Journal of medicinal chemistry · 2025
Novel Dimeric Capsid Assembly Modulators as a Unique Class of Highly Potent Anti-HBV Agents.
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Amblard Franck, Chen Zhe, Kra Kalouna, Patel Dharmeshkumar, Bassit Leda, Gargowitsch Laetitia, Degrouard Jéril, Rat Virgile, Arteni Ana-Andreea, Matthews Lauren, Ravichandran Shreya M, Jiang Alfred, Athanasiadis Antonis, Dangas Georgios, Abate Maedot, Tresset Guillaume, Pronost Julien, Salman Mohammad, Verma Kiran, Kirby Karen A, Michailidis Eleftherios, Rocquigny Hugues de, Durantel David, Bressanelli Stéphane, Sarafianos Stefan G, Schinazi Raymond F
Аннотация
Approximately 250 million people are chronic HBV carriers and are at high risk of developing hepatitis, cirrhosis, and hepatocellular carcinoma. Several drugs are currently approved, but because they do not cure, lifelong therapies are the norm. HBV capsid assembly modulators (CAMs) have emerged as a promising option, as they lower several key markers of HBV replication. Novel dimeric structures (D-CAMs) were designed and evaluated. Their potency and mechanism of action were compared to those of monomeric D-CAMs, such as GLP-26. Among them, D-CAM-14 exhibited improved potency over GLP-26 and a unique effect on capsid morphology and kinetic assembly.