ArticleJournal of hepatology2017
Cyclosporin derivatives inhibit hepatitis B virus entry without interfering with NTCP transporter activity.
Article in Journal of hepatology, 2017. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 73 papers, 1 of them a synthesis that pooled it.
What it found
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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
73 citing papers in PubMed, 1 synthesis or guideline pooled it, 121 citations in OpenAlex.
- Hepatitis B infection and intrahepatic cholestasis of pregnancy: A systematic review and meta-analysis.Medicine · 2020Pooled it
- Effectiveness and safety of cyclosporine A in moderate to severe COVID-19: a randomized, open-label trial.Scientific reports · 2026Trial
- HBV-miR-3 is closely related to HBV replication and strongly predictive of HBeAg seroconversion in PegIFN-α treated patients.Scientific reports · 2024Trial
- Advances in pharmacological interventions for hepatic fibrosis: from pathogenic mechanisms to novel therapeutic targets.Annals of medicine · 2026Review
- Post-Translational Modifications of NTCP: A Regulatory Nexus for Bile Acid Transport and HBV Entry.Biomedicines · 2026Review
- Dynamics and Sensitivity of the Lifecycle of Hepatitis B Virus.Pathogens (Basel, Switzerland) · 2026Article
- Insight into the Biology of Hepatitis B Virus and Recent Therapeutic Approaches.Current microbiology · 2026Review
- Emerging antiviral drugs and immunotherapy for chronic hepatitis B and associated liver disease.Frontiers in immunology · 2026Review
- Interaction between W41 of the hepatitis B virus preS1 surface peptide and Y146/F274 of the cellular receptor molecule NaMolecular pharmacology · 2025Article
- The Evolution of Cell Culture Systems to Study Hepatitis B Virus Pathogenesis and Antiviral Susceptibility.Viruses · 2025Review
- [Research progress on new drugs for the treatment of chronic hepatitis B virus infection].Zhonghua gan zang bing za zhi = Zhonghua ganzangbing zazhi = Chinese journal of hepatology · 2025Review
- Hepatitis B and D virus entry.Nature reviews. Microbiology · 2025Review
- Identification of NTCP animal orthologs supporting hepatitis B virus binding and infection.Journal of virology · 2025Article
- HBV infection and pregnancy: Increased risks of gestational diabetes and preterm birth.Pakistan journal of medical sciences · 2025Article
- Virus infection and vesicle trafficking.Frontiers in immunology · 2025Review
- Article
- Hepatitis B virus-targeting sodium taurocholate cotransporting polypeptide mediates HBV infection and damage in human renal podocytes.Microbiology spectrum · 2024Article
- Hepatitis B: Model Systems and Therapeutic Approaches.Journal of immunology research · 2024Review
- The Culprit Behind HBV-Infected Hepatocytes: NTCP.Drug design, development and therapy · 2024Review
- Article
13 more citing papers are in PubMed but not listed here.
Corrections and comments
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Authors and funding
18 authors at 9 institutions in 3 countries.
Funding
No grant is acknowledged in the PubMed record.
Abstract
BACKGROUND &
aimsThe sodium taurocholate co-transporting polypeptide (NTCP) is the main target of most hepatitis B virus (HBV) specific entry inhibitors. Unfortunately, these agents also block NTCP transport of bile acids into hepatocytes, and thus have the potential to cause adverse effects. We aimed to identify small molecules that inhibit HBV entry while maintaining NTCP transporter function.
methodsWe characterized a series of cyclosporine (CsA) derivatives for their anti-HBV activity and NTCP binding specificity using HepG2 cells overexpressing NTCP and primary human hepatocytes. The four most potent derivatives were tested for their capacity to prevent HBV entry, but maintain NTCP transporter function. Their antiviral activity against different HBV genotypes was analysed.
resultsWe identified several CsA derivatives that inhibited HBV infection with a sub-micromolar IC
conclusionsThis is the first example of small molecule selective inhibition of HBV entry with no decrease in NTCP transporter activity. It suggests that the anti-HBV activity can be functionally separated from bile acid transport. These broadly active anti-HBV molecules are potential candidates for developing new drugs with fewer adverse effects. LAY SUMMARY: In this study, we identified new compounds that selectively inhibited hepatitis B virus (HBV) entry, and did not impair bile acid uptake. Our evidence offers a new strategy for developing anti-HBV drugs with fewer side effects.
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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.