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    Shiga toxin B-subunit as a vector for tumor diagnosis and drug delivery to GB3 expressing tumors
    61.
    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
    62.
    发明申请
    SHIGA TOXIN B-SUBUNIT AS A VECTOR FOR TUMOR DIAGNOSIS AND DRUG DELIVERY TO GB3 EXPRESSING TUMORS 有权
    SHIGA TOXIN B-SUBUNIT作为肿瘤诊断和药物递送给GB3表达肿瘤的载体

    公开(公告)号：US20100329992A1

    公开(公告)日：2010-12-30

    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： A61K49/10 ,  A61K38/00 ,  A61K31/7048 ,  A61K38/47 ,  A61K38/48 ,  A61K49/22 ,  A61P35/00

    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。

    Use of lytic toxins and toxin conjugates
    68.
    发明授权
    Use of lytic toxins and toxin conjugates 失效

    公开(公告)号：US07422740B1

    公开(公告)日：2008-09-09

    申请号：US10129558

    申请日：2000-11-13

    申请人： Desmond Purdy ,  Susan Charlton ,  Ian Henderson

    发明人： Desmond Purdy ,  Susan Charlton ,  Ian Henderson

    IPC分类号： A61K39/395 ,  A61K39/00

    CPC分类号： B82Y5/00 ,  A61K47/6415 ,  A61K47/67 ,  A61K47/6829

    摘要： Agents are provided which are capable of inhibiting the cell division cycle in a target cell of interest. The agents comprise first and second components, wherein the first component is a targeting moiety which is capable of directing the second component to the target cell of interest. The second component is capable of inhibiting the cell division cycle in the target cell of interest. The agents are preferably provided in the form of conjugates, and the second component is preferably a cytolethal distending toxin. Methods for the preparation of the agents, and the use thereof for treating proliferative cell disorders and intracellular pathogens are also provided.

    Lectin-directed prodrug delivery system
    70.
    发明申请
    Lectin-directed prodrug delivery system 审中-公开
    凝集素导向的前药递送系统

    公开(公告)号：US20070253942A1

    公开(公告)日：2007-11-01

    申请号：US11785261

    申请日：2007-04-16

    申请人： Benjamin Davis

    发明人： Benjamin Davis

    IPC分类号： A61K38/46 ,  A61P43/00 ,  C12N9/14 ,  C12P19/00

    CPC分类号： B82Y5/00 ,  A61K47/54 ,  A61K47/543 ,  A61K47/549 ,  A61K47/67

    摘要： The invention provides a kit for lectin-directed prodrug delivery comprising a prodrug and a lectin-directed glycoconjugate, wherein the glycoconjugate is adapted to cleave the prodrug and thereby release the drug. The glycoconjugate generally comprises an enzyme conjugated to a carbohydrate moiety which binds to a lectin. The invention also provides novel glycoconjugates and novel methods of synthesizing prodrugs.

    摘要翻译： 本发明提供用于凝集素指导的前药递送的试剂盒，其包含前药和凝集素指导的糖缀合物，其中糖缀合物适于切割前药并由此释放药物。 糖缀合物通常包含与凝集素结合的碳水化合物部分缀合的酶。 本发明还提供新的糖缀合物和合成前药的新方法。