CAS: 3554-93-6; N-((2S,3R,4R,5R,6R)-2-(Benzyloxy)-4,5-Dihydroxy-6-(Hydroxymethyl)Tetrahydro-2H-Pyran-3-yl)Acetamide

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CAS号3554-96-9 苄基2-乙酰氨基-2-脱氧-3... | CAS号93496-44-7 苄基2-乙酰氨基-2-脱氧-6...

📜D-(+)-Galactosamine Hydrochloride置于盐酸,Sodium Methylate体系中,用 甲醇,水 作为反应溶剂,化学反应 32.5H,反应生成 苄基-2-乙酰胺基-2-脱氧-Alpha-D-吡喃半乳糖苷
参考文献:对muramyl二肽的结构修饰以研究人类nod2刺激活性的进一步见解.
标题:对muramyl二肽的结构修饰以研究人类nod2刺激活性的进一步见解.
摘要:合成了一系列在murnac的c4位置和肽部分的d-异-谷氨酰胺(iso Gln)残基上具有结构修饰的多胺基二肽(mdp)类似物.通过使用cuaac点击策略将叠氮基叠氮基二聚二肽前体与结构上不同的炔烃偶联,可以方便地实现murnac的c4多样化.d-谷氨酸(glu),替换为iso通过羧酸的酯化或酰胺化将gln用于结构多样性.总共合成了26种mdp类似物并对其进行了生物评估,以研究人类nod2在先天免疫应答中的刺激活性.有趣的是,发现具有酯部分的mdp衍生物比参考化合物mdp本身或含有酰胺部分的mdp类似物更有效.在酯衍生物的不同长度的烷基链中,带有d-谷氨酸十二烷基(c12)酯部分的mdp类似物显示出最佳的nod2刺激能力.
DOI:10.1002/asia.202001003

专利信息

专利号:US-4943630-A
优先权日:1982-10-27
标题 :Method for carrying out the organic synthesis of oligosaccharides containing galactosamine-uronic acid patterns, new oligosaccharides obtained and biological applications thereof
发明人：JACQUINET JEAN-CLAUDE; PETITOU MAURICE; SINAY PIERRE; CHOAY JEAN
权利人:CHOAY SA
摘要:Process for the organic synthesis of oligosaccharides forming or corresponding to fragments of acid mucopolysaccharides wherein two compounds comprised of or terminated respectively by patterns of galactosamine structure and patterns of uronic acid structure. Said patterns are specifically substituted. Said process results in oligosaccharides usable particularly in therapy.

专利号:US-7338932-B2
优先权日:2000-05-11
标题 :Methods of modulating functions of polypeptide GalNAc-transferases and of screening test substances to find agents herefor, pharmaceutical compositions comprising such agents and the use of such agents for preparing medicaments
发明人：CLAUSEN HENRIK; BENNETT ERIC PAUL; HASSAN HELLE; REIS CELSO ALBUQUERQUE
权利人:GLYCOZYM APS
摘要:Attachment of O-glycans to proteins is controlled by a large family of homologous polypeptide GalNAc-transferases. Polypeptide GalNAc-transferases contain a C-terminal sequence with similarity to lectins. This invention discloses that the putative lectin domains of GalNAc-transferase isoforms, GalNAc-T4, -T7, -T2, and -T3, are functional and recognize carbohydrates, glycopeptides, and peptides and discloses the lectin domains of GalNAc-T1-T16. These lectin domains have different binding specificities and modulate the functions of GalNAc-transferase isoforms differently. Novel methods for identification of inhibitors or modulators of binding activities mediated by lectin domains of polypeptide GalNAc-transferases are disclosed. Direct binding activity of GalNAc-transferase lectins has been demonstrated for the first time and methods to measure lectin mediated binding of isolated lectins or enzymes with lectin domains are disclosed. The present invention specifically discloses a novel selective inhibitor of polypeptide GalNAc-transferase lectin domains, which provides a major advancement in that this inhibitor and related inhibitors sharing common characteristics of activity bind lectin domains without serving as acceptor substrate for glycosyltransferases involved in synthesis of O-glycans. This inhibitor is represented by the β-anomeric configuration of GalNAc-benzyl, GalNAcβ-benzyl. Methods for inhibiting intracellular transport, cell surface expression, and secretion of mucins and O-glycosylated glycoproteins without affecting O-glycosylation processing are disclosed using the novel selective inhibitor identified.

专利号:EP-1558728-B1
优先权日:2002-11-08
标 题:Methods to identify agents modulating functions of polypeptide galnac-transferases, pharmaceutical compositions comprising such agents and the use of such agents for preparing medicaments
发明人：CLAUSEN HENRIK; BENNETT ERIC PAUL
权利人:GLYCOZYM APS
摘要:Novel methods for identification of inhibitors or modulators of binding activities mediated by lectin domains of polypeptide GalNAc-transferases are disclosed. Direct binding activity of GalNAc-transferase lectins has been demonstrated for the first time and methods to measure lectin mediated binding of isolated lectins or enzymes with lectin domains are disclosed. The present invention specifically discloses a novel selective inhibitor of polypeptide GalNAc-transferase lectin domains, which provides a major advancement in that this inhibitor and related inhibitors sharing common characteristics of activity bind lectin domains without serving as acceptor substrate for glycosyltransferases involved in synthesis of O-glycans. This inhibitor is represented by the O-anomeric configuration of GalNAc-benzyl, GalNAcbeta-benzyl. Methods for inhibiting intracellular transport, cell surface expression, and secretion of mucins and O-glycosylated glycoproteins without affecting O-glycosylation processing are disclosed using the novel selective inhibitor identified.

专利号:US-12227788-B2
优先权日:2014-11-12
标题 :Compositions, methods and treatments for inhibiting cell adhesion and virus binding and penetration
发明人：MATTA KHUSHI L
权利人:TUMOREND LLC
摘要:Disclosed herein are glyco-decoy acceptor compositions that sidetrack or inhibit the activity of biosynthetic enzymes participating in synthesis of ligands binding at selectin, galectin and siglecs receptors; methods of their preparation and uses in drug discovery and in treatments of diseases.

专利号:WO-8401777-A1
优先权日:1982-10-27
标 题 :Method for carrying out the organic synthesis of oligosaccharides containing galactosamine-uronic acid patterns, new oligosaccharides obtained and biological applications thereof

专利号:US-7629150-B2
优先权日:2000-09-01
标 题:Transformed cell harboring DNA or RNA encoding sugar chain synthesizing agent having β1,3-N-acetylglucosaminyltransferase activity
发明人：NARIMATSU HISASHI; SASAKI KATSUTOSHI; NATSUME AYUMI; MIO HIROYUKI; NAKAGAWA SATOSHI; SEKINE SUSUMU; TOGAYACHI AKIRA
权利人:KYOWA HAKKO KIRIN CO LTD
摘要:The present invention provides a novel polypeptide having a β1,3-N-acetylglucosaminyltransferase activity, an agent for synthesizing a sugar chain comprising the polypeptide, a process for producing a sugar chain or a complex carbohydrate using the agent for synthesizing a sugar chain, DNA encoding the polypeptide, a process for producing the polypeptide, an antibody against the polypeptide, and a diagnosis method and a medicament for treatment for inflammation, cancer or tumor metastasis using the DNA or the antibody. The present invention is useful for synthesis of a useful sugar chain and diagnosis and treatment for inflammatory diseases, cancer or tumor metastasis.