Glucagon/GLP-1 receptor co-agonists
    2.
    发明授权
    Glucagon/GLP-1 receptor co-agonists 有权
    胰高血糖素/ GLP-1受体共激动剂

    公开(公告)号:US08969294B2

    公开(公告)日:2015-03-03

    申请号:US13567858

    申请日:2012-08-06

    CPC分类号: C07K14/605

    摘要: Modified glucagon peptides are disclosed having enhanced potency at the glucagon receptor relative to native glucagon. Further modification of the glucagon peptides by forming intramolecular bridges or the substitution of the terminal carboxylic acid with an amide group produces peptides exhibiting glucagon/GLP-1 receptor co-agonist activity. The solubility and stability of these high potency glucagon analogs can be further improved by modification of the polypeptides by pegylation, acylation, alkylation, substitution of carboxy terminal amino acids, C-terminal truncation, or the addition of a carboxy terminal peptide selected from the group consisting of SEQ ID NO: 26 (GPSSGAPPPS), SEQ ID NO: 27 (KRNRNNIA) and SEQ ID NO: 28 (KRNR).

    摘要翻译: 公开了相对于天然胰高血糖素在胰高血糖素受体上具有增强的效力的改良的胰高血糖素肽。 通过形成分子内桥或通过酰胺基取代末端羧酸对胰高血糖素肽进一步修饰产生显示胰高血糖素/ GLP-1受体共激动剂活性的肽。 通过聚乙二醇化,酰化,烷基化,羧基末端氨基酸的取代,C-末端截短或加入选自下组的羧基末端肽,可以进一步改善这些高效胰高血糖素类似物的溶解度和稳定性 由SEQ ID NO:26(GPSSGAPPPS),SEQ ID NO:27(KRNRNNIA)和SEQ ID NO:28(KRNR)组成。

    GLUCAGON/GLP-1 RECEPTOR CO-AGONISTS
    8.
    发明申请
    GLUCAGON/GLP-1 RECEPTOR CO-AGONISTS 有权
    GLUCAGON / GLP-1受体协同作用

    公开(公告)号:US20130090286A1

    公开(公告)日:2013-04-11

    申请号:US13567858

    申请日:2012-08-06

    IPC分类号: C07K14/605

    CPC分类号: C07K14/605

    摘要: Modified glucagon peptides are disclosed having enhanced potency at the glucagon receptor relative to native glucagon. Further modification of the glucagon peptides by forming intramolecular bridges or the substitution of the terminal carboxylic acid with an amide group produces peptides exhibiting glucagon/GLP-1 receptor co-agonist activity. The solubility and stability of these high potency glucagon analogs can be further improved by modification of the polypeptides by pegylation, acylation, alkylation, substitution of carboxy terminal amino acids, C-terminal truncation, or the addition of a carboxy terminal peptide selected from the group consisting of SEQ ID NO: 26 (GPSSGAPPPS), SEQ ID NO: 27 (KRNRNNIA) and SEQ ID NO: 28 (KRNR).

    摘要翻译: 公开了相对于天然胰高血糖素在胰高血糖素受体上具有增强的效力的改良的胰高血糖素肽。 通过形成分子内桥或通过酰胺基取代末端羧酸对胰高血糖素肽进一步修饰产生显示胰高血糖素/ GLP-1受体共激动剂活性的肽。 通过聚乙二醇化,酰化,烷基化,羧基末端氨基酸的取代,C-末端截短或加入选自下组的羧基末端肽,可以进一步改善这些高效胰高血糖素类似物的溶解度和稳定性 由SEQ ID NO:26(GPSSGAPPPS),SEQ ID NO:27(KRNRNNIA)和SEQ ID NO:28(KRNR)组成。