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Updated: May 1, 2026

Early Viral Entry Assays for the Identification and Evaluation of Antiviral Compounds
Published on: October 29, 2015
Nucleoside analogs as anti-HBV agents
Xiao-Xiong Zhou1, Eddy Littler
1Department of Medicinal Chemistry, Medivir AB, Huddinge, Sweden. xiao-xiong.zhou@medivir.com
New nucleoside analogs are needed to combat drug-resistant chronic hepatitis B virus (HBV) infection and prevent viral rebound after treatment cessation. This review explores structure-activity relationships of key anti-HBV agents.
Area of Science:
- Hepatology and Virology
- Medicinal Chemistry
- Drug Development
Background:
- Chronic hepatitis B virus (HBV) infection impacts approximately 400 million individuals globally.
- Nucleoside analogs targeting HBV polymerase are crucial for hepatitis B therapy, with lamivudine, adefovir, and entecavir being established treatments.
- Existing therapies face challenges including drug resistance and viral rebound post-treatment, necessitating novel therapeutic strategies.
Purpose of the Study:
- To review the structure-activity relationships (SAR) of significant anti-HBV nucleoside analogs.
- To discuss the latest advancements in the development of novel nucleoside analog therapeutics for HBV infection.
- To address the unmet needs in hepatitis B treatment, focusing on overcoming resistance and preventing viral rebound.
Main Methods:
- Literature review of scientific publications and clinical trial data.
- Analysis of structure-activity relationships for existing and emerging nucleoside analogs.
- Synthesis and evaluation of pharmacological data on anti-HBV nucleoside analogs.
Main Results:
- Detailed examination of SAR for key nucleoside analogs, highlighting molecular features influencing efficacy and resistance profiles.
- Identification of promising new nucleoside analogs with improved potency and reduced resistance potential.
- Overview of recent developments in drug design and medicinal chemistry aimed at enhancing anti-HBV activity.
Conclusions:
- Nucleoside analogs remain a vital class of drugs for managing chronic HBV infection.
- Understanding SAR is critical for designing next-generation analogs that overcome current therapeutic limitations.
- Continued research and development are essential to provide more effective and durable treatments for the global HBV population.
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