ArticleJournal of medicinal chemistry2010
Potent inhibitors of furin and furin-like proprotein convertases containing decarboxylated P1 arginine mimetics.
Article in Journal of medicinal chemistry, 2010. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 46 papers, 1 of them a synthesis that pooled it.
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The trial behind it
Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
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Who cites it
46 citing papers in PubMed, 1 synthesis or guideline pooled it, 117 citations in OpenAlex.
- Repurposing potential of Ayurvedic medicinal plants derived active principles against SARS-CoV-2 associated target proteins revealed by molecular docking, molecular dynamics and MM-PBSA studies.Biomedicine & pharmacotherapy = Biomedecine & pharmacotherapie · 2021Pooled it
- Furin as target for suppression of mosquito-borne viruses.Virology journal · 2026Article
- Design, Synthesis, and Characterization of Dichlorobiphenyl-Derived Inhibitors of the Proprotein Convertase Furin.Journal of medicinal chemistry · 2025Article
- Structural insights into proprotein convertase activation facilitate the engineering of highly specific furin inhibitors.Nature communications · 2025Article
- Development and Prospects of Furin Inhibitors for Therapeutic Applications.International journal of molecular sciences · 2024Review
- Functional Roles of Furin in Cardio-Cerebrovascular Diseases.ACS pharmacology & translational science · 2024Review
- Structurally Modified Bioactive Peptide Inhibits SARS-CoV-2 Lentiviral Particles Expression.Pharmaceutics · 2022Article
- Comparison of Cell Fusions Induced by Influenza Virus and SARS-CoV-2.International journal of molecular sciences · 2022Review
- In vitro characterization of the furin inhibitor MI-1851: Albumin binding, interaction with cytochrome P450 enzymes and cytotoxicity.Biomedicine & pharmacotherapy = Biomedecine & pharmacotherapie · 2022Article
- The Role of Proprotein Convertases in Upper Airway Remodeling.Molecules and cells · 2022Review
- A perspective on the applications of furin inhibitors for the treatment of SARS-CoV-2.Pharmacological reports : PR · 2022Article
- The Path to Therapeutic Furin Inhibitors: From Yeast Pheromones to SARS-CoV-2.International journal of molecular sciences · 2022Review
- MPI8 is Potent against SARS-CoV-2 by Inhibiting Dually and Selectively the SARS-CoV-2 Main Protease and the Host Cathepsin L.ChemMedChem · 2022Article
- Discovery of diminazene as a dual inhibitor of SARS-CoV-2 human host proteases TMPRSS2 and furin using cell-based assays.Current research in chemical biology · 2022Article
- Peptide-Based Vaccines and Therapeutics for COVID-19.International journal of peptide research and therapeutics · 2022Review
- OFF-State-Specific Inhibition of the Proprotein Convertase Furin.ACS chemical biology · 2021Article
- Article
- Translating bioactive peptides for COVID-19 therapy.European journal of pharmacology · 2021Review
- Role of proteolytic enzymes in the COVID-19 infection and promising therapeutic approaches.Biochemical pharmacology · 2020Review
- Peptide and peptide-based inhibitors of SARS-CoV-2 entry.Advanced drug delivery reviews · 2020Review
Corrections and comments
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Authors and funding
9 authors at 4 institutions in 3 countries.
Funding
Abstract
Furin belongs to the family of proprotein convertases (PCs) and is involved in numerous normal physiological and pathogenic processes, such as viral propagation, bacterial toxin activation, cancer, and metastasis. Furin and related furin-like PCs cleave their substrates at characteristic multibasic consensus sequences, preferentially after an arginine residue. By incorporating decarboxylated arginine mimetics in the P1 position of substrate analogue peptidic inhibitors, we could identify highly potent furin inhibitors. The most potent compound, phenylacetyl-Arg-Val-Arg-4-amidinobenzylamide (15), inhibits furin with a K(i) value of 0.81 nM and has also comparable affinity to other PCs like PC1/3, PACE4, and PC5/6, whereas PC2 and PC7 or trypsin-like serine proteases were poorly affected. In fowl plague virus (influenza A, H7N1)-infected MDCK cells, inhibitor 15 inhibited proteolytic hemagglutinin cleavage and was able to reduce virus propagation in a long-term infection test. Molecular modeling revealed several key interactions of the 4-amidinobenzylamide residue in the S1 pocket of furin contributing to the excellent affinity of these inhibitors.
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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.