Key result
Itraconazole and Estradiol benzoate inhibited SARS-CoV-2 viral entry in vitro by targeting the six-helix fusion core of the spike protein.
Why the study?
With no clinically effective drug available against SARS-CoV-2 infection, targeting the conserved membrane fusion domain of the spike protein represents a promising strategy to develop pan-coronavirus therapeutics.
Do Itraconazole and Estradiol benzoate inhibit SARS-CoV-2 viral entry in vitro?
Do Itraconazole and Estradiol benzoate inhibit SARS-CoV-2 viral entry in vitro?
Itraconazole and Estradiol benzoate demonstrate in vitro efficacy in blocking SARS-CoV-2 viral entry, suggesting potential as repurposed therapeutics for COVID-19.
Answers are grounded in this paper and cite their sources.
Hypothesis-generating for COVID-19 repurposing; leaves open in vivo efficacy and clinical translation.
SARS-CoV-2 caused the emerging epidemic of coronavirus disease in 2019 (COVID-19). To date, there are more than 82.9 million confirmed cases worldwide, there is no clinically effective drug against SARS-CoV-2 infection. The conserved properties of the membrane fusion domain of the spike (S) protein across SARS-CoV-2 make it a promising target to develop pan-CoV therapeutics. Herein, two clinically approved drugs, Itraconazole (ITZ) and Estradiol benzoate (EB), are found to inhibit viral entry by targeting the six-helix (6-HB) fusion core of SARS-CoV-2 S protein. Further studies shed light on the mechanism that ITZ and EB can interact with the heptad repeat 1 (HR1) region of the spike protein, to present anti-SARS-CoV-2 infections in vitro, indicating they are novel potential therapeutic remedies for COVID-19 treatment. Furthermore, ITZ shows broad-spectrum activity targeting 6-HB in the S2 subunit of SARS-CoV and MERS-CoV S protein, inspiring that ITZ have the potential for development as a pan-coronavirus fusion inhibitor.
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Yang et al. (2021) studied COVID-19. Itraconazole and Estradiol benzoate was evaluated on Inhibition of viral entry by targeting the six-helix (6-HB) fusion core of SARS-CoV-2 S protein. Itraconazole and Estradiol benzoate inhibited SARS-CoV-2 viral entry in vitro by targeting the six-helix fusion core of the spike protein.
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