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 LinxiangZhao Jie Zheng Leike Zhang Jia Li YuZhou 

作者机构：Key Laboratory of Structure-Based Drugs Design&Discovery of Ministry of EducationShenyang Pharmaceutical UniversityShenyang 110016China School of Life Sciences and BiopharmaceuticalsShenyang Pharmaceutical UniversityShenyang 110016China Shanghai Institute of Materia MedicaChinese Academy of SciencesShanghai 201203and University of Chinese Academy of SciencesBeijing 100049China State Key Laboratory of Chemical BiologyShanghai Institute of Materia MedicaChinese Academy of SciencesShanghai 201203and University of Chinese Academy of SciencesBeijing 100049China State Key Laboratory of VirologyWuhan Institute of VirologyCenter for Biosafety Mega-ScienceChinese Academy of SciencesWuhan 430071China Lingang LaboratoryShanghai 200031China School of Pharmaceutical Science and TechnologyHangzhou Institute for Advanced StudyUniversity of Chinese Academy of SciencesHangzhou 310024China Hubei Jiangxia LaboratoryWuhan 430200China 

出 版 物：《Acta Pharmaceutica Sinica B》 (药学学报（英文版）)

年 卷 期：2024年第14卷第7期

页      面：3286-3290页

核心收录：

学科分类：1007[医学-药学(可授医学、理学学位)] 081702[工学-化学工艺] 08[工学] 0817[工学-化学工程与技术] 

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 

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

摘      要：To the Editor:The papain-like protease(PLpro),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.