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    Bifunctional glycoproteins having a modified carbohydrate complement and their use in tumor-selective therapy
    1.
    发明授权
    Bifunctional glycoproteins having a modified carbohydrate complement and their use in tumor-selective therapy 失效
    具有修饰的碳水化合物补体的双功能糖蛋白及其在肿瘤选择性治疗中的用途

    公开(公告)号：US08552159B2

    公开(公告)日：2013-10-08

    申请号：US10815925

    申请日：2004-04-02

    申请人： Klaus Bosslet ,  Joerg Czech ,  Dieter Hoffmann

    发明人： Klaus Bosslet ,  Joerg Czech ,  Dieter Hoffmann

    IPC分类号： C07K1/00

    CPC分类号： C12N9/0002 ,  A61K38/00 ,  A61K47/62 ,  A61K47/6851 ,  A61K2039/505 ,  C07K16/30 ,  C07K16/3007 ,  C07K16/3046 ,  C07K19/00 ,  C07K2317/24 ,  C07K2317/622 ,  C07K2319/00 ,  C07K2319/02 ,  C07K2319/61

    摘要： Provided herein are carbohydrate complement-modified bifunctional glycoproteins, and their use in tumor-selective therapy. The bifunctional glycoproteins comprise a first component that specifically binds to a tumor-specific antigen and a second component having enzymatic activity by means of which a non-toxic prodrug is cleaved into a cytotoxic drug. The carbohydrate complement comprises at least one exposed carbohydrate residue selected from the group consisting of mannose, galactose, N-acetylglucosamine, N-acetyllactose, glucose and fucose. The modified carbohydrate complement contributes to increased relative concentration of the glycoproteins at the site of the tumor, and enhanced clearance from the general circulation and non-tumor sites.

    摘要翻译： 本文提供了碳水化合物补体修饰的双功能糖蛋白，以及它们在肿瘤选择性治疗中的用途。 双功能糖蛋白包含特异性结合肿瘤特异性抗原的第一组分和具有酶活性的第二组分，通过其将非毒性前体药物切割成细胞毒性药物。 碳水化合物补体包含至少一种选自甘露糖，半乳糖，N-乙酰葡糖胺，N-乙酰乳糖，葡萄糖和岩藻糖的暴露的碳水化合物残基。 修饰的碳水化合物补体有助于增加肿瘤位置处的糖蛋白的相对浓度，并且增强了与一般循环和非肿瘤部位的清除率。