{"id":547,"date":"2018-03-06T17:09:06","date_gmt":"2018-03-06T08:09:06","guid":{"rendered":"http:\/\/glycoaware.com\/tokai-u\/?page_id=547"},"modified":"2018-10-30T18:46:43","modified_gmt":"2018-10-30T09:46:43","slug":"dual-function-inhibitor","status":"publish","type":"page","link":"http:\/\/glycoaware.com\/tokai-u\/dual-function-inhibitor\/","title":{"rendered":"Dual Function Inhibitor"},"content":{"rendered":"<p><a href=\"http:\/\/glycoaware.com\/tokai-u\/wp-content\/uploads\/1.jpg\"><img loading=\"lazy\" decoding=\"async\" class=\"alignleft size-thumbnail wp-image-553\" src=\"http:\/\/glycoaware.com\/tokai-u\/wp-content\/uploads\/1-150x150.jpg\" alt=\"\" width=\"150\" height=\"150\" \/><\/a>Themagglutinin (HA) and neuraminidase (NA; sialidase) are responsible for immunogenicity and infection process of Influenza virus. The successful molecular design of inhibitors against NA based on X-ray crystallography shows a direction of our future development of pharmaceutical drugs.<\/p>\n<p>Most of the commercial Influenza drugs are targeted toward NA. A reason for this is because it is easy. NA has deep cavity inside it there are catalytic site, in such case we can expect various binding enhancements. The situation differs in HA binding site against silalyated glycan structures. The biding site is shallow and there is no ionic side chains of constituting amino acids available for designing anti-HA agents.<a href=\"http:\/\/glycoaware.com\/tokai-u\/wp-content\/uploads\/5.jpg\"><img loading=\"lazy\" decoding=\"async\" class=\"size-thumbnail wp-image-552 alignright\" src=\"http:\/\/glycoaware.com\/tokai-u\/wp-content\/uploads\/5-150x150.jpg\" alt=\"\" width=\"150\" height=\"150\" \/><\/a><a href=\"http:\/\/glycoaware.com\/tokai-u\/wp-content\/uploads\/4.jpg\"><img loading=\"lazy\" decoding=\"async\" class=\"alignleft size-thumbnail wp-image-551\" src=\"http:\/\/glycoaware.com\/tokai-u\/wp-content\/uploads\/4-150x150.jpg\" alt=\"\" width=\"150\" height=\"150\" \/><\/a><\/p>\n<p>Regardless of the difficulty in anti-HA drugs. We proposed a possibility of inhibiting both NA and HA with a hope that such a compound may prevent emergence of drug resistant virus strains. Let us consider a provability of emergence of resistant strain is 1\/100,000. The number now is applied to two different RNA coding HA and NA.\u00a0 This makes a chance for the virus to escape from the dual functional drug extremely low.<\/p>\n<p>For this reason, we examined our hypothesis by synthesizing a series of sialic acid derivatives. One of the important idea for the designing molecules is to find a spot in the sialic acid residue that is not recognized by both HA and NA.<\/p>\n<p>&nbsp;<\/p>\n<p><strong>Reference<\/strong><\/p>\n<p><a href=\"http:\/\/onlinelibrary.wiley.com\/doi\/10.1002\/1099-0690(200007)2000:14%3C2643::AID-EJOC2643%3E3.0.CO;2-1\/abstract\" target=\"_blank\" rel=\"noopener\">Sun, X.-L.\u00a0<em>et al<\/em>. <em><strong>Eur. J. Org. Chem.<\/strong><\/em>,\u00a0<strong>2000<\/strong>,\u00a0<em>14<\/em>, 2643-2653.<\/a><\/p>\n<p><a href=\"https:\/\/doi.org\/10.1093\/glycob\/12.3.183\" target=\"_blank\" rel=\"noopener\">Guo, C.-T.\u00a0<em>et al<\/em>. <em><strong>Glycobiology<\/strong><\/em>,\u00a0<strong>2002<\/strong>,\u00a0<em>12<\/em>, 183-190.<\/a><\/p>\n<p>&nbsp;<\/p>\n<hr \/>\n<p><span class=\"style_4\">\u30a4\u30f3\u30d5\u30eb\u30a8\u30f3\u30b6\u30a6\u30a4\u30eb\u30b9\u306e\u8868\u9762\u306b\u3042\u308b\uff12\u7a2e\u985e\u306e\u30bf\u30f3\u30d1\u30af\u8cea\u3092\u540c\u6642\u306b\u963b\u5bb3\u3057\u3088\u3046\u3068\u3059\u308b\u300c\u30c7\u30e5\u30a2\u30eb\u30d5\u30a1\u30f3\u30af\u30b7\u30e7\u30f3\u300d\u306e\u8003\u3048\u65b9\u306f\u3001\u5358\u306b\u9762\u767d\u3044\u4ee5\u4e0a\u306e\u52b9\u679c\u3092\u671f\u5f85\u3059\u308b\u3053\u3068\u304c\u3067\u304d\u307e\u3059\u3002\u4eee\u306b\uff11\uff0f\uff11\uff10\uff10\uff10\uff10\uff10\u306e\u78ba\u7acb\u3067\u85ac\u5264\u8010\u6027\u682a\u304c\u51fa\u73fe\u3057\u305f\u3068\u3059\u308b\u3068\uff12\u3064\u963b\u5bb3\u3059\u308b\u3068\u3001\u3046\u307e\u304f\u884c\u3051\u3070\u3053\u306e\uff12\u4e57\u306e\u78ba\u7387\u3068\u306a\u308b\u306e\u3067\u3001\u8010\u6027\u682a\u306e\u51fa\u73fe\u3092\u62bc\u3055\u3048\u8fbc\u3080\u3053\u3068\u304c\u3067\u304d\u308b\u3068\u8003\u3048\u3089\u308c\u307e\u3059\u3002<\/span><span class=\"style_4\"><br \/>\n<\/span><\/p>\n","protected":false},"excerpt":{"rendered":"<p>Themagglutinin (HA) and neuraminidase (NA; sialidase) are responsible \u2026<\/p>\n<p> <a class=\"continue-reading-link\" href=\"http:\/\/glycoaware.com\/tokai-u\/dual-function-inhibitor\/\"><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-547","page","type-page","status-publish","hentry"],"_links":{"self":[{"href":"http:\/\/glycoaware.com\/tokai-u\/wp-json\/wp\/v2\/pages\/547","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=547"}],"version-history":[{"count":12,"href":"http:\/\/glycoaware.com\/tokai-u\/wp-json\/wp\/v2\/pages\/547\/revisions"}],"predecessor-version":[{"id":685,"href":"http:\/\/glycoaware.com\/tokai-u\/wp-json\/wp\/v2\/pages\/547\/revisions\/685"}],"wp:attachment":[{"href":"http:\/\/glycoaware.com\/tokai-u\/wp-json\/wp\/v2\/media?parent=547"}],"curies":[{"name":"wp","href":"https:\/\/api.w.org\/{rel}","templated":true}]}}