ArticleEmerging microbes & infections2021
Structure-based design and characterization of novel fusion-inhibitory lipopeptides against SARS-CoV-2 and emerging variants.
Article in Emerging microbes & infections, 2021. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 20 papers.
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Who cites it
20 citing papers in PubMed, 30 citations in OpenAlex.
- The efficacy and safety of inhaled peptide YKYY017 for COVID-19 patients with mild illness: a phase 2 randomized controlled trial.Nature communications · 2025Trial
- A Bifunctional SARS-CoV-2 Entry Inhibitor Targeting the Host Protease TMPRSS2 and Viral Spike Protein HR1 Region.International journal of molecular sciences · 2025Article
- Enhancing the solubility of SARS-CoV-2 inhibitors to increase future prospects for clinical development.Journal of virology · 2025Article
- Advance in peptide-based drug development: delivery platforms, therapeutics and vaccines.Signal transduction and targeted therapy · 2025Review
- Computational optimization of a pan-coronavirus fusion inhibitory peptide targeting spike's heptapeptide repeat region.Biosafety and health · 2025Article
- Structure and Function of the SARS-CoV-2 6-HB Fusion Core and Peptide-based Fusion Inhibitors: A Review.Current medicinal chemistry · 2025Review
- Article
- Helix-based screening with structure prediction using artificial intelligence has potential for the rapid development of peptide inhibitors targeting class I viral fusion.RSC chemical biology · 2024Article
- A stapled lipopeptide platform for preventing and treating highly pathogenic viruses of pandemic potential.Nature communications · 2024Article
- A pan-coronavirus peptide inhibitor prevents SARS-CoV-2 infection in mice by intranasal delivery.Science China. Life sciences · 2023Article
- Design of a bifunctional pan-sarbecovirus entry inhibitor targeting the cell receptor and viral fusion protein.Journal of virology · 2023Article
- Identification of the SARS-unique domain of SARS-CoV-2 as an antiviral target.Nature communications · 2023Article
- Molecular mechanisms of human coronavirus NL63 infection and replication.Virus research · 2023Review
- Design and characterization of novel SARS-CoV-2 fusion inhibitors with N-terminally extended HR2 peptides.Antiviral research · 2023Article
- Dimerized fusion inhibitor peptides targeting the HR1-HR2 interaction of SARS-CoV-2.RSC advances · 2023Article
- Development of highly effective LCB1-based lipopeptides targeting the spike receptor-binding motif of SARS-CoV-2.Antiviral research · 2023Article
- Significance of Conserved Regions in Coronavirus Spike Protein for Developing a Novel Vaccine against SARS-CoV-2 Infection.Vaccines · 2023Review
- Potent inhibition of diverse Omicron sublineages by SARS-CoV-2 fusion-inhibitory lipopeptides.Antiviral research · 2022Article
- SARS-CoV-2 fusion-inhibitory lipopeptides maintain high potency against divergent variants of concern including Omicron.Emerging microbes & infections · 2022Article
- Resistance profile and mechanism of severe acute respiratory syndrome coronavirus-2 variants to LCB1 inhibitor targeting the spike receptor-binding motif.Frontiers in microbiology · 2022Article
Corrections and comments
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Authors and funding
12 authors at 1 institution in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
The ongoing pandemic of COVID-19, caused by SARS-CoV-2, has severely impacted the global public health and socio-economic stability, calling for effective vaccines and therapeutics. In this study, we continued our efforts to develop more efficient SARS-CoV-2 fusion inhibitors and achieved significant findings. First, we found that the membrane-proximal external region (MPER) sequence of SARS-CoV-2 spike fusion protein plays a critical role in viral infectivity and can serve as an ideal template for design of fusion-inhibitory peptides. Second, a panel of novel lipopeptides was generated with greatly improved activity in inhibiting SARS-CoV-2 fusion and infection. Third, we showed that the new inhibitors maintained the potent inhibitory activity against emerging SARS-CoV-2 variants, including those with the major mutations of the B.1.1.7 and B.1.351 strains circulating in the United Kingdom and South Africa, respectively. Fourth, the new inhibitors also cross-inhibited other human CoVs, including SARS-CoV, MERS-CoV, HCoV-229E, and HCoV-NL63. Fifth, the structural properties of the new inhibitors were characterized by circular dichroism (CD) spectroscopy and crystallographic approach, which revealed the mechanisms underlying the high binding and inhibition. Combined, our studies provide important information for understanding the mechanism of SARS-CoV-2 fusion and a framework for the development of peptide therapeutics for the treatment of SARS-CoV-2 and other CoVs.
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