Inhibitors of E-, P- and L-selectin binding
    2.
    发明授权
    Inhibitors of E-, P- and L-selectin binding 失效
    E-,P-和L-选择素结合的抑制剂

    公开(公告)号:US5830871A

    公开(公告)日:1998-11-03

    申请号:US744744

    申请日:1996-10-28

    CPC分类号: C07H7/02 C07H15/00

    摘要: Inhibitors of E-, P- and L-selectin binding are synthesized by an aldol addition reaction between a glycoside aldehyde precursor and dihydroxyacetone phosphate or a derivative thereof. The addition reaction is catalyzed by aldolase. The inhibitors exhibit an activity comparable to sialyl Lewis X with respect to the E-selectin binding assay and high activities in the P- and L-selectin binding assays. The inhibitors are employable for blocking neutrophil inflamatory conditions.

    摘要翻译: 通过醛糖醛前体和磷酸二羟丙酮或其衍生物之间的醛醇醛加成反应合成E-,P-和L-选择蛋白结合的抑制剂。 加成反应由醛缩酶催化。 相对于E-选择蛋白结合测定,抑制剂表现出与唾液酸基路易斯X相当的活性,并且P-和L-选择蛋白结合测定中的高活性。 抑制剂可用于阻断嗜中性粒细胞炎症状况。

    Quantitative analysis of carbohydrate-protein interactions using glycan microarrays: determination of surface and solution dissociation constants
    5.
    发明授权
    Quantitative analysis of carbohydrate-protein interactions using glycan microarrays: determination of surface and solution dissociation constants 有权
    使用聚糖微阵列对碳水化合物 - 蛋​​白质相互作用的定量分析:测定表面和溶液解离常数

    公开(公告)号:US08906832B2

    公开(公告)日:2014-12-09

    申请号:US12423733

    申请日:2009-04-14

    摘要: A method, system and device to identify, study and/or mimic carbohydrate-protein interactions on cell surfaces and in solution measured by a glycan microarray. In some instances the method, system and device uses very small quantities of carbohydrate as low as attomol. In some instances the system, method and device is high-throughput. The small quantity sensitivity may allow for close placement of carbohydrate array members wherein due to close proximity multivalent interactions with proteins may be identified.

    摘要翻译: 鉴定,研究和/或模拟细胞表面和聚糖微阵列测量溶液中碳水化合物 - 蛋​​白质相互作用的方法,系统和装置。 在某些情况下,该方法,系统和装置使用非常少量的碳水化合物,与阿托莫尔一样低。 在某些情况下,系统,方法和设备是高吞吐量的。 小量的灵敏度可以允许碳水化合物阵列成员的紧密放置,其中由于与蛋白质的近似多价相互作用可以被鉴定。

    GLYCOPROTEOMIC PROBES FOR FLUORESCENT IMAGING OF FUCOSYLATED GLYCANS IN VIVO
    8.
    发明申请
    GLYCOPROTEOMIC PROBES FOR FLUORESCENT IMAGING OF FUCOSYLATED GLYCANS IN VIVO 有权
    血液中富含荧光成像的GLYCOPROTEOMIC PROBES

    公开(公告)号:US20110257376A1

    公开(公告)日:2011-10-20

    申请号:US13053192

    申请日:2011-03-21

    IPC分类号: C07K14/47 C07H19/207

    摘要: Methods are provided for labeling cellular glycans bearing azide groups via fluorescent labeling comprising Cu(I)-catalyzed [3+2] cycloaddition of a probe comprising alkynyl group. Generation of fluorescent probes from a nonfluorescent precursor, 4-ethynyl-N-ethyl-1,8-naphthalimide, by Cu(I)-catalyzed [3+2] cycloaddition of the alkyne group of the probe to an azido-modified sugar are provided. Incorporation of azido-containing fucose analog into glycoconjugates via the fucose salvage pathway are disclosed. Fluorescent visualization of fucosylated cells by flow cytometry of cells treated with 6-azidofucose labeled with click-activated fluorogenic probe or biotinylated alkyne is disclosed. Visualization of intracellular location of fucosylated glycoconjugates by fluorescence microscopy are disclosed.

    摘要翻译: 提供了通过含有包含炔基的探针的Cu(I)催化的[3 + 2]环加成的荧光标记来标记携带叠氮基的细胞聚糖的方法。 通过Cu(I)催化的[3 + 2]环加成的探针的炔基与叠氮改性的糖,从非荧光前体4-乙炔基-N-乙基-1,8-萘二甲酰亚胺生成荧光探针是 提供。 公开了通过岩藻糖补救途径将叠氮基岩藻糖类似物掺入糖缀合物。 公开了通过用用点击激活的荧光探针或生物素化的炔标记的6-叠氮基聚糖处理的细胞的流式细胞术的岩藻糖基化细胞的荧光可视化。 公开了通过荧光显微镜观察岩藻糖基化糖缀合物的细胞内位置。

    Alkynyl sugar analogs for the labeling and visualization of glycoconjugates in cells
    10.
    发明授权
    Alkynyl sugar analogs for the labeling and visualization of glycoconjugates in cells 有权
    炔基糖类似物用于细胞中糖缀合物的标记和可视化

    公开(公告)号:US07960139B2

    公开(公告)日:2011-06-14

    申请号:US12079226

    申请日:2008-03-24

    IPC分类号: G01N33/53

    摘要: The present disclosure relates to a method for metabolic oligosaccharide engineering that incorporates derivatized alkyne-bearing sugar analogs as “tags” into cellular glycoconjugates. The disclosed method incorporates alkynyl derivatized Fuc and alkynyl derivatized ManNAc sugars into a cellular glycoconjugate. A chemical probe comprising an azide group and a visual probe or a fluorogenic probe is used to label the alkyne-derivatized sugar-tagged glycoconjugate. In one aspect, the chemical probe binds covalently to the alkynyl group by Cu(I)-catalyzed [3+2] azide-alkyne cycloaddition and is visualized at the cell surface, intracellularly, or in a cellular extract. The labeled glycoconjugate is capable of detection by flow cytometry, SDS-PAGE, Western blot, ELISA or confocal microscopy, and mass spectrometry.

    摘要翻译: 本公开内容涉及将衍生的含炔烃类似物作为“标签”掺入细胞糖缀合物的代谢寡糖工程方法。 所公开的方法将炔基衍生化的Fuc和炔基衍生的ManNAc糖引入细胞糖缀合物中。 使用包含叠氮化物基团和视觉探针或荧光探针的化学探针来标记炔衍生的糖标记的糖缀合物。 在一个方面,化学探针通过Cu(I)催化的[3 + 2]叠氮炔环加成共价结合到炔基上,并且在细胞表面,细胞内或细胞提取物中可视化。 标记的糖缀合物能够通过流式细胞术,SDS-PAGE,Western印迹,ELISA或共聚焦显微镜和质谱检测。