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10.1016/j.virol.2021.05.009

http://scihub22266oqcxt.onion/10.1016/j.virol.2021.05.009
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34052578!8144927!34052578
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suck abstract from ncbi


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pmid34052578      Virology 2021 ; 560 (ä): 110-115
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  • Azelastine inhibits viropexis of SARS-CoV-2 spike pseudovirus by binding to SARS-CoV-2 entry receptor ACE2 #MMPMID34052578
  • Ge S; Lu J; Hou Y; Lv Y; Wang C; He H
  • Virology 2021[Aug]; 560 (ä): 110-115 PMID34052578show ga
  • A recent study have reported that pre-use of azelastine is associated with a decrease in COVID-19 positive test results among susceptible elderly people. Besides, it has been reported that antihistamine drugs could prevent viruses from entering cells. The purpose of this study is to investigate whether azelastine have antiviral activity against SARS-CoV-2 in vitro and the possible mechanism. Here, we discovered antihistamine azelastine has an affinity to ACE2 by cell membrane chromatography (CMC); Then we determined the equilibrium dissociation constant (K(D)) of azelastine-ACE2 as (2.58 +/- 0.48) x 10(-7) M by surface plasmon resonance (SPR). The results of molecular docking showed that azelastine could form an obvious hydrogen bond with Lys353. The pseudovirus infection experiments showed that azelastine effectively inhibited viral entry (EC(50) = 3.834 muM). Our work provides a new perspective for the screening method of drug repositioning for COVID-19, and an attractive and promising drug candidate for anti-SARS-CoV-2.
  • |Angiotensin-Converting Enzyme 2/*metabolism[MESH]
  • |Antiviral Agents/metabolism/*pharmacology[MESH]
  • |Cell Membrane/metabolism[MESH]
  • |Chromatography, Affinity[MESH]
  • |Drug Repositioning[MESH]
  • |HEK293 Cells[MESH]
  • |Histamine H1 Antagonists, Non-Sedating/metabolism/pharmacology[MESH]
  • |Humans[MESH]
  • |Molecular Docking Simulation[MESH]
  • |Phthalazines/metabolism/*pharmacology[MESH]
  • |Protein Binding[MESH]
  • |SARS-CoV-2[MESH]
  • |Spike Glycoprotein, Coronavirus/*antagonists & inhibitors/metabolism[MESH]


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