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Stapled ACE2 peptidomimetics designed to target the SARS-CoV-2 spike protein do not prevent virus internalization.
Morgan, Danielle C; Morris, Caroline; Mahindra, Amit; Blair, Connor M; Tejeda, Gonzalo; Herbert, Imogen; Turnbull, Matthew L; Lieber, Gauthier; Willett, Brian J; Logan, Nicola; Smith, Brian; Tobin, Andrew B; Bhella, David; Baillie, George; Jamieson, Andrew G.
  • Morgan DC; School of Chemistry, University of Glasgow Glasgow UK.
  • Morris C; School of Chemistry, University of Glasgow Glasgow UK.
  • Mahindra A; School of Chemistry, University of Glasgow Glasgow UK.
  • Blair CM; School of Chemistry, University of Glasgow Glasgow UK.
  • Tejeda G; MRC-University of Glasgow Centre for Virus Research Glasgow UK.
  • Herbert I; Sir Michael Stoker Building Glasgow UK.
  • Turnbull ML; Centre for Translational Pharmacology Institute of Molecular Cell and Systems Biology, Davidson Building, University of Glasgow Glasgow UK.
  • Lieber G; Centre for Translational Pharmacology Institute of Molecular Cell and Systems Biology, Davidson Building, University of Glasgow Glasgow UK.
  • Willett BJ; MRC-University of Glasgow Centre for Virus Research Glasgow UK.
  • Logan N; MRC-University of Glasgow Centre for Virus Research Glasgow UK.
  • Smith B; MRC-University of Glasgow Centre for Virus Research Glasgow UK.
  • Tobin AB; MRC-University of Glasgow Centre for Virus Research Glasgow UK.
  • Bhella D; MRC-University of Glasgow Centre for Virus Research Glasgow UK.
  • Baillie G; Centre for Translational Pharmacology Institute of Molecular Cell and Systems Biology, Davidson Building, University of Glasgow Glasgow UK.
  • Jamieson AG; Centre for Translational Pharmacology Institute of Molecular Cell and Systems Biology, Davidson Building, University of Glasgow Glasgow UK.
Pept Sci (Hoboken) ; 113(4): e24217, 2021 Jul.
Article in English | MEDLINE | ID: covidwho-1014097
ABSTRACT
COVID-19 is caused by a novel coronavirus called severe acute respiratory syndrome-coronavirus 2 (SARS-CoV-2). Virus cell entry is mediated through a protein-protein interaction (PPI) between the SARS-CoV-2 spike protein and angiotensin-converting enzyme 2 (ACE2). A series of stapled peptide ACE2 peptidomimetics based on the ACE2 interaction motif were designed to bind the coronavirus S-protein RBD and inhibit binding to the human ACE2 receptor. The peptidomimetics were assessed for antiviral activity in an array of assays including a neutralization pseudovirus assay, immunofluorescence (IF) assay and in-vitro fluorescence polarization (FP) assay. However, none of the peptidomimetics showed activity in these assays, suggesting that an enhanced binding interface is required to outcompete ACE2 for S-protein RBD binding and prevent virus internalization.
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Full text: Available Collection: International databases Database: MEDLINE Language: English Journal: Pept Sci (Hoboken) Year: 2021 Document Type: Article

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Full text: Available Collection: International databases Database: MEDLINE Language: English Journal: Pept Sci (Hoboken) Year: 2021 Document Type: Article