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- | Journal: Mutations in the nucleocapsid protein were complemented by mutations in the L protein to restore viral RNA synthesis. (Pubmed Central) - Mar 29, 2019
This mechanism of action allows the sequestered RNA to be released locally without disrupting the overall structure of the nucleocapsid. Since this flexible structural motif is present in the N proteins of many NSVs, release of the sequestered RNA genome by local conformational changes in the N protein may be a general mechanism in NSV viral RNA synthesis.
- | Journal: 5-Aminothiophene-2,4-dicarboxamide analogues as hepatitis B virus capsid assembly effectors. (Pubmed Central) - Mar 28, 2019
In the end, these medicinal chemistry efforts led to the identification of multiple analogues strongly binding to Cp, potently inhibiting HBV replication in nanomolar range without cytotoxicity, and exhibiting good oral bioavailability (F). Two of our analogues, 19o (EC = 0.11 μM, CC > 100 μM, F = 25%) and 19k (EC = 0.31 μM, CC > 100 μM, F = 46%), displayed overall lead profiles superior to reported CAEs 7-10 used in our studies.
- | Preclinical, Journal: Design and synthesis of aminothiazole based Hepatitis B Virus (HBV) capsid inhibitors. (Pubmed Central) - Mar 28, 2019
This compound exerted potent inhibitory effect upon HBV production, either in cell culture or in mice with no obvious acute toxicity. We propose that further development of this compound could lead to novel potent anti-HBV inhibitors that target HBV capsid assembly.