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    4(1H)-QUINOLONE DERIVATIVES AND USES THEREOF
    32.
    发明申请
    4(1H)-QUINOLONE DERIVATIVES AND USES THEREOF 审中-公开

    公开(公告)号：US20200330449A1

    公开(公告)日：2020-10-22

    申请号：US16831346

    申请日：2020-03-26

    Applicant: Academia Sinica

    Inventor： Rong-Jie CHEIN ,  Pan-Chyr YANG ,  Chi-Huey WONG ,  Ming-Shiu LIN ,  Ting-Jen CHENG ,  Ting-Hung CHOU

    IPC: A61K31/47 ,  C07D215/233 ,  A61K45/06 ,  A61P35/00

    Abstract: Compounds of Formula (I) and methods for treating, delaying, and/or preventing the adverse effects of proliferative diseases, such as cancers including, for example, lung cancer, breast cancer, ovarian cancer, prostate cancer, head cancer, neck cancer, head and neck cancer, or leukemia (e.g., cancer resistant to treatment by one or more microtubule-targeting agents, e.g., cancer resistant to multiple drugs associated with P-glycoprotein (P-gp) overexpression). Methods of inhibiting polymerization of a cancer cell microtubule in a subject in need thereof or a cell, tissue, or biological sample, binding p-tubulin, inhibiting microtubule assembly and, inducing apoptosis in a cancer cell resistant to multiple drugs in a tissue, biological sample, or subject. Pharmaceutical compositions, kits, and methods of using the compounds for treating any of the target diseases described herein.

    ALKYNYL SUGAR ANALOGS FOR LABELING AND VISUALIZATION OF GLYCOCONJUGATES IN CELLS
    33.
    发明申请
    ALKYNYL SUGAR ANALOGS FOR LABELING AND VISUALIZATION OF GLYCOCONJUGATES IN CELLS 审中-公开

    公开(公告)号：US20190269227A1

    公开(公告)日：2019-09-05

    申请号：US16415411

    申请日：2019-05-17

    Applicant: ACADEMIA SINICA

    Inventor： Chi-Huey WONG ,  Tsui-Ling HSU ,  Sarah R. HANSON ,  Masaaki SAWA

    IPC: A45F3/14 ,  A41F9/02 ,  A45F5/02 ,  A45F3/00 ,  A45F3/10

    Abstract: 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.

    METHODS FOR MODIFYING HUMAN ANTIBODIES BY GLYCAN ENGINEERING
    34.
    发明申请
    METHODS FOR MODIFYING HUMAN ANTIBODIES BY GLYCAN ENGINEERING 审中-公开

    公开(公告)号：US20190100573A1

    公开(公告)日：2019-04-04

    申请号：US16150190

    申请日：2018-10-02

    Applicant: Academia Sinica

    Inventor： Chi-Huey WONG ,  Chung-Yi WU

    IPC: C07K16/00 ,  C12P21/00

    Abstract: Modified Fc regions of antibodies and antibody fragments, both human and humanized, and having enhanced stability and efficacy, are provided. Fc regions with core fucose residues removed, and attached to oligosaccharides comprising terminal sialyl residues, are provided. Antibodies comprising homogeneous glycosylation of Fc regions with specific oligosaccharides are provided. Fc regions conjugated with homogeneous glycoforms of monosaccharides and trisaccharides, are provided. Methods of preparing human antibodies with modified Fc using glycan engineering, are provided.

