Exploring covalent inhibitors of SARS-CoV-2 main protease: from peptidomimetics to novel scaffolds

探索SARS-CoV-2主蛋白酶的共价抑制剂:从肽模拟物到新型支架

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Abstract

Peptidomimetic inhibitors mimic natural peptide substrates, employing electrophilic warheads to covalently interact with the catalytic Cys145 of M(pro). Examples include aldehydes, α-ketoamides, and aza-peptides, with discussions on their mechanisms of action, potency, and structural insights. Non-peptidomimetic inhibitors utilise diverse scaffolds and mechanisms, achieving covalent modification of M(pro).

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