Targeting SARS-CoV-2 papain-like protease in the postvaccine era
Copyright © 2022 Elsevier Ltd. All rights reserved..
While vaccines remain at the forefront of global healthcare responses, pioneering therapeutics against SARS-CoV-2 are expected to fill the gaps for waning immunity. Rapid development and approval of orally available direct-acting antivirals targeting crucial SARS-CoV-2 proteins marked the beginning of the era of small-molecule drugs for COVID-19. In that regard, the papain-like protease (PLpro) can be considered a major SARS-CoV-2 therapeutic target due to its dual biological role in suppressing host innate immune responses and in ensuring viral replication. Here, we summarize the challenges of targeting PLpro and innovative early-stage PLpro-specific small molecules. We propose that state-of-the-art computer-aided drug design (CADD) methodologies will play a critical role in the discovery of PLpro compounds as a novel class of COVID-19 drugs.
| Medienart: |
E-Artikel |
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| Erscheinungsjahr: |
2022 |
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| Erschienen: |
2022 |
| Enthalten in: |
Zur Gesamtaufnahme - volume:43 |
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| Enthalten in: |
Trends in pharmacological sciences - 43(2022), 11 vom: 15. Nov., Seite 906-919 |
| Sprache: |
Englisch |
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| Beteiligte Personen: |
Ton, Anh-Tien [VerfasserIn] |
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| Links: |
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| Anmerkungen: |
Date Completed 18.10.2022 Date Revised 17.12.2022 published: Print-Electronic Citation Status MEDLINE |
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| doi: |
10.1016/j.tips.2022.08.008 |
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| funding: |
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| Förderinstitution / Projekttitel: |
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NLM346307600 |
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| 520 | |a Copyright © 2022 Elsevier Ltd. All rights reserved. | ||
| 520 | |a While vaccines remain at the forefront of global healthcare responses, pioneering therapeutics against SARS-CoV-2 are expected to fill the gaps for waning immunity. Rapid development and approval of orally available direct-acting antivirals targeting crucial SARS-CoV-2 proteins marked the beginning of the era of small-molecule drugs for COVID-19. In that regard, the papain-like protease (PLpro) can be considered a major SARS-CoV-2 therapeutic target due to its dual biological role in suppressing host innate immune responses and in ensuring viral replication. Here, we summarize the challenges of targeting PLpro and innovative early-stage PLpro-specific small molecules. We propose that state-of-the-art computer-aided drug design (CADD) methodologies will play a critical role in the discovery of PLpro compounds as a novel class of COVID-19 drugs | ||
| 650 | 4 | |a Journal Article | |
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| 700 | 1 | |a Smith, Jason R |e verfasserin |4 aut | |
| 700 | 1 | |a Ban, Fuqiang |e verfasserin |4 aut | |
| 700 | 1 | |a Fernandez, Michael |e verfasserin |4 aut | |
| 700 | 1 | |a Cherkasov, Artem |e verfasserin |4 aut | |
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