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Early Viral Entry Assays for the Identification and Evaluation of Antiviral Compounds
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Inhibition of Ebola and Marburg Virus Entry by G Protein-Coupled Receptor Antagonists

Han Cheng1, Calli M Lear-Rooney2, Lisa Johansen3

  • 1Department of Microbiology and Immunology, College of Medicine, University of Illinois at Chicago, Chicago, Illinois, USA.

Journal of Virology
|July 24, 2015
PubMed
Abstract

Insights

G protein-coupled receptor (GPCR) antagonists show broad antiviral activity against deadly Ebola virus (EBOV) and Marburg virus (MARV). These compounds block viral entry, offering a promising new therapeutic strategy for filoviral hemorrhagic fevers.

Area of Science:

  • Virology
  • Pharmacology
  • Infectious Diseases

Background:

  • Filoviruses, including Ebola virus (EBOV) and Marburg virus (MARV), cause severe hemorrhagic fevers with high mortality rates.
  • No approved vaccines or antiviral therapies currently exist for filoviral infections, highlighting an urgent need for effective treatments.
  • The 2013-2015 West Africa epidemic emphasized gaps in understanding filovirus pathogenesis and the necessity of drug development.

Purpose of the Study:

  • To identify small molecules that can inhibit filoviral replication.
  • To investigate the potential of G protein-coupled receptor (GPCR) antagonists as antiviral agents against EBOV and MARV.
  • To elucidate the mechanism of action of identified inhibitors in blocking filoviral entry.

Main Methods:

  • Screening of a chemical library to identify small molecule inhibitors.
  • Testing inhibitors against infectious EBOV and MARV replication.
  • Conducting time-of-addition experiments and microscopic studies to determine the stage of viral entry inhibited.

Main Results:

  • Numerous known GPCR antagonists targeting various GPCRs (e.g., histamine, serotonin, muscarinic, adrenergic receptors) were identified as potent inhibitors.
  • These GPCR antagonists demonstrated broad antiviral activity, effectively blocking replication of both EBOV and MARV.
  • GPCR antagonists were found to inhibit filoviral entry at a post-attachment, pre-fusion stage.

Conclusions:

  • G protein-coupled receptors play a crucial role in the entry of filoviruses into host cells.
  • GPCR antagonists represent a promising class of compounds for developing novel anti-EBOV and anti-MARV therapies.
  • Targeting GPCRs offers a potential strategy for prophylactic and therapeutic interventions against filoviral outbreaks.

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