ArticleInternational journal of molecular sciences2022
Identification of Entry Inhibitors against Delta and Omicron Variants of SARS-CoV-2.
Article in International journal of molecular sciences, 2022. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 17 papers.
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Who cites it
17 citing papers in PubMed, 28 citations in OpenAlex.
- SARS-CoV-2 Evolution in Humans Enables Its Transmission to Nonhuman Primates.Molecular biology and evolution · 2025Article
- Screening of an FDA-Approved Drug Library: Menadione Induces Multiple Forms of Programmed Cell Death in Colorectal Cancer Cells via MAPK8 Cascades.Pharmaceuticals (Basel, Switzerland) · 2025Article
- Using Nano-Luciferase Binary (NanoBiT) Technology to Assess the Interaction Between Viral Spike Protein and Angiotensin-Converting Enzyme II by Aptamers.Biotech (Basel (Switzerland)) · 2025Article
- Colloidal Aggregation Confounds Cell-Based Covid-19 Antiviral Screens.Journal of medicinal chemistry · 2024Article
- Systematic Studies on the Anti-SARS-CoV-2 Mechanisms of Tea Polyphenol-Related Natural Products.ACS omega · 2024Article
- Prediction of Drug-Target Affinity Using Attention Neural Network.International journal of molecular sciences · 2024Article
- Natural products as a source of Coronavirus entry inhibitors.Frontiers in cellular and infection microbiology · 2024Review
- Colloidal aggregation confounds cell-based Covid-19 antiviral screens.bioRxiv : the preprint server for biology · 2023Article
- SARS-CoV-2 proteins structural studies using synchrotron radiation.Biophysical reviews · 2023Review
- Development and evaluation of a novel chromium III-based compound for potential inhibition of emerging SARS-CoV-2 variants.Heliyon · 2023Article
- Importance, Applications and Features of Assays Measuring SARS-CoV-2 Neutralizing Antibodies.International journal of molecular sciences · 2023Review
- HIV and SARS-CoV-2 Co-Infection: From Population Study Evidence to In Vitro Studies.Life (Basel, Switzerland) · 2022Review
- Small molecules in the treatment of COVID-19.Signal transduction and targeted therapy · 2022Review
- Effect of Delta and Omicron Mutations on the RBD-SD1 Domain of the Spike Protein in SARS-CoV-2 and the Omicron Mutations on RBD-ACE2 Interface Complex.International journal of molecular sciences · 2022Article
- Broad-Spectrum Small-Molecule Inhibitors of the SARS-CoV-2 Spike-ACE2 Protein-Protein Interaction from a Chemical Space of Privileged Protein Binders.Pharmaceuticals (Basel, Switzerland) · 2022Article
- Combined effect of traditional Chinese herbal-based formulations Jing Si herbal tea and Jing Si nasal drop inhibits adhesion and transmission of SARS-CoV2 in diabetic SKH-1 mice.Frontiers in pharmacology · 2022Article
- Dual-targeting cyclic peptides of receptor-binding domain (RBD) and main protease (Mpro) as potential drug leads for the treatment of SARS-CoV-2 infection.Frontiers in pharmacology · 2022Article
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Authors and funding
14 authors at 3 institutions in 1 country.
Funding
Abstract
Entry inhibitors against severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) are urgently needed to control the outbreak of coronavirus disease 2019 (COVID-19). This study developed a robust and straightforward assay that detected the molecular interaction between the receptor-binding domain (RBD) of viral spike protein and the angiotensin-converting enzyme 2 (ACE2) receptor in just 10 min. A drug library of 1068 approved compounds was used to screen for SARS-CoV2 entry inhibition, and 9 active drugs were identified as specific pseudovirus entry inhibitors. A plaque reduction neutralization test using authentic SARS-CoV-2 virus in Vero E6 cells confirmed that 2 of these drugs (Etravirine and Dolutegravir) significantly inhibited the infection of SARS-CoV-2. With molecular docking, we showed that both Etravirine and Dolutegravir are preferentially bound to primary ACE2-interacting residues on the RBD domain, implying that these two drug blocks may prohibit the viral attachment of SARS-CoV-2. We compared the neutralizing activities of these entry inhibitors against different pseudoviruses carrying spike proteins from alpha, beta, gamma, and delta variants. Both Etravirine and Dolutegravir showed similar neutralizing activities against different variants, with EC50 values between 4.5 to 5.8 nM for Etravirine and 10.2 to 22.9 nM for Dolutegravir. These data implied that Etravirine and Dolutegravir may serve as general spike inhibitors against dominant viral variants of SARS-CoV-2.
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