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    PROCESS FOR THE MODIFICATION OF A GLYCOPROTEIN USING A GLYCOSYLTRANSFERASE THAT IS OR IS DERIVED FROM A (1,4)-N-ACETYLGALACTOSAMINYLTRANSFERASE
    82.
    发明公开
    PROCESS FOR THE MODIFICATION OF A GLYCOPROTEIN USING A GLYCOSYLTRANSFERASE THAT IS OR IS DERIVED FROM A (1,4)-N-ACETYLGALACTOSAMINYLTRANSFERASE 有权
    METHODS FOR MODIFICATION FROM A A-（1,4）-N- acetylgalactosaminyl转移酶糖基转移酶衍生的糖蛋白的一种手段

    公开(公告)号：EP3134520A1

    公开(公告)日：2017-03-01

    申请号：EP16722547.3

    申请日：2016-04-25

    申请人： SynAffix B.V.

    发明人： VAN BERKEL, Sander Sebastiaan ,  VAN GEEL, Remon ,  WIJDEVEN, Maria Antonia ,  VAN DELFT, Floris Louis

    IPC分类号： C12N9/10

    CPC分类号： C12P21/005 ,  A61K47/6803 ,  A61K47/6849 ,  C07K16/2878 ,  C07K16/32 ,  C07K2317/14 ,  C07K2317/41 ,  C12N9/1051 ,  C12Y204/01038 ,  C12Y204/01092

    摘要： The present invention relates to a process for the enzymatic modification of a glycoprotein. The process comprises the step of contacting a glycoprotein comprising a glycan comprising a terminal GlcNAc-moiety, in the presence of glycosyltransferasethat is,or is derived from,a β-(1,4)-N-acetylgalactosaminyltransferase, with anon-natural sugar-derivative nucleotide. Thenon-natural sugar-derivative nucleotide is according to formula (3): wherein A is selected from the group consisting of -N3, -C(O)R3, -(CH2)iC≡C-R4, - SH, -SC(O)R8, -SC(0)OR8, -SC(S)OR8, -F, -CI, -Br -I, -OS(O)2R5, terminal C2 - C24 alkenyl groups, C3 - C5 cycloalkenyl groups, C4 - C8 alkadienyl groups, terminal C3 - C24 allenyl groups and amino groups. The invention further relates to a glycoprotein obtainable by the process according to the invention, to a bioconjugate that can be obtained by conjugating the glycoprotein with a linker-conjugate, and to β-(1,4)-Ν- acetylgalactosaminyltransferases that can be used in preparing the the glycoprotein according to the invention.

    摘要翻译： 本发明涉及一种用于糖蛋白的酶修饰的方法。 该方法包括使一种糖蛋白，其包括含有聚糖一个末端GlcNAc部分，在glycosyltransferasethat是存在的步骤中，或者由一个β-（1,4）-N- acetylgalactosaminyltransferase衍生，具有匿名天然糖 衍生物的核苷酸。 扩散核武器天然糖衍生物核苷酸gemäß到式（3）：worin A被选自-N 3，C（O）R 3，所选择的 - （CH2）iC≡C-R4， - SH，-S（ O）R8，-SC（O）OR 8，-S-C（S）OR 8，-F，-Cl，-Br，-I，-OS（O）2 R 5，端子C2 - C24烯基，C3 - C5环烯基，C4 - C8链二烯基，端C3 - C24丙二烯基和氨基。 本发明进一步涉及由该方法gemäß本发明的糖蛋白可获得的，涉及一种生物共轭也可以通过用左缀合物缀合糖蛋白来获得，并以β-（1,4）-Ν-乙酰氨基半乳糖也可以使用 在制备糖蛋白gemäß于本发明。

    CONJUGATED COMPOUNDS COMPRISING CYSTEINE-ENGINEERED ANTIBODIES
    85.
    发明公开
    CONJUGATED COMPOUNDS COMPRISING CYSTEINE-ENGINEERED ANTIBODIES 审中-公开
    康乃馨VERBINDUNGEN MIT CYSTEIN-MANIPULIERTENANTIKÖRPERN

    公开(公告)号：EP3129406A1

    公开(公告)日：2017-02-15

    申请号：EP15777039.7

    申请日：2015-04-10

    申请人： Medimmune, LLC

    发明人： GAO, Changshou ,  RAINEY, Godfrey ,  GAO, Cuihua

    IPC分类号： C07K16/30

    CPC分类号： A61K47/68 ,  A61K47/6803 ,  A61K47/6811 ,  A61K47/6817 ,  A61K47/6889 ,  C07K16/00 ,  C07K16/30 ,  C07K2317/40 ,  C07K2317/52 ,  C07K2317/524 ,  C07K2317/526 ,  C07K2317/71 ,  C07K2317/73 ,  C07K2317/92 ,  C07K2317/94 ,  C07K2319/30

    摘要： This disclosure provides conjugate compounds comprising antibodies and fragments thereof engineered with one or more reactive cysteine residues and more specifically to conjugate compounds with therapeutic or diagnostic applications. The conjugate compounds comprise cysteine-engineered antibodies or fragments thereof conjugated, for example, with chemotherapeutic drugs, toxins, and detection labels such as radionuclides or fluorophores. The disclosure also provides methods of using the disclosed conjugate compounds for in vitro, in situ, ex vivo, and in vivo diagnosis or treatment of mammalian cells, or associated pathological conditions.

    摘要翻译： 本公开提供了缀合物化合物，其包含用一种或多种反应性半胱氨酸残基改造的抗体及其片段，更具体地涉及具有治疗或诊断应用的缀合物。 缀合物化合物包含与化疗药物，毒素和检测标记例如放射性核素或荧光团缀合的半胱氨酸改造的抗体或其片段。 本公开还提供了使用所公开的缀合化合物用于体外，原位，离体和体内诊断或治疗哺乳动物细胞或相关病理状况的方法。

    SITE-SPECIFIC ANTIBODY-DRUG GLYCOCONJUGATES AND METHODS
    86.
    发明公开
    SITE-SPECIFIC ANTIBODY-DRUG GLYCOCONJUGATES AND METHODS 审中-公开
    VERFAHREN ORTSSPEZIFISCHEANTIKÖRPER-WIRKSTOFF-GLYKOKONJUGATE

    公开(公告)号：EP3129402A1

    公开(公告)日：2017-02-15

    申请号：EP15776105.7

    申请日：2015-04-08

    申请人： University Of Georgia Research Foundation, Inc.

    发明人： BOONS, Geert-Jan

    IPC分类号： C07K16/00

    CPC分类号： A61K31/4188 ,  A61K47/6803 ,  A61K47/6809 ,  A61K47/6849 ,  A61K49/0043 ,  A61K49/0058 ,  C07K16/00 ,  C07K16/2803 ,  C07K2317/41 ,  C07K2317/92

    摘要： Compounds, compositions, and methods are provided for covalently linking an antibody or an antibody fragment to a cargo molecule, such as a therapeutic or a diagnostic agent, using a combination of enzymatic glycan remodeling and click chemistry. The method allows a cargo molecule to be selectively and efficiently attached post-translationally to an antibody or an antibody fragment. Also provided are antibody drug conjugates, methods of making, and uses thereof.

    摘要翻译： 提供化合物，组合物和方法，使用酶促聚糖重组和点击化学的组合将抗体或抗体片段与货物分子（例如治疗剂或诊断剂）共价连接。 该方法允许货物分子在翻译后选择性和有效地附着于抗体或抗体片段。 还提供了抗体药物共轭物，其制备方法和用途。