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    Shiga toxin B-subunit as a vector for tumor diagnosis and drug delivery to Gb3 expressing tumors
    4.
    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。