SARS-CoV-2 M pro inhibitors with antiviral activity in a transgenic mouse model-Reference-Cited by-同舟云学术

SARS-CoV-2 M pro inhibitors with antiviral activity in a transgenic mouse model

Published:2021-03-26 Issue:6536 Volume:371 Page:1374-1378
ISSN:0036-8075
Container-title:Science
language:en
Short-container-title:Science

Author:

Qiao Jingxin¹^ORCID,Li Yue-Shan¹^ORCID,Zeng Rui¹^ORCID,Liu Feng-Liang²³^ORCID,Luo Rong-Hua²³^ORCID,Huang Chong¹^ORCID,Wang Yi-Fei⁴^ORCID,Zhang Jie¹^ORCID,Quan Baoxue¹^ORCID,Shen Chenjian¹^ORCID,Mao Xin¹^ORCID,Liu Xinlei¹^ORCID,Sun Weining¹^ORCID,Yang Wei¹^ORCID,Ni Xincheng¹^ORCID,Wang Kai¹^ORCID,Xu Ling²³^ORCID,Duan Zi-Lei²³^ORCID,Zou Qing-Cui³^ORCID,Zhang Hai-Lin³⁵^ORCID,Qu Wang³^ORCID,Long Yang-Hao-Peng³^ORCID,Li Ming-Hua³^ORCID,Yang Rui-Cheng¹^ORCID,Liu Xiaolong¹^ORCID,You Jing¹^ORCID,Zhou Yangli¹^ORCID,Yao Rui¹^ORCID,Li Wen-Pei¹^ORCID,Liu Jing-Ming¹^ORCID,Chen Pei⁴^ORCID,Liu Yang¹^ORCID,Lin Gui-Feng¹^ORCID,Yang Xin¹^ORCID,Zou Jun¹^ORCID,Li Linli⁴^ORCID,Hu Yiguo¹^ORCID,Lu Guang-Wen¹^ORCID,Li Wei-Min¹^ORCID,Wei Yu-Quan¹^ORCID,Zheng Yong-Tang²³^ORCID,Lei Jian¹⁶^ORCID,Yang Shengyong¹^ORCID

Affiliation:

1. State Key Laboratory of Biotherapy, West China Hospital, Sichuan University, Chengdu, Sichuan 610041, China.

2. Key Laboratory of Animal Models and Human Disease Mechanisms of the Chinese Academy of Sciences, Kunming Institute of Zoology, Chinese Academy of Sciences, Kunming, Yunnan 650223, China.

3. Kunming National High-level Biosafety Research Center for Non-human Primates, Center for Biosafety Mega-Science, Kunming Institute of Zoology, Chinese Academy of Sciences, Kunming, Yunnan 650107, China.

4. Key Laboratory of Drug Targeting and Drug Delivery Systems, Ministry of Education, West China School of Pharmacy, Sichuan University, Chengdu, Sichuan 610041, China.

5. State Key Laboratory of Genetic Resources and Evolution, Kunming Institute of Zoology, Chinese Academy of Sciences, Kunming, Yunnan 650223, China.

6. National Clinical Research Center for Geriatrics, West China Hospital, Sichuan University, Chengdu, Sichuan 610041, China.

Abstract

Targeting the SARS-CoV-2 main protease Vaccines are an important tool in the fight against COVID-19, but developing antiviral drugs is also a high priority, especially with the rise of variants that may partially evade vaccines. The viral protein main protease is required for cleaving precursor polyproteins into functional viral proteins. This essential function makes it a key drug target. Qiao et al. designed 32 inhibitors based on either boceprevir or telaprevir, both of which are protease inhibitors approved to treat hepatitis C virus. Six compounds protected cells from viral infection with high potency, and two of these were selected for in vivo studies based on pharmokinetic experiments. Both showed strong antiviral activity in a mouse model. Science , this issue p. 1374

Funder

Department of Science and Technology of Sichuan Province

Publisher

American Association for the Advancement of Science (AAAS)

Subject

Multidisciplinary

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