Structure-based design of antiviral drug candidates targeting the SARS-CoV-2 main protease
China Pharmaceutical University · Chinese Academy of Sciences · +8 more institutions
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.…
Citation impact
- FWCI
- 33.87
- Percentile
- 100%
- References
- 29
Authors
27- WDWenhao DaiCorresponding
China Pharmaceutical University, Chinese Academy of Sciences, Shanghai Institute of Materia Medica
- BZBing ZhangCorresponding
ShanghaiTech University
- XJXia-Ming JiangCorresponding
Chinese Academy of Sciences, Wuhan Institute of Virology
- HSHaixia SuCorresponding
Chinese Academy of Sciences, Shanghai Institute of Materia Medica, University of Chinese Academy of Sciences
- JLJian Li
Nanjing University of Chinese Medicine, Chinese Academy of Sciences, Shanghai Institute of Materia Medica
Topics & keywords
- Coronavirus
- Protease
- Antiviral drug
- In vivo
- Chemistry
- Virology
- Severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2)
- Coronavirus disease 2019 (COVID-19)
- Good health and well-being
Funding
- SSSalt Science Research FoundationAwards: BL19U1, BL18U1
- IRInnovative Research Group Project of the National Natural Science Foundation of ChinaAward: 21632008, 21672231, 21877118, 31970165, 81620108027
- NNNational Natural Science Foundation of ChinaAwards: 21877118, 81620108027, 91953000, 21632008, 31970165, 21672231
- CAChinese Academy of SciencesAwards: XDA12040107, XDA12040201
- SAScience and Technology Commission of Shanghai MunicipalityAwards: 81620108027, 20431900200, 21632008, 20431900100
- SAScience and Technology Department of Guangxi Zhuang AutonomousAward: 2020AB40007
- CAChinese Academy of Engineering
- NKNational Key Research and Development Program of China Stem Cell and Translational ResearchAward: 2017YFC0840300 and 2020YFA0707500