    GLYCAN ARRAYS ON PTFE-LIKE ALUMINUM COATED GLASS SLIDES AND RELATED METHODS
    37.
    发明申请
    GLYCAN ARRAYS ON PTFE-LIKE ALUMINUM COATED GLASS SLIDES AND RELATED METHODS 审中-公开
    GLYCAN阵列在PTFE类铝合金玻璃滑块及相关方法上

    公开(公告)号：US20170038378A1

    公开(公告)日：2017-02-09

    申请号：US14182290

    申请日：2014-02-18

    Applicant: Academia Sinica

    Inventor： Chi-Huey WONG ,  Chung-Yi WU ,  Susan Y. TSENG

    IPC: G01N33/553 ,  G01N33/58

    CPC classification number: G01N33/553 ,  C40B40/12 ,  C40B50/14 ,  G01N33/582 ,  G01N2333/942 ,  G01N2400/10 ,  H01J49/40

    Abstract: Aluminum coated glass slides provide a novel glycan array platform. Specifically, aluminum coated glass slides increase sensitivity of fluorescent based assay methods. Additionally, aluminum coated glass slides allows for mass spectroscopic analysis of carbohydrates and provide a platform for examining activity of cellulases. The unique properties of ACG slides include: 1) the metal oxide layer on the surface can be activated for grafting organic compounds such as modified oligosaccharides; 2) the surface remains electrically conductive, and the grafted oligosaccharides can be simultaneously characterized by mass spectrometry and carbohydrate-binding assay; and 3) the slides are more sensitive than transparent glass slides in binding analysis.

    Abstract translation: 镀铝玻璃片提供了一种新的聚糖阵列平台。 具体来说，铝涂层玻璃片增加了基于荧光的测定方法的灵敏度。 另外，铝涂层玻璃载玻片允许碳水化合物的质谱分析，并提供一个检查纤维素酶活性的平台。 ACG载玻片的独特性质包括：1）表面上的金属氧化物层可以活化，用于接枝有机化合物如改性寡糖; 2）表面保持导电，并且接枝的寡糖可以通过质谱法和碳水化合物结合测定同时表征; 和3）在结合分析中，载玻片比透明玻片更敏感。

    HUMAN iNKT CELL ACTIVATION USING GLYCOLIPIDS WITH ALTERED GLYCOSYL GROUPS
    40.
    发明申请
    HUMAN iNKT CELL ACTIVATION USING GLYCOLIPIDS WITH ALTERED GLYCOSYL GROUPS 有权
    使用具有改变的糖苷类的甘氨酸的人体神经细胞激活

    公开(公告)号：US20150071960A1

    公开(公告)日：2015-03-12

    申请号：US14480521

    申请日：2014-09-08

    Applicant: Academia Sinica

    Inventor： Chi-Huey WONG ,  Alice L. Yu ,  Kun-Hsien Lin ,  Tai-Na Chen

    IPC: A61K39/39 ,  C07H15/18

    CPC classification number: A61K39/39 ,  A61K2039/55511 ,  A61K2039/57 ,  C07H15/18

    Abstract: Glycosphingolipids (GSLs) bearing α-glucose (α-Glc) that preferentially stimulate human invariant NKT (iNKT) cells are provided. GSLs with α-glucose (α-Glc) that exhibit stronger induction in humans (but weaker in mice) of cytokines and chemokines and expansion and/or activation of immune cells than those with α-galactose (α-Gal) are disclosed. GSLs bearing α-glucose (α-Glc) and derivatives of α-Glc with F at the 4 and/or 6 positions are provided. Methods for iNKT-independent induction of chemokines by the GSL with α-Glc and derivatives thereof are disclosed. Methods for immune stimulation in humans using GSLs with α-Glc and derivatives thereof are provided.

    Abstract translation: 提供了优先刺激人类不变NKT（iNKT）细胞的含有α-葡萄糖（α-Glc）的糖鞘糖脂（GSLs）。 公开了具有α-葡萄糖（α-Glc）的GSL，其具有比具有α-半乳糖（α-Gal）的细胞因子和趋化因子更强的诱导（但是在小鼠中较弱）和免疫细胞的膨胀和/或活化。 提供了带有α-葡萄糖（α-Glc）的GSL和α-Glc的衍生物，其中F在4和/或6位。 公开了通过具有α-Glc的GSL和其衍生物对iNKT独立诱导趋化因子的方法。 提供了使用具有α-Glc的GSL及其衍生物在人体中免疫刺激的方法。

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