{"id":105,"date":"2018-02-21T14:32:50","date_gmt":"2018-02-21T05:32:50","guid":{"rendered":"http:\/\/glycoaware.com\/tokai-u\/?page_id=105"},"modified":"2018-10-30T18:59:29","modified_gmt":"2018-10-30T09:59:29","slug":"shape-shifting-supramolecule","status":"publish","type":"page","link":"http:\/\/glycoaware.com\/tokai-u\/shape-shifting-supramolecule\/","title":{"rendered":"Shape Shifting Supramolecule"},"content":{"rendered":"<p><strong><img loading=\"lazy\" decoding=\"async\" class=\"size-medium wp-image-99 alignright\" src=\"http:\/\/glycoaware.com\/tokai-u\/wp-content\/uploads\/shapeimage_2-300x145.png\" alt=\"\" width=\"300\" height=\"145\" srcset=\"http:\/\/glycoaware.com\/tokai-u\/wp-content\/uploads\/shapeimage_2-300x145.png 300w, http:\/\/glycoaware.com\/tokai-u\/wp-content\/uploads\/shapeimage_2.png 385w\" sizes=\"auto, (max-width: 300px) 100vw, 300px\" \/>Supramolecule that Changes Its Structure on Binding with Receptor Molecule<br \/>\n<\/strong><\/p>\n<p>A novel strategy for the inhibition of influenza virus infection by\u00a0disrupting the receptor functions was\u00a0proposed and described. \u00a0A\u00a0polymeric inhibitor that contains lyso GM3\u00a0ganglioside was synthesized as\u00a0amphiphilic polymer with receptor\u00a0specific ligands.<\/p>\n<p>9-Fluorenylmethyloxylcarbonyl (Fmoc) protected\u00a0(\u03b5-amino group) L-lysine was attached with the fluorescent tag BODIPY,\u00a0which was then coupled with lyso GM3\u00a0ganglioside to yield a fluorescent GM3\u00a0analog. Removal of the Fmoc group followed by amide formation with\u00a0activated poly-L-glutamic acid (PGA) provided lyso GM3-PGA containing the BODIPY fluorophore. The lyso GM3\u00a0content was calculated from the u.v. absorption of the fluorophore to\u00a0be 3 mol %. Because of the\u00a0amphiphilic nature, the polymer was shown to\u00a0have folded structure in aqueous media. The inhibitory\u00a0activities of\u00a0lyso GM3-PGA, lyso GM3, and GM3\u00a0oligosaccharide (sialyl lactose)\u00a0against the binding of\u00a0influenza A\/PR\/8\/34 (H1N1) were investigated using an ELISA assay. The IC<sub>50<\/sub>\u00a0values for the polymeric\u00a0inhibitor, GM3, lyso GM3, and sialyllactose were 7.5 x 10<sup>-12<\/sup>, 1.0 x 10<sup>-9<\/sup>, 3.0 x 10<sup>-9<\/sup>, and 1.5 x 10<sup>-7<\/sup>\u00a0molar,\u00a0respectively, based on monomeric sialic acid. PGA showed no inhibition against the influenza.<\/p>\n<p>Furthermore, later we discovered the type of polymer ligand-type inhibitor synergistically inhibits influenza virus infection together with zanamivir and\u00a0oseltamivir, thus is considered as a new potential candidate for influenza control and for use in combination with NAI drugs for minimizing toxicity, delayed development of resistance.<\/p>\n<p>Although we did not stress the polymer was found to inhibit both HA and NA. This effect was considered due to a part of the steric stabilization of a viral particle by this polymer. We postulate a mechanism to the polymer backbone interferes the NA reaction as the polymer rap around the virus.