The inhibitory effects of PGG and EGCG against the SARS-CoV-2 3C-like protease.

Biochemical and Biophysical Research Communications
Wei-Chung ChiouCheng Huang

Abstract

The coronavirus disease (COVID-19) pandemic, resulting from human-to-human transmission of a novel severe acute respiratory syndrome coronavirus (SARS-CoV-2), has led to a global health crisis. Given that the 3 chymotrypsin-like protease (3CLpro) of SARS-CoV-2 plays an indispensable role in viral polyprotein processing, its successful inhibition halts viral replication and thus constrains virus spread. Therefore, developing an effective SARS-CoV-2 3CLpro inhibitor to treat COVID-19 is imperative. A fluorescence resonance energy transfer (FRET)-based method was used to assess the proteolytic activity of SARS-CoV-2 3CLpro using intramolecularly quenched fluorogenic peptide substrates corresponding to the cleavage sequence of SARS-CoV-2 3CLpro. Molecular modeling with GEMDOCK was used to simulate the molecular interactions between drugs and the binding pocket of SARS-CoV-2 3CLpro. This study revealed that the Vmax of SARS-CoV-2 3CLpro was about 2-fold higher than that of SARS-CoV 3CLpro. Interestingly, the proteolytic activity of SARS-CoV-2 3CLpro is slightly more efficient than that of SARS-CoV 3CLpro. Meanwhile, natural compounds PGG and EGCG showed remarkable inhibitory activity against SARS-CoV-2 3CLpro than against SARS-CoV 3...Continue Reading

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Citations

Apr 9, 2021·The Journal of General Virology·Lisa HenssBarbara S Schnierle
Aug 31, 2021·Computational and Structural Biotechnology Journal·Fangfang Yan, Feng Gao
Sep 14, 2021·Frontiers in Pharmacology·Wei-Chung ChiouCheng Huang

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Methods Mentioned

BETA
fluorescence resonance
FRET

Software Mentioned

Spark® Control [UNK]
GEMDOCK
GraphPad Prism

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