LARGE SCALE ENZYMATIC SYNTHESIS OF OLIGOSACCHARIDES
    281.
    发明申请
    LARGE SCALE ENZYMATIC SYNTHESIS OF OLIGOSACCHARIDES 审中-公开
    大规模合成低聚糖

    公开(公告)号:WO2014031602A1

    公开(公告)日:2014-02-27

    申请号:PCT/US2013/055731

    申请日:2013-08-20

    CPC classification number: C12P19/18 C12P19/04 C12Y207/0701

    Abstract: A novel UDP-Gal regeneration process and its combined use with a galactosyltransferease to add galactose to a suitable acceptor substrate. Also described herein are synthetic methods for generating Globo-series oligosaccharides in large scale, wherein the methods may involve the combination of a glycosyltransferase reaction and a nucleotide sugar regeneration process.

    Abstract translation: 一种新型的UDP-Gal再生过程及其与半乳糖基转移酶的组合使用,以将半乳糖添加到合适的受体底物。 本文还描述了大规模生产Globo系列寡糖的合成方法,其中所述方法可涉及糖基转移酶反应和核苷酸糖再生过程的组合。

    QUANTITATIVE MEASUREMENT OF NANO / MICRO PARTICLE ENDOCYTOSIS WITH CELL MASS SPECTROMETRY
    286.
    发明申请
    QUANTITATIVE MEASUREMENT OF NANO / MICRO PARTICLE ENDOCYTOSIS WITH CELL MASS SPECTROMETRY 审中-公开
    纳米/微粒子内毒素与细胞质谱的定量测量

    公开(公告)号:WO2011123479A1

    公开(公告)日:2011-10-06

    申请号:PCT/US2011/030407

    申请日:2011-03-29

    CPC classification number: G01N33/5091 G01N33/5008 G01N33/569 G01N33/6848

    Abstract: Methods for detecting the presence of nanoparticles or microparticles by cell mass spectrometry (CMS) are provided. CMS methods are provided for determining the number of nanoparticles or microparticles in each cell. Nanoparticles whose intracellular concentration can be determines by the CMS methods of the invention include polymeric nanoparticles (NPs), liposomes, viral-based NPs, carbon nanotubes, diamond NPs, polymeric micelles, nanocarriers, liposomes, and viral nanoparticles. Determination of the efficiency of drug delivery and intracellular titer of pathogens according to the invention is disclosed. Methods for determining intracellular uptake of virus particles are provided.

    Abstract translation: 提供了通过细胞质谱法(CMS)检测纳米颗粒或微粒的存在的方法。 提供CMS方法用于确定每个细胞中纳米颗粒或微粒的数量。 通过本发明的CMS方法可以确定其细胞内浓度的纳米颗粒包括聚合物纳米颗粒(NP),脂质体,基于病毒的NP,碳纳米管,金刚石NP,聚合胶束,纳米载体,脂质体和病毒纳米颗粒。 公开了根据本发明的药物递送效率和病原体细胞内滴度的测定。 提供了确定病毒颗粒的细胞内吸收的方法。

    ALPHA-SELECTIVE SIALYL PHOSPHATE DONORS FOR PREPARATION OF SIALOSIDES AND SIALOSIDE ARRAYS FOR INFLUENZA VIRUS DETECTION
    287.
    发明申请
    ALPHA-SELECTIVE SIALYL PHOSPHATE DONORS FOR PREPARATION OF SIALOSIDES AND SIALOSIDE ARRAYS FOR INFLUENZA VIRUS DETECTION 审中-公开
    用于制备用于流感病毒检测的糖尿病和糖尿病病毒颗粒的ALPHA-选择性磷酸二氢钠

    公开(公告)号:WO2010111703A1

    公开(公告)日:2010-09-30

    申请号:PCT/US2010/029058

    申请日:2010-03-29

    Abstract: A novel N-acetyl-5- N ,4- O -carbonyl-protected dibutyl sialyl phosphate donor for sialylation of both primary and sterically hindered secondary acceptors to prepare sialosides with high yield and α-selectivity is disclosed. Methods for making disaccharide building blocks comprising α(2→3), α(2→6), α(2→8), α(2→8)/α(2→9) alternate, and α(2→9) sialosides are provided. methods for one-pot synthesis of complex sialosides are disclosed. Libraries of sialosides and methods for using the libraries for detection and receptor binding analysis of surface glycoproteins or pathogens and cancer cells are disclosed. Methods for distinguishing between hemagglutanin (HA) from various strains of influenza are provided.

