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SARS-CoV-2 Entry Inhibitors: Small Molecules and Peptides Targeting Virus or Host Cells

The pandemic evolution of SARS-CoV-2 infection is forcing the scientific community to unprecedented efforts to explore all possible approaches against COVID-19. In this context, targeting virus entry is a promising antiviral strategy for controlling viral infections. The main strategies pursued to i...

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Detalles Bibliográficos
Autores principales: Cannalire, Rolando, Stefanelli, Irina, Cerchia, Carmen, Beccari, Andrea R., Pelliccia, Sveva, Summa, Vincenzo
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2020
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7460888/
https://www.ncbi.nlm.nih.gov/pubmed/32784899
http://dx.doi.org/10.3390/ijms21165707
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author Cannalire, Rolando
Stefanelli, Irina
Cerchia, Carmen
Beccari, Andrea R.
Pelliccia, Sveva
Summa, Vincenzo
author_facet Cannalire, Rolando
Stefanelli, Irina
Cerchia, Carmen
Beccari, Andrea R.
Pelliccia, Sveva
Summa, Vincenzo
author_sort Cannalire, Rolando
collection PubMed
description The pandemic evolution of SARS-CoV-2 infection is forcing the scientific community to unprecedented efforts to explore all possible approaches against COVID-19. In this context, targeting virus entry is a promising antiviral strategy for controlling viral infections. The main strategies pursued to inhibit the viral entry are considering both the virus and the host factors involved in the process. Primarily, direct-acting antivirals rely on inhibition of the interaction between ACE2 and the receptor binding domain (RBD) of the Spike (S) protein or targeting the more conserved heptad repeats (HRs), involved in the membrane fusion process. The inhibition of host TMPRSS2 and cathepsins B/L may represent a complementary strategy to be investigated. In this review, we discuss the development entry inhibitors targeting the S protein, as well as the most promising host targeting strategies involving TMPRSS2 and CatB/L, which have been exploited so far against CoVs and other related viruses.
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spelling pubmed-74608882020-09-14 SARS-CoV-2 Entry Inhibitors: Small Molecules and Peptides Targeting Virus or Host Cells Cannalire, Rolando Stefanelli, Irina Cerchia, Carmen Beccari, Andrea R. Pelliccia, Sveva Summa, Vincenzo Int J Mol Sci Review The pandemic evolution of SARS-CoV-2 infection is forcing the scientific community to unprecedented efforts to explore all possible approaches against COVID-19. In this context, targeting virus entry is a promising antiviral strategy for controlling viral infections. The main strategies pursued to inhibit the viral entry are considering both the virus and the host factors involved in the process. Primarily, direct-acting antivirals rely on inhibition of the interaction between ACE2 and the receptor binding domain (RBD) of the Spike (S) protein or targeting the more conserved heptad repeats (HRs), involved in the membrane fusion process. The inhibition of host TMPRSS2 and cathepsins B/L may represent a complementary strategy to be investigated. In this review, we discuss the development entry inhibitors targeting the S protein, as well as the most promising host targeting strategies involving TMPRSS2 and CatB/L, which have been exploited so far against CoVs and other related viruses. MDPI 2020-08-09 /pmc/articles/PMC7460888/ /pubmed/32784899 http://dx.doi.org/10.3390/ijms21165707 Text en © 2020 by the authors. Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC BY) license (http://creativecommons.org/licenses/by/4.0/).
spellingShingle Review
Cannalire, Rolando
Stefanelli, Irina
Cerchia, Carmen
Beccari, Andrea R.
Pelliccia, Sveva
Summa, Vincenzo
SARS-CoV-2 Entry Inhibitors: Small Molecules and Peptides Targeting Virus or Host Cells
title SARS-CoV-2 Entry Inhibitors: Small Molecules and Peptides Targeting Virus or Host Cells
title_full SARS-CoV-2 Entry Inhibitors: Small Molecules and Peptides Targeting Virus or Host Cells
title_fullStr SARS-CoV-2 Entry Inhibitors: Small Molecules and Peptides Targeting Virus or Host Cells
title_full_unstemmed SARS-CoV-2 Entry Inhibitors: Small Molecules and Peptides Targeting Virus or Host Cells
title_short SARS-CoV-2 Entry Inhibitors: Small Molecules and Peptides Targeting Virus or Host Cells
title_sort sars-cov-2 entry inhibitors: small molecules and peptides targeting virus or host cells
topic Review
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7460888/
https://www.ncbi.nlm.nih.gov/pubmed/32784899
http://dx.doi.org/10.3390/ijms21165707
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