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    Shiga toxin B-subunit as a vector for tumor diagnosis and drug delivery to Gb3 expressing tumors
    2.
    发明申请
    Shiga toxin B-subunit as a vector for tumor diagnosis and drug delivery to Gb3 expressing tumors 有权
    志贺毒素B亚基作为肿瘤诊断和药物递送至Gb3表达肿瘤的载体

    公开(公告)号：US20060008475A1

    公开(公告)日：2006-01-12

    申请号：US11046786

    申请日：2005-02-01

    申请人： Ludger Johannes ,  David Grierson ,  Sylvie Robine ,  Jean-Claude Florent ,  Philipe Maillard ,  Jacky Roger

    发明人： Ludger Johannes ,  David Grierson ,  Sylvie Robine ,  Jean-Claude Florent ,  Philipe Maillard ,  Jacky Roger

    IPC分类号： A61K39/095

    CPC分类号： A61K49/085 ,  A61K38/00 ,  A61K41/0071 ,  A61K47/6415 ,  A61K47/67 ,  A61K49/0008 ,  A61K49/14 ,  B82Y5/00 ,  C07K14/25 ,  C07K14/36

    摘要： The invention relates to new compounds for cancer therapy or diagnosis and to the use of a non-toxic B subunit of Shiga toxin mutant as a vector for diagnostic products or drugs in over-expressing Gb3 receptor cells, such compounds having the following formula: STxB-Z(n)-Cys-Y(m)-T wherein—STxB is the Shiga Toxin B subunit or a functional equivalent thereof, —Z(n) wherein n is 0 or 1, Z is an amino-acid residue devoid of sulfydryl groups, or is a polypeptide, —T is a molecule linked by a covalent bound to the S part of Cys, selected from: agents for in vivo diagnosis, cytotoxic agents, prodrugs, or enzymes for the conversion of a prodrug to a drug, —Y(m) wherein m is 0 or 1, Y is a linker between T and Cys, which is either cleavable or not cleavable for the release of T after the internalization of the hybrid compound into cells.

    摘要翻译： 本发明涉及用于癌症治疗或诊断的新化合物，以及使用志贺毒素突变体的无毒性B亚基作为过表达Gb3受体细胞的诊断产品或药物的载体，具有下式：STxB -Z（n）-Cys-Y（m）-T其中-STxB是志贺毒素B亚基或其功能等同物，-Z（n）其中n为0或1，Z为不含 或者是多肽，-T是通过与Sys的S部分的共价结合连接的分子，其选自：用于体内诊断的试剂，细胞毒性剂，前药或用于将前药转化为药物的酶 -Y（m）其中m是0或1，Y是T和Cys之间的连接体，其在将杂化化合物内化为细胞后可以切割或不可切割以释放T。

    Shiga toxin B-subunit as a vector for tumor diagnosis and drug delivery to GB3 expressing tumors
    3.
    发明授权
    Shiga toxin B-subunit as a vector for tumor diagnosis and drug delivery to GB3 expressing tumors 有权
    志贺毒素B亚基作为肿瘤诊断和药物递送到GB3表达肿瘤的载体

    公开(公告)号：US07981400B2

    公开(公告)日：2011-07-19

    申请号：US12723361

    申请日：2010-03-12

    申请人： Ludger Johannes ,  David Grierson ,  Sylvie Robine ,  Jean-Claude Florent ,  Philipe Maillard ,  Jacky Roger

    发明人： Ludger Johannes ,  David Grierson ,  Sylvie Robine ,  Jean-Claude Florent ,  Philipe Maillard ,  Jacky Roger

    IPC分类号： A61K49/00 ,  C07K14/00

    CPC分类号： A61K49/085 ,  A61K38/00 ,  A61K41/0071 ,  A61K47/6415 ,  A61K47/67 ,  A61K49/0008 ,  A61K49/14 ,  B82Y5/00 ,  C07K14/25 ,  C07K14/36

    摘要： The invention relates to new compounds for cancer therapy or diagnosis and more specifically to the use of a non-toxic B subunit of Shiga toxin mutant as a vector for diagnostic products or drugs in over-expressing Gb3 receptor cells, such compounds having the following formula: STxB-Z(n)-Cys-Y(m)-T wherein STxB is the Shiga Toxin B subunit or a functional equivalent thereof, Z(n) wherein n is 0 or 1 and when n is 1, Z is an amino-acid residue devoid of sulfhydryl group, or is a polypeptide, Cys is the amino-acid residue for Cysteine, T is a molecule linked by a covalent bound to the S part of Cys, selected in a group comprising: agents for in vivo diagnosis, cytotoxic agents, prodrugs, or enzymes for the conversion of a prodrug to a drug, Y(m) wherein m is 0 or 1 and when m is 1, Y is a linker between T and Cys, said linker being either cleavable or not cleavable for the release of T after the internalization of the hybrid compound into said cells.

