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Development of Highly Potent Noncovalent Inhibitors of SARS- CoV-2 3CLpro

文献类型： 外文期刊

作者： Hou, Ningke 1 ; Shuai, Lei 4 ; Zhang, Lijing 6 ; Xie, Xuping 8 ; Tang, Kaiming 9 ; Zhu, Yunkai 10 ; Yu, Yin 10 ; Zhang, Wenyi 6 ; Tan, Qiaozhu 6 ; Zhong, Gongxun 4 ; Wen, Zhiyuan 1 ; Wang, Chong 4 ; He, Xijun 4 ; Huo, Hong 4 ; Gao, Haishan 6 ; Xu, You 6 ; Xue, Jing 6 ; Peng, Chen 6 ; Zou, Jing 8 ; Schindewolf, Craig 1 ; Menachery, Vineet 11 ; Su, Wenji 12 ; Yuan, Youlang 12 ; Shen, Zuyuan 12 ; Zhang, Rong 10 ; Yuan, Shuofeng 9 ; Yu, Hongtao 6 ; Shi, Pei-Yong 8 ; Bu, Zhigao 4 ; Huang, Jing 6 ; Hu, Qi 6 ;

作者机构： 1.Westlake Univ, Sch Life Sci, Key Lab Struct Biol Zhejiang Prov, Hangzhou 310024, Zhejiang, Peoples R China

2.Ctr Infect Dis Res, Westlake Lab Life Sci & Biomed, Hangzhou 310024, Zhejiang, Peoples R China

3.Inst Biol, Westlake Inst Adv Study, Hangzhou 310024, Zhejiang, Peoples R China

4.Chinese Acad Agr Sci, Harbin Vet Res Inst, State Key Lab Vet Biotechnol, Harbin 150069, Peoples R China

5.Natl High Containment Lab Anim Dis Control & Preve, Harbin 150069, Peoples R China

6.Westlake Univ, Key Lab Struct Biol Zhejiang Prov, Westlake Lab Life Sci & Biomed, Sch Life Sci,Ctr Infect Dis Res,Inst Biol,Westlake, Hangzhou 310024, Zhejiang, Peoples R China

7.Zhejiang Univ, Hangzhou 310058, Zhejiang, Peoples R China

8.Univ Texas Med Branch, Inst Human Infect & Immun, Dept Biochem & Mol Biol, Galveston, TX 77555 USA

9.Univ Hong Kong, Li Ka Shing Fac Med, Dept Microbiol, State Key Lab Emerging Infect Dis,Pokfulam, Hong Kong, Peoples R China

10.Fudan Univ, Shanghai Inst Infect Dis & Biosecur, Key Lab Med Mol Virol MOE NHC CAMS, Sch Basic Med Sci,Shanghai Med Coll,Biosafety Leve, Shanghai 200032, Peoples R China

11.Univ Texas Med Branch, Dept Microbiol & Immunol, Galveston, TX 77555 USA

12.WuXiAppTec Shanghai Co Ltd, Shanghai 200131, Peoples R China

期刊名称：ACS CENTRAL SCIENCE （ 影响因子：18.2； 五年影响因子：17.1 ）

ISSN： 2374-7943

年卷期： 2023 年

页码：

收录情况： SCI

摘要： The 3C-like protease (3CLpro) is an essential enzyme for the replication of SARS-CoV-2 and other coronaviruses and thus is a target for coronavirus drug discovery. Nearly all inhibitors of coronavirus 3CLpro reported so far are covalent inhibitors. Here, we report the development of specific, noncovalent inhibitors of 3CLpro. The most potent one, WU-04, effectively blocks SARS-CoV-2 replications in human cells with EC50 values in the 10-nM range. WU-04 also inhibits the 3CLpro of SARS-CoV and MERS-CoV with high potency, indicating that it is a pan-inhibitor of coronavirus 3CLpro. WU-04 showed anti-SARS-CoV-2 activity similar to that of PF-07321332 (Nirmatrelvir) in K18-hACE2 mice when the same dose was administered orally. Thus, WU-04 is a promising drug candidate for coronavirus treatment.

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