ArticleAntimicrobial agents and chemotherapy2013
Phenothiazines inhibit hepatitis C virus entry, likely by increasing the fluidity of cholesterol-rich membranes.
Article in Antimicrobial agents and chemotherapy, 2013. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 31 papers.
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Who cites it
31 citing papers in PubMed, 55 citations in OpenAlex.
- A Comprehensive Analysis of the Therapeutic Potential of N-substituted Phenothiazine Derivatives in Medicinal Chemistry.Mini reviews in medicinal chemistry · 2026Review
- Bovine coronavirus enters HRT-18 cells via membrane fusion and clathrin-mediated endocytosis in a low pH-, dynamin-, cholesterol-, microtubule-, Rab7-, and Rab11-dependent manner.Journal of virology · 2025Article
- Repurposing Neurological Drugs Against Dengue Virus Infection.Journal of tropical medicine · 2025Review
- In vitro synergistic antiviral activity of repurposed drugs against enterovirus 71.Archives of virology · 2024Article
- Article
- Methotrimeprazine is a neuroprotective antiviral in JEV infection via adaptive ER stress and autophagy.EMBO molecular medicine · 2024Article
- G4-binding drugs, chlorpromazine and prochlorperazine, repurposed against COVID-19 infection in hamsters.Frontiers in molecular biosciences · 2023Article
- Inhibition of dengue virus infection by trifluoperazine.Archives of virology · 2022Article
- Mitolysosome exocytosis, a mitophagy-independent mitochondrial quality control in flunarizine-induced parkinsonism-like symptoms.Science advances · 2022Article
- Entry Inhibitors of Hepatitis C Virus.Advances in experimental medicine and biology · 2022Article
- Identification of candidate repurposable drugs to combat COVID-19 using a signature-based approach.Scientific reports · 2021Article
- Effect of a fever in viral infections - the 'Goldilocks' phenomenon?World journal of clinical cases · 2021Review
- Antiviral activity of chlorpromazine, fluphenazine, perphenazine, prochlorperazine, and thioridazine towards RNA-viruses. A review.European journal of pharmacology · 2020Review
- The Application of CA and PCA to the Evaluation of Lipophilicity and Physicochemical Properties of Tetracyclic Diazaphenothiazine Derivatives.Journal of analytical methods in chemistry · 2019Article
- Review
- Betanodavirus-like particles enter host cells via clathrin-mediated endocytosis in a cholesterol-, pH- and cytoskeleton-dependent manner.Veterinary research · 2017Article
- Clinically Approved Ion Channel Inhibitors Close Gates for Hepatitis C Virus and Open Doors for Drug Repurposing in Infectious Viral Diseases.Journal of virology · 2017Review
- Abl Tyrosine Kinase Regulates Hepatitis C Virus Entry.Frontiers in microbiology · 2017Article
- Desmosterol Increases Lipid Bilayer Fluidity during Hepatitis C Virus Infection.ACS infectious diseases · 2016Article
- Hepatitis C virus cell entry: a target for novel antiviral strategies to address limitations of direct acting antivirals.Hepatology international · 2016Review
Corrections and comments
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Authors and funding
6 authors at 3 institutions in 2 countries.
Funding
Abstract
Despite recent progress in the development of direct-acting antiviral agents against hepatitis C virus (HCV), more effective therapies are still urgently needed. We and others previously identified three phenothiazine compounds as potent HCV entry inhibitors. In this study, we show that phenothiazines inhibit HCV entry at the step of virus-host cell fusion, by intercalating into cholesterol-rich domains of the target membrane and increasing membrane fluidity. Perturbation of the alignment/packing of cholesterol in lipid membranes likely increases the energy barrier needed for virus-host fusion. A screening assay based on the ability of molecules to selectively increase the fluidity of cholesterol-rich membranes was subsequently developed. One compound that emerged from the library screen, topotecan, is able to very potently inhibit the fusion of liposomes with cell culture-derived HCV (HCVcc). These results yield new insights into HCV infection and provide a platform for the identification of new HCV 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.