Heparin can target SARS-CoV-2 spike protein

The anticoagulant drug could be repurposed for COVID-19 treatment

January 28, 2021
Mel J. Yeates

LIVERPOOL, UK—An international team of researchers, led by the University of Liverpool and Keele University, has discovered that the anticoagulant drug heparin inhibits the SARS-CoV-2 virus spike protein. The research, which has been published in articles in British Journal of Pharmacology and Thrombosis and Haemostasis, found that heparin interacts with and destabilizes the spike protein’s structure — thereby preventing it from docking with the ACE2 receptor on human cells.

“This is exciting news since heparin could be rapidly repurposed to help alleviate COVID-19 infections, or possibly as a prophylactic treatment for high-risk groups such as medical staff or care workers,” said Professor Jeremy Turnbull from the Department of Biochemistry and Systems Biology at the University of Liverpool. “The results have also led us to investigate other novel compounds which mimic heparin that could potentially be effective against SARS-CoV-2.”

Molecular modeling by collaborators at Queensland University in Australia showed how heparin adheres to the surface of the spike protein to achieve these effects. Studies with live SARS-CoV-2, carried out at a Public Health England laboratory, proved that unfractionated heparin (but not low molecular weight heparins) could inhibit cell infectivity at doses similar to those used as an anticoagulant. The data strongly supported the clinical testing of inhaled (nebulized) unfractionated heparin, since the doses known to be delivered to the lungs would have potent anti-viral effects.

“These results strengthen the need for further investigation of heparin as a treatment in COVID-19 patients,” noted Dr. Quentin Nunes, consultant at the East Lancashire Hospitals NHS Trust, who is leading efforts to begin clinical trials of nebulised heparin in COVID-19 patients. 

“We also know that heparins inhibit a range of other viruses, so studying these drugs could provide new therapeutic strategies, and possibly a first-line of defense against emerging viral threats in the future — for example, while vaccines are developed,” added Dr. Mark Skidmore from the School of Life Sciences at Keele University, who co-led the research.

The researchers plan to further their work by exploring the potential of heparin, and heparin-mimicking compounds, as potential broad-spectrum antiviral drugs for COVID-19 and other future viral threats.

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