{"id":950,"date":"2024-01-03T18:59:47","date_gmt":"2024-01-03T17:59:47","guid":{"rendered":"https:\/\/sites.unimi.it\/apisgroup\/?p=950"},"modified":"2024-01-03T18:59:53","modified_gmt":"2024-01-03T17:59:53","slug":"identification-of-a-short-ace2-derived-stapled-peptide-targeting-the-sars-cov-2-spike-protein","status":"publish","type":"post","link":"https:\/\/sites.unimi.it\/apisgroup\/2024\/01\/03\/identification-of-a-short-ace2-derived-stapled-peptide-targeting-the-sars-cov-2-spike-protein\/","title":{"rendered":"Identification of a short ACE2-derived stapled peptide targeting the SARS-CoV-2 spike protein"},"content":{"rendered":"\n<p class=\"wp-block-paragraph\">The design and synthesis of a series of peptide derivatives based on a short ACE2 \u03b1-helix 1 epitope and subse\u0002quent [i &#8211; i+4] stapling of the secondary structure resulted in the identification of a 9-mer peptide capable to compete with recombinant ACE2 towards Spike RBD in the micromolar range. Specifically, SARS-CoV-2 Spike inhibitor screening based on colorimetric ELISA assay and structural studies by circular dichroism showed the ring-closing metathesis cyclization being capable to stabilize the helical structure of the 9-mer 34HEAEDLFYQ42 epitope better than the triazole stapling via click chemistry. MD simulations showed the stapled peptide being able not only to bind the Spike RBD, sterically interfering with ACE2, but also showing higher affinity to the target as compared to parent epitope.<\/p>\n\n\n\n<p class=\"wp-block-paragraph\"><a href=\"https:\/\/doi.org\/10.1016\/j.ejmech.2023.115118\">European Journal of Medicinal Chemistry 249 (2023) 115118<\/a><\/p>\n","protected":false},"excerpt":{"rendered":"<p>The design and synthesis of a series of peptide derivatives based on a short ACE2 \u03b1-helix 1 epitope and subse\u0002quent [i &#8211; i+4] stapling of the secondary structure resulted in the identification of a&#46;&#46;&#46;<\/p>\n","protected":false},"author":1,"featured_media":951,"comment_status":"open","ping_status":"open","sticky":false,"template":"","format":"standard","meta":{"footnotes":""},"categories":[6,109,69],"tags":[131,130],"class_list":["post-950","post","type-post","status-publish","format-standard","has-post-thumbnail","hentry","category-application","category-peptides","category-proteins","tag-ace2-derived","tag-sars-cov-2"],"yoast_head":"<!-- This site is optimized with the Yoast SEO plugin v28.5 - https:\/\/yoast.com\/product\/yoast-seo-wordpress\/ -->\n<title>Identification of a short ACE2-derived stapled peptide targeting the SARS-CoV-2 spike protein - APIS group<\/title>\n<meta name=\"robots\" content=\"noindex, follow\" \/>\n<meta property=\"og:locale\" content=\"it_IT\" \/>\n<meta property=\"og:type\" content=\"article\" \/>\n<meta property=\"og:title\" content=\"Identification of a short ACE2-derived stapled peptide targeting the SARS-CoV-2 spike protein - APIS 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