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10.1002/adtp.202000224

http://scihub22266oqcxt.onion/10.1002/adtp.202000224
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33786369!7994988!33786369
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suck abstract from ncbi


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pmid33786369      Adv+Ther+(Weinh) 2021 ; 4 (5): 2000224
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  • Drug Repurposing of Itraconazole and Estradiol Benzoate against COVID-19 by Blocking SARS-CoV-2 Spike Protein-Mediated Membrane Fusion #MMPMID33786369
  • Yang C; Pan X; Huang Y; Cheng C; Xu X; Wu Y; Xu Y; Shang W; Niu X; Wan Y; Li Z; Zhang R; Liu S; Xiao G; Xu W
  • Adv Ther (Weinh) 2021[May]; 4 (5): 2000224 PMID33786369show ga
  • 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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