Targeting lipid biosynthesis pathways for hepatitis B virus cure

PLoS One. 2022 Aug 4;17(8):e0270273. doi: 10.1371/journal.pone.0270273. eCollection 2022.

Abstract

Chronic hepatitis B virus (HBV) infection is characterized by the presence of high circulating levels of non-infectious lipoprotein-like HBV surface antigen (HBsAg) particles thought to contribute to chronic immune dysfunction in patients. Lipid and metabolomic analysis of humanized livers from immunodeficient chimeric mice (uPA/SCID) revealed that HBV infection dysregulates several lipid metabolic pathways. Small molecule inhibitors of lipid biosynthetic pathway enzymes acetyl-CoA carboxylase (ACC), fatty acid synthase, and subtilisin kexin isozyme-1/site-1 protease in HBV-infected HepG2-NTCP cells demonstrated potent and selective reduction of extracellular HBsAg. However, a liver-targeted ACC inhibitor did not show antiviral activity in HBV-infected liver chimeric mice, despite evidence of on-target engagement. Our study suggests that while HBsAg production may be dependent on hepatic de novo lipogenesis in vitro, this may be overcome by extrahepatic sources (such as lipolysis or diet) in vivo. Thus, a combination of agents targeting more than one lipid metabolic pathway may be necessary to reduce HBsAg levels in patients with chronic HBV infection.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Antiviral Agents / metabolism
  • Antiviral Agents / pharmacology
  • Antiviral Agents / therapeutic use
  • DNA, Viral / metabolism
  • Hepatitis B Surface Antigens / metabolism
  • Hepatitis B virus / genetics
  • Hepatitis B*
  • Hepatitis B, Chronic* / drug therapy
  • Lipids / therapeutic use
  • Mice
  • Mice, SCID

Substances

  • Antiviral Agents
  • DNA, Viral
  • Hepatitis B Surface Antigens
  • Lipids

Grants and funding

All the work in this manuscript was supported by Gilead Sciences. The funders had no role in study design, data collection and analysis, decision to publish, or preparation of the manuscript.