    Abstract translation: 公开了一种新型的N-乙酰基-5-N,4-O-羰基保护的二丁基唾液酸磷酸盐供体,用于主要和空间位阻二级受体的唾液酸化,以高产率和选择性选择性制备唾液酸苷。 包含(2→3),(2→6),(2〜8),(2〜8)/ a(2〜9)交替和(2〜9) 提供唾液酸苷。 公开了一锅合成唾液酸苷的方法。 公开了唾液酸的文库和使用文库进行表面糖蛋白或病原体和癌细胞的检测和受体结合分析的方法。 提供了用于区分来自各种流感病毒株的血凝素(HA)的方法。

    ALPHA-GALACTOSYL CERAMIDE ANALOGS AND THEIR USE AS IMMUNOTHERAPIES
    290.
    发明申请
    ALPHA-GALACTOSYL CERAMIDE ANALOGS AND THEIR USE AS IMMUNOTHERAPIES 审中-公开
    ALPHA-GALACTOSYL CERAMIDE ANALOGS及其作为免疫球蛋白使用

    公开(公告)号:WO2008128207A1

    公开(公告)日:2008-10-23

    申请号:PCT/US2008060275

    申请日:2008-04-14

    Abstract: The present disclosure relates to synthetic alpha-galactosyl ceramide (a-GalCer) analogs, and their use as immunotherapies. In one aspect, a method of activating a cytokine response in a subject includes administering an effective amount of a compound to a subject, wherein the subject has an adaptive immune system that includes a population of cells, the population including at least one lymphocyte and at least one antigen-presenting cell, and wherein the compound is represented by the structure of formula (1) wherein, n is 0 to 25; X is selected from O and S; R 1 is selected from H, CH 3 , and phenyl, where phenyl is optionally substituted with H, OH, OCH 3 , F, CF 3 , phenyl, phenyl-F, C 1 -C 6 alkyl, or C 2 -C 6 branched alkyl; R 2 is selected from OH and H; R 3 is selected from C 1 -C 15 alkyl, and phenyl, where phenyl is optionally substituted with H, OH, OCH 3 , F, CF 3 , phenyl, C 1 -C 6 alkyl, or C 2 -C 6 branched alkyl; R 4 is selected from OH, OSO 3 H, OSO 3 Na, and OSO 3 K; and R 5 is selected from CH 2 OH and CO 2 H; or a pharmaceutically acceptable salt thereof; forming a complex between the compound and the antigen-presenting cell, wherein the formation of the complex results in the activation of a receptor on the lymphocyte; and activating the lymphocyte to produce the cytokine response.

    Abstract translation: 本公开内容涉及合成的α-半乳糖神经酰胺(a-GalCer)类似物,以及它们作为免疫治疗的用途。 一方面,在受试者中激活细胞因子应答的方法包括向受试者施用有效量的化合物,其中所述受试者具有包括细胞群的适应性免疫系统,所述群体包括至少一种淋巴细胞和 至少一个抗原呈递细胞,并且其中所述化合物由式(1)的结构表示,其中n为0至25; X选自O和S; R 1选自H,CH 3和苯基,其中苯基任选被H,OH,OCH 3,F,CF 苯基,苯基-F,C 1 -C 6烷基或C 2 -C 6亚烷基 >支链烷基; R 2选自OH和H; R 3选自C 1 -C 15烷基和苯基,其中苯基任选被H,OH,OCH 3取代, 3,F,CF 3,苯基,C 1 -C 6烷基或C 2 H 2 -C 6 -C 6支链烷基; R 4选自OH,OSO 3 H,OSO 3 Na和OSO 3 K; 和R 5选自CH 2 OH和CO 2 H; 或其药学上可接受的盐; 在化合物和抗原呈递细胞之间形成复合物,其中复合物的形成导致淋巴细胞上受体的活化; 并激活淋巴细胞以产生细胞因子反应。

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