Targeting viral suppressor of RNAi confers anti-coronaviral activity

Mol Ther. 2025 Jan 8;33(1):201-214. doi: 10.1016/j.ymthe.2024.12.009. Epub 2024 Dec 10.

Abstract

Infections caused by coronaviruses are persistent threats to human health in recent decades, necessitating the development of innovative anti-coronaviral therapies. RNA interference (RNAi) is a conserved cell-intrinsic antiviral mechanism in diverse eukaryotic organisms, including mammals. To counteract, many viruses encode viral suppressors of RNAi (VSRs) to evade antiviral RNAi, implying that targeting VSRs could be a promising strategy to develop antiviral therapies. Here, we designed a series of peptides specifically targeting the SARS-CoV-2-encoded VSR, nucleocapsid (N) protein. Among these peptides, one designated GL directly interacts with N protein and inactivates its VSR activity, which unlocks a potent RNAi response and effectively inhibits severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) replication. Moreover, GL exhibited RNAi-dependent antiviral effects not only against various SARS-CoV-2 variants, including Delta, Omicron BA.5, XBB, and JN.1, but also against other coronaviruses such as human coronavirus (HCoV)-229E, HCoV-OC43, and mouse hepatitis virus. The in vivo anti-coronaviral activity of GL was also confirmed. Our findings indicate that the VSR-targeting peptide GL has the potential to be further developed as a broad-spectrum anti-coronaviral treatment, highlighting the functional importance and therapeutic potential of antiviral RNAi.

Keywords: N protein; SARS-CoV-2; antiviral RNAi; antiviral peptide; coronavirus; viral suppressors of RNAi.

MeSH terms

  • Animals
  • Antiviral Agents* / pharmacology
  • COVID-19 / therapy
  • COVID-19 / virology
  • Humans
  • Mice
  • Nucleocapsid Proteins / genetics
  • Nucleocapsid Proteins / metabolism
  • Peptides / pharmacology
  • RNA Interference*
  • SARS-CoV-2* / drug effects
  • SARS-CoV-2* / genetics
  • Virus Replication* / drug effects

Substances

  • Antiviral Agents
  • Peptides
  • Nucleocapsid Proteins

Supplementary concepts

  • SARS-CoV-2 variants