ArticleJournal of medicinal chemistry2018
Discovery of Hydrocarbon-Stapled Short α-Helical Peptides as Promising Middle East Respiratory Syndrome Coronavirus (MERS-CoV) Fusion Inhibitors.
Article in Journal of medicinal chemistry, 2018. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 30 papers.
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Who cites it
30 citing papers in PubMed, 60 citations in OpenAlex.
- Targeting Middle East Respiratory Syndrome Coronavirus Spike Fusion Machinery With Antiviral Peptides: In Silico Exploration of the Heptad Repeat 2 Domain.MicrobiologyOpen · 2026Article
- MERS-related coronavirus circulating in pangolins exhibits strong fusogenicity in human cells and high sensitivity to fusion inhibitors.Cell reports. Medicine · 2025Article
- Structure and Function of the SARS-CoV-2 6-HB Fusion Core and Peptide-based Fusion Inhibitors: A Review.Current medicinal chemistry · 2025Review
- A Mini-Review on the Common Antiviral Drug Targets of Coronavirus.Microorganisms · 2024Review
- In silico guided screening of active components of3 Biotech · 2023Article
- Structure-Based Design and Synthesis of StapledJournal of medicinal chemistry · 2023Article
- Peptide Stapling Applied to Antimicrobial Peptides.Antibiotics (Basel, Switzerland) · 2023Review
- Antitarget, Anti-SARS-CoV-2 Leads, Drugs, and the Drug Discovery-Genetics Alliance Perspective.Journal of medicinal chemistry · 2023Review
- Stapled peptides as potential inhibitors of SARS-CoV-2 binding to the hACE2 receptor.Journal of peptide science : an official publication of the European Peptide Society · 2022Review
- Leveraging the therapeutic, biological, and self-assembling potential of peptides for the treatment of viral infections.Journal of controlled release : official journal of the Controlled Release Society · 2022Review
- Recent advances in developing small-molecule inhibitors against SARS-CoV-2.Acta pharmaceutica Sinica. B · 2022Review
- Peptide-based inhibitors hold great promise as the broad-spectrum agents against coronavirus.Frontiers in microbiology · 2022Review
- Molecular mechanism of interaction between SARS-CoV-2 and host cells and interventional therapy.Signal transduction and targeted therapy · 2021Review
- Antiviral peptides against Coronaviridae family: A review.Peptides · 2021Review
- Peptide-Based Antiviral Drugs.Advances in experimental medicine and biology · 2021Article
- Design, Synthesis and Fungicidal Activity of New 1,2,4-Triazole Derivatives Containing Oxime Ether and Phenoxyl Pyridinyl Moiety.Molecules (Basel, Switzerland) · 2020Article
- Application prospect of polysaccharides in the development of anti-novel coronavirus drugs and vaccines.International journal of biological macromolecules · 2020Review
- 1-Phenyl-RSC advances · 2020Article
- A Simple Work-Up-free, Solvent-free Approach to Novel Amino Acid Linked 1,4-Disubstituted 1,2,3-Triazoles as Potent Antituberculosis Agents.ACS omega · 2020Article
- Small Molecule Inhibitors of Middle East Respiratory Syndrome Coronavirus Fusion by Targeting Cavities on Heptad Repeat Trimers.Biomolecules & therapeutics · 2020Article
Corrections and comments
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Authors and funding
9 authors at 4 institutions in 2 countries.
Funding
No grant is acknowledged in the PubMed record.
Abstract
The hexameric α-helical coiled-coil formed between the C-terminal and N-terminal heptad repeat (CHR and NHR) regions of class I viral fusion proteins plays an important role in mediating the fusion of the viral and cellular membranes and provides a clear starting point for molecular mimicry that drives viral fusion inhibitor design. Unfortunately, such peptide mimicry of the short α-helical region in the CHR of Middle East respiratory syndrome coronavirus (MERS-CoV) spike protein has been thwarted by the loss of the peptide's native α-helical conformation when taken out of the parent protein structure. Here, we describe that appropriate all-hydrocarbon stapling of the short helical portion-based peptide to reinforce its bioactive secondary structure remarkably improves antiviral potency. The resultant stapled peptide P21S10 could effectively inhibit infection by MERS-CoV pseudovirus and its spike protein-mediated cell-cell fusion; additionally, P21S10 exhibits improved pharmacokinetic properties than HR2P-M2, suggesting strong potential for development as an anti-MERS-CoV therapeutic.
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Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.