PEGYLATED TISSUE KALLIKREIN, AND PREPARATION METHOD THEREFOR AND USES THEREOF
    4.
    发明申请
    PEGYLATED TISSUE KALLIKREIN, AND PREPARATION METHOD THEREFOR AND USES THEREOF 审中-公开
    聚乙烯吡唑啉酮组合物及其制备方法及用途

    公开(公告)号:US20170049864A1

    公开(公告)日:2017-02-23

    申请号:US15109364

    申请日:2014-01-09

    IPC分类号: A61K38/48 C12N9/64 A61K47/48

    摘要: The present invention relates to polyethylene glycol (PEG) modified protein drugs, and a PEGylated tissue kallikrein, a preparation method and use thereof are disclosed. The tissue kallikrein has a sequence as shown in SEQ ID No. 1 or SEQ ID No. 2, and the tissue kallikrein may be natural or recombinant. The PEG has a molecular weight of 20 to 40 kDa, and is conjugated to the N-terminal primary amino of the tissue kallikrein. In addition to the advantages of significantly extended half-life, significantly reduced immunogenicity and stable and uniform structure, the biological activity of the PEGylated KLK1 provided in the present invention is improved to a higher extent, which is more significant in the treatment of cerebral apoplexy and diabetic nephropathy in particular.

    摘要翻译: 本发明涉及聚乙二醇(PEG)改性蛋白质药物和聚乙二醇化组织激肽释放酶,其制备方法和用途被公开。 组织激肽释放酶具有SEQ ID No.1或SEQ ID No.2所示的序列,组织激肽释放酶可以是天然的或重组的。 PEG具有20至40kDa的分子量,并且与组织激肽释放酶的N-末端的初级氨基缀合。 除了显着延长半衰期,免疫原性显着降低和结构稳定均匀的优点外,本发明提供的聚乙二醇化KLK1的生物活性也提高到更高程度,这在治疗脑中风中更为显着 特别是糖尿病肾病。