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Article

Effects of SARS-CoV-2 Main Protease Mutations at Positions L50, E166, and L167 Rendering Resistance to Covalent and Noncovalent Inhibitors.

Journal of medicinal chemistry - 24 Oct 2024

Kovalevsky Andrey, Aniana Annie, Ghirlando Rodolfo, Coates Leighton, Drago Victoria N, Wear Lauren, Gerlits Oksana, Nashed Nashaat T, Louis John M

Abstract excerpt

SARS-CoV-2 propagation under nirmatrelvir and ensitrelvir pressure selects for main protease (MPro) drug-resistant mutations E166V (DRM2), L50F/E166V (DRM3), E166A/L167F (DRM4), and L50F/E166A/L167F (DRM5). DRM2-DRM5 undergoes N-terminal autoprocessing to produce mature MPro with dimer dissociation constants (Kdimer) 2-3 times larger than that of the wildtype. Co-selection of L50F restores catalytic activity of...

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PMID: 39370853
DOI: 10.1021/acs.jmedchem.4c01781

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