Heparin interacts with the main protease of SARS-CoV-2 and inhibits its activity.

ABSTRACT: The ability of SARS-CoV-2 to replicate in host cells is dependent on its main protease (M^pro, also called 3CLpro) that cut the viral precursor polyproteins and is a major target for antiviral drug design. Here, we showed that heparin interacts with the M^pro of SARS-CoV-2 and inhibits its activity. Protein fluorescence quenching showed that heparin strongly binds to the M^pro protein with dissociation constants K_D of 16.66 and 31.60 μM at 25 and 35 °C, respectively. From thermodynamic parameters of the interaction, there are hydrophobic and hydrogen bond interactions between them. Fluorescence resonance energy transfer (FRET) assay demonstrated that heparin inhibits the proteolytic activity of M^pro with an inhibition constant Ki of 6.9 n

SUBMITTER: Li J 

PROVIDER: S-EPMC8591854 | biostudies-literature | 2022 Feb

REPOSITORIES: biostudies-literature