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    Methods for modifying human antibodies by glycan engineering
    3.
    发明授权
    Methods for modifying human antibodies by glycan engineering 有权

    公开(公告)号：US11377485B2

    公开(公告)日：2022-07-05

    申请号：US16150164

    申请日：2018-10-02

    申请人： Academia Sinica

    发明人： Chi-Huey Wong ,  Chung-Yi Wu

    IPC分类号： C07K16/18 ,  C12P21/00 ,  C07K16/28

    摘要： Methods for making modified Fc regions of antibodies and antibody fragments, both human and humanized, and having enhanced stability and efficacy, are provided. Antibodies comprising 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.

    Methods for modular synthesis of N-glycans and arrays thereof
    5.
    发明授权
    Methods for modular synthesis of N-glycans and arrays thereof 有权

    公开(公告)号：US10336784B2

    公开(公告)日：2019-07-02

    申请号：US15453836

    申请日：2017-03-08

    申请人： Academia Sinica

    发明人： Chi-Huey Wong ,  Chung-Yi Wu ,  Sachin S. Shivatare

    IPC分类号： C07H5/06 ,  A61K31/702 ,  C12N9/10 ,  C07K16/10 ,  C12P19/04 ,  G01N33/50 ,  G01N33/532 ,  G01N33/68 ,  C08B37/00 ,  G01N33/569 ,  C12P19/28

    摘要： The present disclosure relates to novel modular methods for generating a diversity of N-glycans of high mannose, hybrid and complex types. The present disclosure also relates to exemplary arrays of the synthesized N-glycans spotted onto aluminium oxide coated slides. These arrays can be used to detect and analyze binding interactions between the synthesized N-glycans and glycan binding molecules, such as HIV-1 neutralizing antibodies. The present disclosure also relates to methods for identifying agents that bind to various types of molecules on the arrays and to defining the structural elements of the molecules on the arrays that bind to those agents. The arrays and methods provided herein may be used for general epitope identification, drug discovery and as analytical tools. The present disclosure also provides useful glycans and epitope determinants that are useful in detecting, diagnosing, recurrence monitoring and preventing pathological diseases such as HIV.

    Enhanced anti-influenza agents conjugated with anti-inflammatory activity
    8.
    发明授权
    Enhanced anti-influenza agents conjugated with anti-inflammatory activity 有权

    公开(公告)号：US10130714B2

    公开(公告)日：2018-11-20

    申请号：US13836356

    申请日：2013-03-15

    申请人： Academia Sinica

    发明人： Chi-Huey Wong ,  Jim-Min Fang ,  Kung-Cheng Liu ,  Jia-Tsrong Jan ,  Yih-Shyun E. Cheng ,  Ting-Jen R. Cheng

    IPC分类号： A61K31/351 ,  C07D309/28 ,  A61K47/55 ,  A61K47/48

    摘要： Novel dual-targeted, bifunctional anti-influenza drugs formed by conjugation with anti-inflammatory agents are disclosed. Exemplary drugs according to the invention include caffeic acid (CA)-bearing zanamivir (ZA) conjugates ZA-7-CA (1), ZA-7-CA-amide (7) and ZA-7-Nap (43) for simultaneous inhibition of influenza virus neuraminidase and suppression of proinflammatory cytokines. Synthetic methods for preparation of these enhanced anti-influenza conjugate drugs are provided. The synthetic bifunctional ZA conjugates act synergistically towards protection of mice lethally infected by H1N1 or H5N1 influenza viruses. The efficacy of ZA-7-CA, ZA-7-CA-amide and ZA-7-Nap conjugates is much greater than the combination therapy of ZA with anti-inflammatory agents.