    摘要翻译： 本发明涉及用于癌症治疗或诊断的新化合物，更具体地涉及使用志贺毒素突变体的无毒性B亚基作为过表达Gb3受体细胞的诊断产物或药物的载体，具有下式 ：STxB-Z（n）-Cys-Y（m）-T其中STxB是滋贺毒素B亚基或其功能等同物，Z（n）其中n为0或1，当n为1时，Z为氨基 - 没有巯基的酸性残基，或是多肽，Cys是半胱氨酸的氨基酸残基，T是通过共价结合到Cys的S部分的分子连接的分子，所述组分选自：用于体内诊断的试剂 ，前药或前药转化为药物的Y（m），其中m为0或1，当m为1时，Y为T和Cys之间的接头，所述接头可切割或不切割 在将杂化化合物内化至所述细胞后，可以切割T释放T。

    Shiga toxin B-subunit as a vector for tumor diagnosis and drug delivery to GB3 expressing tumors
    4.
    发明授权
    Shiga toxin B-subunit as a vector for tumor diagnosis and drug delivery to GB3 expressing tumors 有权
    志贺毒素B亚基作为肿瘤诊断和药物递送到GB3表达肿瘤的载体

    公开(公告)号：US08313731B2

    公开(公告)日：2012-11-20

    申请号：US13159124

    申请日：2011-06-13

    申请人： Ludger Johannes ,  David Grierson ,  Sylvie Robine ,  Jean-Claude Florent ,  Philipe Maillard ,  Jacky Roger

    发明人： Ludger Johannes ,  David Grierson ,  Sylvie Robine ,  Jean-Claude Florent ,  Philipe Maillard ,  Jacky Roger

    IPC分类号： A61K49/00 ,  C07K14/00

    CPC分类号： A61K49/085 ,  A61K38/00 ,  A61K41/0071 ,  A61K47/6415 ,  A61K47/67 ,  A61K49/0008 ,  A61K49/14 ,  B82Y5/00 ,  C07K14/25 ,  C07K14/36

    摘要： The invention relates to new compounds for cancer therapy or diagnosis and more specifically to the use of a non-toxic B subunit of Shiga toxin mutant as a vector for diagnostic products or drugs in over-expressing Gb3 receptor cells, such compounds having the following formula: STxB-Z(n)-Cys-Y(m)-T wherein STxB is the Shiga Toxin B subunit or a functional equivalent thereof, Z(n) wherein n is 0 or 1 and when n is 1, Z is an amino-acid residue devoid of sulfydryl group, or is a polypeptide, Cys is the amino-acid residue for Cysteine, T is a molecule linked by a covalent bound to the S part of Cys, selected in a group comprising: agents for in vivo diagnosis, cytotoxic agents, prodrugs, or enzymes for the conversion of a prodrug to a drug, Y(m) wherein m is 0 or 1 and when m is 1, Y is a linker between T and Cys, said linker being either cleavable or not cleavable for the release of T after the internalization of the hybrid compound into said cells.

    摘要翻译： 本发明涉及用于癌症治疗或诊断的新化合物，更具体地涉及使用志贺毒素突变体的无毒性B亚基作为过表达Gb3受体细胞的诊断产物或药物的载体，具有下式 ：STxB-Z（n）-Cys-Y（m）-T其中STxB是滋贺毒素B亚基或其功能等同物，Z（n）其中n为0或1，当n为1时，Z为氨基 - 不含巯基的酸性残基，或是多肽，Cys是半胱氨酸的氨基酸残基，T是通过与Sys的S部分共价结合连接的分子，选自以下组中：包括用于体内诊断的试剂 ，前药或前药转化为药物的Y（m），其中m为0或1，当m为1时，Y为T和Cys之间的接头，所述接头可切割或不切割 在将杂化化合物内化至所述细胞后，可以切割T释放T。

    Shiga toxin B-subunit as a vector for tumor diagnosis and drug delivery to Gb3 expressing tumors
    5.
    发明授权
    Shiga toxin B-subunit as a vector for tumor diagnosis and drug delivery to Gb3 expressing tumors 有权
    志贺毒素B亚基作为肿瘤诊断和药物递送至Gb3表达肿瘤的载体

    公开(公告)号：US07718601B2

    公开(公告)日：2010-05-18

    申请号：US11046786

    申请日：2005-02-01

    申请人： Ludger Johannes ,  David Grierson ,  Sylvie Robine ,  Jean-Claude Florent ,  Philipe Maillard ,  Jacky Roger

    发明人： Ludger Johannes ,  David Grierson ,  Sylvie Robine ,  Jean-Claude Florent ,  Philipe Maillard ,  Jacky Roger

    IPC分类号： C07K14/00 ,  A61K38/00

    CPC分类号： A61K49/085 ,  A61K38/00 ,  A61K41/0071 ,  A61K47/6415 ,  A61K47/67 ,  A61K49/0008 ,  A61K49/14 ,  B82Y5/00 ,  C07K14/25 ,  C07K14/36

    摘要： The invention relates to new compounds for cancer therapy or diagnosis and to the use of a non-toxic B subunit of Shiga toxin mutant as a vector for diagnostic products or drugs in over-expressing Gb3 receptor cells, such compounds having the following formula: STxB-Z(n)-Cys-Y(m)-T wherein-STxB is the Shiga Toxin B subunit or a functional equivalent thereof, -Z(n) wherein n is 0 or 1, Z is an amino-acid residue devoid of sulfydryl groups, or is a polypeptide, -T is a molecule linked by a covalent bound to the S part of Cys, selected from: agents for in vivo diagnosis, cytotoxic agents, prodrugs, or enzymes for the conversion of a prodrug to a drug, - Y(m) wherein m is 0 or 1, Y is a linker between T and Cys, which is either cleavable or not cleavable for the release of T after the internalization of the hybrid compound into cells.

    摘要翻译： 本发明涉及用于癌症治疗或诊断的新化合物，以及使用志贺毒素突变体的无毒性B亚基作为过表达Gb3受体细胞的诊断产品或药物的载体，具有下式：STxB -Z（n）-Cys-Y（m）-T其中-STxB是志贺毒素B亚基或其功能等同物，-Z（n）其中n为0或1，Z为不含 或者是多肽，-T是通过与Sys的S部分的共价结合连接的分子，其选自：用于体内诊断的试剂，细胞毒性剂，前药或用于将前药转化成药物的酶 ， - Y（m）其中m是0或1，Y是T和Cys之间的连接体，在混合化合物内化到细胞中之后，它们是可切割的或不可裂解的用于释放T。