Structure-based design of antiviral drug candidates targeting the SARS-CoV-2 main protease-Reference-Cited by-全球学者库

Structure-based design of antiviral drug candidates targeting the SARS-CoV-2 main protease

Published:2020-06-19 Issue:6497 Volume:368 Page:1331-1335
ISSN:0036-8075
Container-title:Science
language:en
Short-container-title:Science

Author:

Dai Wenhao¹²^ORCID,Zhang Bing³^ORCID,Jiang Xia-Ming⁴,Su Haixia¹⁵^ORCID,Li Jian¹⁶,Zhao Yao³^ORCID,Xie Xiong¹⁵,Jin Zhenming³^ORCID,Peng Jingjing¹⁵,Liu Fengjiang³^ORCID,Li Chunpu¹⁵,Li You⁷,Bai Fang³^ORCID,Wang Haofeng³^ORCID,Cheng Xi¹^ORCID,Cen Xiaobo⁷,Hu Shulei¹,Yang Xiuna³,Wang Jiang¹⁵^ORCID,Liu Xiang⁸^ORCID,Xiao Gengfu⁴,Jiang Hualiang¹²³⁵^ORCID,Rao Zihe³^ORCID,Zhang Lei-Ke⁴,Xu Yechun¹⁵^ORCID,Yang Haitao³^ORCID,Liu Hong¹²⁵⁶^ORCID

Affiliation:

1. State Key Laboratory of Drug Research, CAS Key Laboratory of Receptor Research, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai 201203, China.

2. School of Pharmacy, China Pharmaceutical University, Nanjing 210009, Jiangsu, China.

3. Shanghai Institute for Advanced Immunochemical Studies and School of Life Science and Technology, ShanghaiTech University, Shanghai 201210, China.

4. State Key Laboratory of Virology, Wuhan Institute of Virology, Center for Biosafety Mega-Science, Chinese Academy of Sciences, Wuhan 430071, China.

5. University of Chinese Academy of Sciences, Beijing 100049, China.

6. College of Pharmacy, Nanjing University of Chinese Medicine, Qixia District, Nanjing 210023, China.

7. National Chengdu Center for Safety Evaluation of Drugs, Westchina Hospital of Sichuan University, High-Tech Development Zone, Chengdu, Sichuan 610041, China.

8. State Key Laboratory of Medicinal Chemical Biology, Frontiers Science Center for Cell Response, College of Life Sciences, College of Pharmacy, Nankai University, Tianjin 300353, China.

Abstract

Promising antiviral protease inhibitors With no vaccine or proven effective drug against the virus that causes coronavirus disease 2019 (COVID-19), scientists are racing to find clinical antiviral treatments. A promising drug target is the viral main protease M pro , which plays a key role in viral replication and transcription. Dai et al. designed two inhibitors, 11a and 11b, based on analyzing the structure of the M pro active site. Both strongly inhibited the activity of M pro and showed good antiviral activity in cell culture. Compound 11a had better pharmacokinetic properties and low toxicity when tested in mice and dogs, suggesting that this compound is a promising drug candidate. Science , this issue p. 1331

Funder

Innovative Research Group Project of the National Natural Science Foundation of China

Science and Technology Commission of Shanghai Municipality

National Key Research and Development Program of China Stem Cell and Translational Research

Chinese Academy of Engineering and Ma Yun Foundation

Department of Science and Technology of Guangxi Zhuang Autonomous Region

Publisher

American Association for the Advancement of Science (AAAS)

Subject

Multidisciplinary

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