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A head-to-head comparison of the inhibitory activities of 15 peptidomimetic SARS-CoV-2 3CLpro inhibitors

Bioorg Med Chem Lett. 2021-07; 
Subramanyam Vankadara, Yun Xuan Wong, Boping Liu, Yi Yang See, Li Hong Tan, Qian Wen Tan, Gang Wang, Ratna Karuna, Xue Guo, Shu Ting Tan, Jia Yi Fong, Joma Joy, C S Brian Chia
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Peptide Synthesis The peptide substrate (Dabcyl)KTSAVLQSGFRKM(Glu)(EDANS) was synthesized by Genscript (USA) Get A Quote

摘要

The COVID-19 pandemic caused by SARS-CoV-2 has created an unprecedented global health emergency. As of July 2021, only three antiviral therapies have been approved by the FDA for treating infected patients, highlighting the urgent need for more antiviral drugs. The SARS-CoV-2 3CL protease (3CLpro) is deemed an attractive drug target due to its essential role in viral polyprotein processing and pathogenesis. Indeed, a number of peptidomimetic 3CLpro inhibitors armed with electrophilic warheads have been reported by various research groups that can potentially be developed for treating COVID-19. However, it is currently impossible to compare their relative potencies due to the different assays employed. To solve ... More

关键词

3CLpro, Cysteine protease inhibitors, Mpro, Peptidomimetic inhibitors, SARS-CoV-2
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