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

doi:10.3390/ijms21165707

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

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Department of Pharmacy, University of Napoli “Federico II”, via D. Montesano 49, 80131 Napoli, Italy

Dompé Farmaceutici SpA, via Campo di Pile, 67100 L’Aquila, Italy

Author to whom correspondence should be addressed.

Int. J. Mol. Sci. 2020, 21(16), 5707; https://doi.org/10.3390/ijms21165707

Received: 15 June 2020 / Revised: 7 August 2020 / Accepted: 7 August 2020 / Published: 9 August 2020

(This article belongs to the Special Issue Exscalate4CoV: Innovative High Performing Computing (HPC) Strategies to Tackle Pandemic Crisis)

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Abstract

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. View Full-Text

Keywords: SARS-CoV-2 entry inhibitors; COVID-19; coronavirus; spike; TMPRSS2; cathepsins; small molecules inhibitors; peptides inhibitors

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This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited

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Cannalire, R.; Stefanelli, I.; Cerchia, C.; Beccari, A.R.; Pelliccia, S.; Summa, V. SARS-CoV-2 Entry Inhibitors: Small Molecules and Peptides Targeting Virus or Host Cells. Int. J. Mol. Sci. 2020, 21, 5707. https://doi.org/10.3390/ijms21165707

AMA Style

Cannalire R, Stefanelli I, Cerchia C, Beccari AR, Pelliccia S, Summa V. SARS-CoV-2 Entry Inhibitors: Small Molecules and Peptides Targeting Virus or Host Cells. International Journal of Molecular Sciences. 2020; 21(16):5707. https://doi.org/10.3390/ijms21165707

Chicago/Turabian Style

Cannalire, Rolando, Irina Stefanelli, Carmen Cerchia, Andrea R. Beccari, Sveva Pelliccia, and Vincenzo Summa. 2020. "SARS-CoV-2 Entry Inhibitors: Small Molecules and Peptides Targeting Virus or Host Cells" International Journal of Molecular Sciences 21, no. 16: 5707. https://doi.org/10.3390/ijms21165707

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

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