<\/p>\n<p><img loading=\"lazy\" decoding=\"async\" class=\"aligncenter wp-image-103\" src=\"http:\/\/glycoaware.com\/tokai-u\/wp-content\/uploads\/Polymer.dark_.pict_.jpg\" alt=\"\" width=\"589\" height=\"453\" srcset=\"http:\/\/glycoaware.com\/tokai-u\/wp-content\/uploads\/Polymer.dark_.pict_.jpg 456w, http:\/\/glycoaware.com\/tokai-u\/wp-content\/uploads\/Polymer.dark_.pict_-300x231.jpg 300w\" sizes=\"auto, (max-width: 589px) 100vw, 589px\" \/><\/p>\n<p><strong>Reference<\/strong><\/p>\n<p class=\"paragraph_style_5\"><a class=\"class1\" title=\"http:\/\/www3.interscience.wiley.com\/journal\/10004797\/abstract\" href=\"http:\/\/www3.interscience.wiley.com\/journal\/10004797\/abstract\" target=\"_blank\" rel=\"noopener\">Lyso GM3 ganglioside-poly-L-glutamic acid conjugate as inhibitor of influenza hemagglutinin.\u00a0<\/a>Kamitakahara, H. Kanie, O. Wong, C,-H. <em><strong><span class=\"style_4\">Angew. Chem. Int. Ed.<\/span><\/strong><\/em>, <strong><span class=\"style_5\">1998<\/span><\/strong>, <em><span class=\"style_6\">37<\/span><\/em>, 1524-1528.<\/p>\n<p><a href=\"https:\/\/academic.oup.com\/jac\/article\/70\/10\/2797\/831314\" target=\"_blank\" rel=\"noopener\">6SLN-lipo PGA specifically catches (coats) human influenza virus and synergizes neuraminidase-targeting drugs for human influenza therapeutic potential.\u00a0<\/a>Sriwilaijaroen, N. <em>et al. <strong>J. Antimicrob. Chemother.<\/strong><\/em>, <strong>2015<\/strong>, <em>70<\/em>, 2797-2809.<\/p>\n<p>&nbsp;<\/p>\n","protected":false},"excerpt":{"rendered":"<p>Supramolecule that Changes Its Structure on Binding with Receptor Mole\u2026<\/p>\n<p> <a class=\"continue-reading-link\" href=\"http:\/\/glycoaware.com\/tokai-u\/shape-shifting-supramolecule\/\"><span>Continue reading<\/span><i class=\"crycon-right-dir\"><\/i><\/a> <\/p>\n","protected":false},"author":1,"featured_media":0,"parent":0,"menu_order":0,"comment_status":"closed","ping_status":"closed","template":"","meta":{"footnotes":""},"class_list":["post-105","page","type-page","status-publish","hentry"],"_links":{"self":[{"href":"http:\/\/glycoaware.com\/tokai-u\/wp-json\/wp\/v2\/pages\/105","targetHints":{"allow":["GET"]}}],"collection":[{"href":"http:\/\/glycoaware.com\/tokai-u\/wp-json\/wp\/v2\/pages"}],"about":[{"href":"http:\/\/glycoaware.com\/tokai-u\/wp-json\/wp\/v2\/types\/page"}],"author":[{"embeddable":true,"href":"http:\/\/glycoaware.com\/tokai-u\/wp-json\/wp\/v2\/users\/1"}],"replies":[{"embeddable":true,"href":"http:\/\/glycoaware.com\/tokai-u\/wp-json\/wp\/v2\/comments?post=105"}],"version-history":[{"count":10,"href":"http:\/\/glycoaware.com\/tokai-u\/wp-json\/wp\/v2\/pages\/105\/revisions"}],"predecessor-version":[{"id":688,"href":"http:\/\/glycoaware.com\/tokai-u\/wp-json\/wp\/v2\/pages\/105\/revisions\/688"}],"wp:attachment":[{"href":"http:\/\/glycoaware.com\/tokai-u\/wp-json\/wp\/v2\/media?parent=105"}],"curies":[{"name":"wp","href":"https:\/\/api.w.org\/{rel}","templated":true}]}}