An update review of emerging small-molecule therapeutic options for COVID-19 - 19/03/21
, Liang Xin b, Xiaolin Xie c, Dezhu Zhang c, Minge Wan d, Han Li b, Xueqi Fu a, Hong Liu e, ⁎ , Wenqiang Cao e, ⁎
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Graphical abstract |
Highlights |
• | The present review showcases the major pharmaceutical drug targets that can be used to fight against the SARS-CoV-2 pandemic. |
• | Nonstructural protein inhibitors are essential in preventing host cell entry of coronaviruses and are thoroughly discussed. |
• | Potential SARS-CoV-2 drug targets, including their structures, effects and potential impacts, are reviewed. |
• | Small-molecule therapeutics and their modes of disease suppression are explained in detail. |
Abstract |
The SARS-CoV-2 outbreak and pandemic that began near the end of 2019 has posed a challenge to global health. At present, many candidate small-molecule therapeutics have been developed that can inhibit both the infection and replication of SARS-CoV-2 and even potentially relieve cytokine storms and other related complications. Meanwhile, host-targeted drugs that inhibit cellular transmembrane serine protease (TMPRSS2) can prevent SARS-CoV-2 from entering cells, and its combination with chloroquine and dihydroorotate dehydrogenase (DHODH) inhibitors can limit the spread of SARS-CoV-2 and reduce the morbidity and mortality of patients with COVID-19. The present article provides an overview of these small-molecule therapeutics based on insights from medicinal chemistry research and focuses on RNA-dependent RNA polymerase (RdRp) inhibitors, such as the nucleoside analogues remdesivir, favipiravir and ribavirin. This review also covers inhibitors of 3C-like protease (3CLpro), papain-like protease (PLpro) and other potentially innovative active ingredient molecules, describing their potential targets, activities, clinical status and side effects.
Le texte complet de cet article est disponible en PDF.Abbreviations : 3CLpro, 6MP, 6TG, ACE2, AMPK, BECN1, BSAs, CoV, COVID-19, CQ, CMK, CPE, DAAs, DHO, DHODH, E, EBOV, ELs, EUA, FDA, GM1, GTP, HA, HC, HIV, HTAs, HyCoSuL, IMPDH, IFN, IRF3, LPV/r, M, MERS-CoV, Mpro, N, NIAID, nsps, PC, PIP2, PLpro, PP2A, RBV, RDP, RdRp, RMP, RTP, S, SAR, SARS-CoV, SARS-CoV-2, SKP2, TGN, WHO
Keywords : Coronaviruses, SARS-CoV-2, RNA-dependent RNA polymerase (RdRp), 3C-like protease (3CLpro), Papain-like protease (PLpro), Transmembrane serine protease (TMPRSS2)
Plan
Vol 137
Article 111313- mai 2021 Retour au numéro
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