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    Cysteine Engineered Antibodies and Conjugates
    14.
    发明申请
    Cysteine Engineered Antibodies and Conjugates 审中-公开

    公开(公告)号：US20200339664A1

    公开(公告)日：2020-10-29

    申请号：US16787280

    申请日：2020-02-11

    Applicant: Genentech, Inc.

    Inventor： Sunil Bhakta ,  Jagath R. Junutula

    IPC: C07K16/00 ,  A61K51/10 ,  A61K47/68 ,  C07K16/30 ,  C07K16/32

    Abstract: Cysteine engineered antibodies comprising a free cysteine amino acid in the heavy chain or light chain are prepared by mutagenizing a nucleic acid sequence of a parent antibody and replacing one or more amino acid residues by cysteine to encode the cysteine engineered antibody; expressing the cysteine engineered antibody; and isolating the cysteine engineered antibody. Certain highly reactive cysteine engineered antibodies were identified by the PHESELECTOR assay. Isolated cysteine engineered antibodies may be covalently attached to a capture label, a detection label, a drug moiety, or a solid support.

    Cysteine engineered anti-MUC16 antibodies and antibody drug conjugates
    15.
    再颁专利
    Cysteine engineered anti-MUC16 antibodies and antibody drug conjugates 有权

    公开(公告)号：USRE47194E1

    公开(公告)日：2019-01-08

    申请号：US14680457

    申请日：2015-04-07

    Applicant: Genentech, Inc.

    Inventor： Jagath R. Junutula ,  William Mallet

    IPC: C07K16/00 ,  C12P21/08 ,  C07K16/28 ,  A61K47/68 ,  A61K51/10 ,  A61K39/00

    Abstract: Cysteine engineered anti-MUC16 antibodies are engineered by replacing one or more amino acids of a parent anti-MUC16 antibody with non cross-linked, reactive cysteine amino acids. Methods of design, preparation, screening, and selection of the cysteine engineered anti-MUC16 antibodies are provided. Cysteine engineered anti-MUC16 antibodies (Ab) are conjugated with one or more drug moieties (D) through a linker (L) to form cysteine engineered anti-MUC16 antibody-drug conjugates having Formula I: Ab-(L-D)p   I where p is 1 to 4. Diagnostic and therapeutic uses for cysteine engineered antibody drug compounds and compositions are disclosed.

    ZIRCONIUM-RADIOLABELED, CYSTEINE ENGINEERED ANTIBODY CONJUGATES
    17.
    发明申请
    ZIRCONIUM-RADIOLABELED, CYSTEINE ENGINEERED ANTIBODY CONJUGATES 审中-公开
    青霉素 - 放射性标记物，CYSTEINE工程抗体结合蛋白

    公开(公告)号：US20150017094A1

    公开(公告)日：2015-01-15

    申请号：US14300630

    申请日：2014-06-10

    Applicant: Genentech, Inc.

    Inventor： Herman Gill ,  Jagath R. Junutula ,  Henry B. Lowman ,  Jan Marik ,  Jeff Tinianow ,  Simon Williams

    IPC: A61K51/10

    CPC classification number: A61K51/1093 ,  A01K2267/0331 ,  A61K51/1027 ,  A61K51/1051 ,  C07C259/06 ,  C07C323/60 ,  C07C2601/14 ,  C07K16/00 ,  C07K16/32 ,  C07K2317/21 ,  C07K2317/51 ,  C07K2317/52 ,  C07K2317/55 ,  C07K2317/624

    Abstract: Antibodies are engineered by replacing one or more amino acids of a parent antibody with non cross-linked, highly reactive cysteine amino acids. Antibody fragments may also be engineered with one or more cysteine amino acids to form cysteine engineered antibody fragments (ThioFab). Methods of design, preparation, screening, and selection of the cysteine engineered antibodies are provided. Cysteine engineered antibodies (Ab) are conjugated with one or more zirconium complex (Z) labels through a linker (L) to form cysteine engineered zirconium-labeled antibody conjugates having Formula I: Ab-(L-Z)p  I where p is 1 to 4. Imaging methods and diagnostic uses for zirconium-radiolabeled, cysteine engineered antibody conjugate compositions are disclosed.

    Abstract translation: 通过用非交联的高反应性半胱氨酸氨基酸替代亲本抗体的一个或多个氨基酸来设计抗体。 抗体片段也可以用一个或多个半胱氨酸氨基酸进行工程化以形成半胱氨酸改造的抗体片段（ThioFab）。 提供了设计，制备，筛选和选择半胱氨酸改造的抗体的方法。 半胱氨酸改造的抗体（Ab）通过接头（L）与一个或多个锆络合物（Z）标记物缀合以形成具有式I：Ab-（LZ）p I的半胱氨酸改造的锆标记的抗体缀合物，其中p为1至4 公开了用于放射性标记的半胱氨酸改造的抗体缀合物组合物的成像方法和诊断用途。

    CYSTEINE ENGINEERED ANTIBODIES AND CONJUGATES
    18.
    发明申请
    CYSTEINE ENGINEERED ANTIBODIES AND CONJUGATES 审中-公开
    CYSTEINE工程抗体和结合物

    公开(公告)号：US20140288280A1

    公开(公告)日：2014-09-25

    申请号：US14185080

    申请日：2014-02-20

    Applicant: Genentech, Inc.

    Inventor： Sunil Bhakta ,  Jagath R. Junutula

    IPC: A61K47/48

    CPC classification number: C07K16/00 ,  A61K47/6801 ,  A61K47/6803 ,  A61K47/6811 ,  A61K47/6817 ,  A61K47/6829 ,  A61K47/6851 ,  A61K47/6855 ,  A61K47/6889 ,  A61K51/1051 ,  C07K16/3092 ,  C07K16/32 ,  C07K2317/52 ,  C07K2317/55 ,  C07K2319/31

    Abstract: Cysteine engineered antibodies comprising a free cysteine amino acid in the heavy chain or light chain are prepared by mutagenizing a nucleic acid sequence of a parent antibody and replacing one or more amino acid residues by cysteine to encode the cysteine engineered antibody; expressing the cysteine engineered antibody; and isolating the cysteine engineered antibody. Certain highly reactive cysteine engineered antibodies were identified by the PHESELECTOR assay. Isolated cysteine engineered antibodies may be covalently attached to a capture label, a detection label, a drug moiety, or a solid support.

    Abstract translation: 在重链或轻链中包含游离半胱氨酸氨基酸的半胱氨酸改造的抗体是通过诱变亲本抗体的核酸序列并用半胱氨酸代替一个或多个氨基酸残基来编码半胱氨酸改造的抗体来制备的; 表达半胱氨酸改造的抗体; 并分离半胱氨酸改造的抗体。 通过PHESELECTOR测定鉴定某些高反应性半胱氨酸工程化抗体。 分离的半胱氨酸改造的抗体可以共价连接到捕获标记，检测标记，药物部分或固体支持物上。

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