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Phase Diagrams Map the Properties of Antiviral Agents Directed against Hepatitis B Virus Core Assembly
Authors:Lichun Li  Srinivas Reddy Chirapu  M. G. Finn  Adam Zlotnick
Affiliation:aDepartment of Molecular and Cellular Biochemistry, Indiana University, Bloomington, Indiana, USA;bDepartment of Chemistry and Biochemistry and The Skaggs Institute for Chemical Biology, The Scripps Research Institute, La Jolla, California, USA
Abstract:Assembly effectors are small molecules that induce inappropriate virus capsid assembly to antiviral effect. To identify attributes of hepatitis B virus (HBV) assembly effectors, assembly reaction products (normal capsid, noncapsid polymer, intermediates, and free dimeric core protein) were quantified in the presence of three experimental effectors: HAP12, HAP13, and AT-130. Effectors bound stoichiometrically to capsid protein polymers, but not free protein. Thermodynamic and kinetic effects, not aberrant assembly, correlate with maximal antiviral activity.
Keywords:
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