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Identification of hepatitis B virus core protein residues critical for capsid assembly, pgRNA encapsidation and resistance to capsid assembly modulators
Journal article   Open access   Peer reviewed

Identification of hepatitis B virus core protein residues critical for capsid assembly, pgRNA encapsidation and resistance to capsid assembly modulators

Yue Luo, Junjun Cheng, Zhanying Hu, Haiqun Ban, Shuo Wu, Nicky Hwang, John Kulp, Yuhuan Li, Yanming Du, Jinhong Chang, …
Antiviral research, v 191, 105080
01 Jul 2021
PMID: 33933516
url
https://doi.org/10.1016/j.antiviral.2021.105080View
Published, Version of Record (VoR) Open

Abstract

Antiviral Capsid assembly Capsid assembly modulators Core protein allosteric modulators Drug resistance Hepatitis B virus
Assembly of hepatitis B virus (HBV) capsids is driven by the hydrophobic interaction of core protein (Cp) at dimer-dimer interface. Binding of core protein allosteric modulators (CpAMs) to a hydrophobic “HAP” pocket formed between the inter-dimer interface strengths the dimer-dimer interaction and misdirects the assembly of Cp dimers into non-capsid Cp polymers or morphologically normal capsids devoid of viral pregenomic (pg) RNA and DNA polymerase. In this study, we performed a systematic mutagenesis analysis to identify Cp amino acid residues at Cp dimer-dimer interface that are critical for capsid assembly, pgRNA encapsidation and resistance to CpAMs. By analyzing 70 mutant Cp with a single amino acid substitution of 25 amino acid residues around the HAP pocket, our study revealed that residue W102 and Y132 are critical for capsid assembly. However, substitution of many other residues did not significantly alter the amount of capsids, but reduced the amount of encapsidated pgRNA, suggesting their critical roles in pgRNA packaging. Interestingly, several mutant Cp with a single amino acid substitution of residue P25, T33 or I105 supported high levels of DNA replication, but conferred strong resistance to multiple chemotypes of CpAMs. In addition, we also found that WT Cp, but not the assembly incompetent Cp, such as Y132A Cp, interacted with HBV DNA polymerase (Pol). This later finding implies that encapsidation of viral DNA polymerase may depend on the interaction of Pol with a capsid assembly intermediate, but not free Cp dimers. Taking together, our findings reported herein shed new light on the mechanism of HBV nucleocapsid assembly and mode of CpAM action. •Cp dimer-dimer interface interaction differentially modulates the assembly of empty capsids and nucleocapsids.•Cp residues W102 and Y132 play critical role in capsid assembly.•Mutations at P25, T33 and I105 confer resistance to multiple chemotypes of CpAMs.•HBV DNA polymerase interacts with wild-type, but not the assembly incompetent Cp.

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Collaboration types
Domestic collaboration
International collaboration
Web of Science research areas
Pharmacology & Pharmacy
Virology
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