Bithiazole Inhibitors of Phosphatidylinositol 4-Kinase (PI4KIIIβ) as Broad-Spectrum Antivirals Blocking the Replication of SARS-CoV-2, Zika Virus, and Human Rhinoviruses

ChemMedChem. 2021 Dec 6;16(23):3548-3552. doi: 10.1002/cmdc.202100483. Epub 2021 Sep 7.

Abstract

Over half a century since the description of the first antiviral drug, "old" re-emerging viruses and "new" emerging viruses still represent a serious threat to global health. Their high mutation rate and rapid selection of resistance toward common antiviral drugs, together with the increasing number of co-infections, make the war against viruses quite challenging. Herein we report a host-targeted approach, based on the inhibition of the lipid kinase PI4KIIIβ, as a promising strategy for inhibiting the replication of multiple viruses hijacking this protein. We show that bithiazole inhibitors of PI4KIIIβ block the replication of human rhinoviruses (hRV), Zika virus (ZIKV) and SARS-CoV-2 at low micromolar and sub-micromolar concentrations. However, while the anti-hRV/ZIKV activity can be directly linked to PI4KIIIβ inhibition, the role of PI4KIIIβ in SARS-CoV-2 entry/replication is debated.

Keywords: Broad-spectrum antivirals; PI4KIIIb; SARS-CoV-2; bithiazole; rhinovirus; zika virus.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • 1-Phosphatidylinositol 4-Kinase / antagonists & inhibitors*
  • 1-Phosphatidylinositol 4-Kinase / metabolism
  • Antiviral Agents / chemistry
  • Antiviral Agents / metabolism
  • Antiviral Agents / pharmacology*
  • COVID-19 / pathology
  • COVID-19 / virology
  • Cell Line
  • Drug Stability
  • Enzyme Inhibitors / chemistry*
  • Enzyme Inhibitors / metabolism
  • Enzyme Inhibitors / pharmacology
  • Humans
  • Rhinovirus / physiology*
  • SARS-CoV-2 / isolation & purification
  • SARS-CoV-2 / physiology*
  • Thiazoles / chemistry*
  • Thiazoles / metabolism
  • Virus Replication / drug effects*
  • Zika Virus / isolation & purification
  • Zika Virus / physiology*
  • Zika Virus Infection / pathology

Substances

  • Antiviral Agents
  • Enzyme Inhibitors
  • Thiazoles
  • 1-Phosphatidylinositol 4-Kinase