Assessing the inhibition efficacy of clinical drugs against the main proteases of SARS-CoV-2 variants and other coronaviruses  

作　　者：Wenlong Zhao Cecylia SLupala Shifeng Hou Shuxin Yang Ziqi Yan Shujie Liao Xuefei Li Nan Li 

机构地区：[1]Key Laboratory of Quantitative Synthetic Biology,Shenzhen Institute of Synthetic Biology,Shenzhen Institutes of Advanced Technology,Chinese Academy of Sciences,Shenzhen,China [2]University of Chinese Academy of Sciences,Beijing,China

出　　处：《Quantitative Biology》2024年第3期324-328,共5页定量生物学（英文版）

基　　金：National Key Research and Development Program of China,Grant/Award Number:2023YFA0913900;National Natural Science Foundation of China,Grant/Award Numbers:31971354,32100146,32170672,32271501。

摘　　要：The rapid evolution of severe acute respiratory syndrome coronavirus 2(SARS-CoV-2)mainly due to its high mutation rate and rapid viral replication,has led to new variants resistant to the available vaccines and monoclonal antibodies.In contrast,oral clinical drugs targeting viral protease and RNA polymerase remain effective against Omicron variants[1].Main protease(Mpro)plays a crucial role in the maturation and replication of viral strains,making it an attractive target for developing antiviral drugs.Nirmatrelvir(NTV)is the first-in-class Mpro peptidomimetic covalent inhibitor known as“Paxlovid”approved in 2021 by the Food and Drug Administration[2].Nevertheless,NTV-resistant Mpro mutants particularly the E166V mutation,have been characterized in the Global Initiative on Sharing Avian Influenza Data(GISAID)database[3]and reported in COVID-19 patients[4,5].

关 键 词：drug resistance enzymatic activity main protease SARS-CoV-2 

分 类 号：R965[医药卫生—药理学]