构地区：[1]Key Laboratory of Structure-Based Drugs Design&Discovery of Ministry of Education,Shenyang Pharmaceutical University,Shenyang 110016,China [2]School of Life Sciences and Biopharmaceuticals,Shenyang Pharmaceutical University,Shenyang 110016,China [3]Shanghai Institute of Materia Medica,Chinese Academy of Sciences,Shanghai 201203,and University of Chinese Academy of Sciences,Beijing 100049,China [4]State Key Laboratory of Chemical Biology,Shanghai Institute of Materia Medica,Chinese Academy of Sciences,Shanghai 201203,and University of Chinese Academy of Sciences,Beijing 100049,China [5]State Key Laboratory of Virology,Wuhan Institute of Virology,Center for Biosafety Mega-Science,Chinese Academy of Sciences,Wuhan 430071,China [6]Lingang Laboratory,Shanghai 200031,China [7]School of Pharmaceutical Science and Technology,Hangzhou Institute for Advanced Study,University of Chinese Academy of Sciences,Hangzhou 310024,China [8]Hubei Jiangxia Laboratory,Wuhan 430200,China

出　　处：《Acta Pharmaceutica Sinica B》2024年第7期3286-3290,共5页药学学报（英文版）

基　　金：National Natural Science Foundation of China(82151219,82130105);the Strategic Priority Research Program of Chinese Academy of Sciences(SIMM010109,SIMM010111);Shanghai Institute of Materia Medica of Chinese Academy of Sciences(SIMM0120231003)for the financial support.

摘　　要：To the Editor:The papain-like protease(PL^(pro)),as one of the most important proteases of SARS-CoV-2,has emerged as a highly promising target protein,its inhibitor probably holds dual potentials,namely blocking the cleavage of viral polyprotein and intercepting the deubiquitination and deISGylation functions to restore antiviral immunity1.

关 键 词：Non-covalent PL^(pro)inhibitors Antiviral activity Structural-based drug design Imidazo[4 5-b]pyridine scaffold 

分 类 号：R563.1[医药卫生—呼吸系统]