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An update review of emerging small-molecule therapeutic options for COVID-19

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 o...

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Autores principales: Tian, Dengke, Liu, Yuzhi, Liang, Chengyuan, Xin, Liang, Xie, Xiaolin, Zhang, Dezhu, Wan, Minge, Li, Han, Fu, Xueqi, Liu, Hong, Cao, Wenqiang
Formato: Online Artículo Texto
Lenguaje:English
Publicado: The Author(s). Published by Elsevier Masson SAS. 2021
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7857046/
https://www.ncbi.nlm.nih.gov/pubmed/33556871
http://dx.doi.org/10.1016/j.biopha.2021.111313
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author Tian, Dengke
Liu, Yuzhi
Liang, Chengyuan
Xin, Liang
Xie, Xiaolin
Zhang, Dezhu
Wan, Minge
Li, Han
Fu, Xueqi
Liu, Hong
Cao, Wenqiang
author_facet Tian, Dengke
Liu, Yuzhi
Liang, Chengyuan
Xin, Liang
Xie, Xiaolin
Zhang, Dezhu
Wan, Minge
Li, Han
Fu, Xueqi
Liu, Hong
Cao, Wenqiang
author_sort Tian, Dengke
collection PubMed
description 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 (3CL(pro)), papain-like protease (PL(pro)) and other potentially innovative active ingredient molecules, describing their potential targets, activities, clinical status and side effects.
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spelling pubmed-78570462021-02-04 An update review of emerging small-molecule therapeutic options for COVID-19 Tian, Dengke Liu, Yuzhi Liang, Chengyuan Xin, Liang Xie, Xiaolin Zhang, Dezhu Wan, Minge Li, Han Fu, Xueqi Liu, Hong Cao, Wenqiang Biomed Pharmacother Review 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 (3CL(pro)), papain-like protease (PL(pro)) and other potentially innovative active ingredient molecules, describing their potential targets, activities, clinical status and side effects. The Author(s). Published by Elsevier Masson SAS. 2021-05 2021-02-03 /pmc/articles/PMC7857046/ /pubmed/33556871 http://dx.doi.org/10.1016/j.biopha.2021.111313 Text en © 2021 The Author(s) Since January 2020 Elsevier has created a COVID-19 resource centre with free information in English and Mandarin on the novel coronavirus COVID-19. The COVID-19 resource centre is hosted on Elsevier Connect, the company's public news and information website. Elsevier hereby grants permission to make all its COVID-19-related research that is available on the COVID-19 resource centre - including this research content - immediately available in PubMed Central and other publicly funded repositories, such as the WHO COVID database with rights for unrestricted research re-use and analyses in any form or by any means with acknowledgement of the original source. These permissions are granted for free by Elsevier for as long as the COVID-19 resource centre remains active.
spellingShingle Review
Tian, Dengke
Liu, Yuzhi
Liang, Chengyuan
Xin, Liang
Xie, Xiaolin
Zhang, Dezhu
Wan, Minge
Li, Han
Fu, Xueqi
Liu, Hong
Cao, Wenqiang
An update review of emerging small-molecule therapeutic options for COVID-19
title An update review of emerging small-molecule therapeutic options for COVID-19
title_full An update review of emerging small-molecule therapeutic options for COVID-19
title_fullStr An update review of emerging small-molecule therapeutic options for COVID-19
title_full_unstemmed An update review of emerging small-molecule therapeutic options for COVID-19
title_short An update review of emerging small-molecule therapeutic options for COVID-19
title_sort update review of emerging small-molecule therapeutic options for covid-19
topic Review
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7857046/
https://www.ncbi.nlm.nih.gov/pubmed/33556871
http://dx.doi.org/10.1016/j.biopha.2021.111313
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