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Imatinib inhibits SARS-CoV-2 infection by an off-target-mechanism

Romano Strobelt1, Julia Adler1, Nir Paran2

  • 1Department of Molecular Genetics, Weizmann Institute of Science, Rehovot, Israel.

Scientific Reports
|April 7, 2022
PubMed

Insights

Imatinib, an Abl tyrosine kinase inhibitor, effectively reduces SARS-CoV-2 infection by inhibiting viral entry. This repurposed drug shows promise for treating COVID-19 by targeting the Spike protein.

Area of Science:

  • Virology
  • Pharmacology
  • Drug Repurposing

Background:

  • The COVID-19 pandemic, caused by SARS-CoV-2, necessitates urgent therapeutic interventions.
  • Repurposing existing FDA-approved drugs offers a faster and more cost-effective approach to drug development compared to de novo design.

Purpose of the Study:

  • To investigate the potential of imatinib, an Abl tyrosine kinase inhibitor, as a therapeutic agent against SARS-CoV-2.
  • To elucidate the mechanism by which imatinib inhibits SARS-CoV-2 infection.

Main Methods:

  • Testing imatinib's efficacy against SARS-CoV-2 and a surrogate lentivector pseudotype.
  • Quantifying SARS-CoV-2 Spike-mediated cell-cell membrane fusion in real-time.
  • Utilizing cellular thermal shift assay (CETSA) to detect direct drug-target interactions.

Main Results:

  • Imatinib significantly decreased SARS-CoV-2 infection and viral entry via endocytosis and membrane fusion.
  • Imatinib inhibited Spike-hACE2 mediated membrane fusion independently of Abl1 and Abl2.
  • CETSA confirmed a direct interaction between imatinib and the SARS-CoV-2 Spike protein, altering its trypsin susceptibility.

Conclusions:

  • Imatinib demonstrates robust antiviral activity against SARS-CoV-2 by inhibiting early infection steps.
  • The mechanism involves an off-target interaction with the Spike protein, hindering viral entry.
  • Imatinib represents a promising candidate for COVID-19 therapy, particularly for inhibiting viral entry.

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