Exploring covalent inhibitors of SARS-CoV-2 main protease: from peptidomimetics to novel scaffolds
Peptidomimetic inhibitors mimic natural peptide substrates, employing electrophilic warheads to covalently interact with the catalytic Cys145 of Mpro. Examples include aldehydes, α-ketoamides, and aza-peptides, with discussions on their mechanisms of action, potency, and structural insights. Non-pep...
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| Format: | Article |
| Language: | English |
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Taylor & Francis Group
2025-12-01
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| Series: | Journal of Enzyme Inhibition and Medicinal Chemistry |
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| Online Access: | https://www.tandfonline.com/doi/10.1080/14756366.2025.2460045 |
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| _version_ | 1832086569870163968 |
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| author | Noor Atatreh Radwa E. Mahgoub Mohammad A. Ghattas |
| author_facet | Noor Atatreh Radwa E. Mahgoub Mohammad A. Ghattas |
| author_sort | Noor Atatreh |
| collection | DOAJ |
| description | Peptidomimetic inhibitors mimic natural peptide substrates, employing electrophilic warheads to covalently interact with the catalytic Cys145 of Mpro. 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 Mpro. |
| format | Article |
| id | doaj-art-4abb7f23fa88442295296b2bae63f9f5 |
| institution | Kabale University |
| issn | 1475-6366 1475-6374 |
| language | English |
| publishDate | 2025-12-01 |
| publisher | Taylor & Francis Group |
| record_format | Article |
| series | Journal of Enzyme Inhibition and Medicinal Chemistry |
| spelling | doaj-art-4abb7f23fa88442295296b2bae63f9f52025-02-06T11:35:14ZengTaylor & Francis GroupJournal of Enzyme Inhibition and Medicinal Chemistry1475-63661475-63742025-12-0140110.1080/14756366.2025.2460045Exploring covalent inhibitors of SARS-CoV-2 main protease: from peptidomimetics to novel scaffoldsNoor Atatreh0Radwa E. Mahgoub1Mohammad A. Ghattas2College of Pharmacy, Al Ain University, Abu Dhabi, United Arab EmiratesCollege of Pharmacy, Al Ain University, Abu Dhabi, United Arab EmiratesCollege of Pharmacy, Al Ain University, Abu Dhabi, United Arab EmiratesPeptidomimetic inhibitors mimic natural peptide substrates, employing electrophilic warheads to covalently interact with the catalytic Cys145 of Mpro. 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 Mpro.https://www.tandfonline.com/doi/10.1080/14756366.2025.2460045Anti-viralirreversible inhibitioncovalent inhibitorCovid-19warheads reactivity |
| spellingShingle | Noor Atatreh Radwa E. Mahgoub Mohammad A. Ghattas Exploring covalent inhibitors of SARS-CoV-2 main protease: from peptidomimetics to novel scaffolds Journal of Enzyme Inhibition and Medicinal Chemistry Anti-viral irreversible inhibition covalent inhibitor Covid-19 warheads reactivity |
| title | Exploring covalent inhibitors of SARS-CoV-2 main protease: from peptidomimetics to novel scaffolds |
| title_full | Exploring covalent inhibitors of SARS-CoV-2 main protease: from peptidomimetics to novel scaffolds |
| title_fullStr | Exploring covalent inhibitors of SARS-CoV-2 main protease: from peptidomimetics to novel scaffolds |
| title_full_unstemmed | Exploring covalent inhibitors of SARS-CoV-2 main protease: from peptidomimetics to novel scaffolds |
| title_short | Exploring covalent inhibitors of SARS-CoV-2 main protease: from peptidomimetics to novel scaffolds |
| title_sort | exploring covalent inhibitors of sars cov 2 main protease from peptidomimetics to novel scaffolds |
| topic | Anti-viral irreversible inhibition covalent inhibitor Covid-19 warheads reactivity |
| url | https://www.tandfonline.com/doi/10.1080/14756366.2025.2460045 |
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