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    • 1. 发明申请
    • Glucagon-like-peptide-2 (GLP-2) analogues
    • 胰高血糖素样肽-2(GLP-2)类似物
    • US20070117752A1
    • 2007-05-24
    • US11595496
    • 2006-11-09
    • Bjarne LarsenYvette Petersen
    • Bjarne LarsenYvette Petersen
    • A61K38/26
    • C07K14/605A61K9/0019A61K9/19A61K35/54A61K35/74A61K38/00A61K38/26A61K47/26A61K48/00C12N7/00C12N2710/10043C12N2710/20043C12N2710/22043C12N2760/20243
    • GLP-2 analogues are disclosed which comprise one of more substitutions as compared to [hGly2]GLP-2 and which improved biological activity in vivo and/or improved chemical stability, e.g., as assessed in in vitro stability assays. More particularly, preferred GLP-2 analogues disclosed herein comprise substitutions at one or more of positions 8, 16, 24 and/or 28 of the wild-type GLP-2 sequence, optionally in combination with further substitutions at position 2 (as mentioned in the introduction) and one or more of positions 3, 5, 7, 10 and 11, and/or a deletion of one or more of amino acids 31 to 33 and/or the addition of a N-terminal or C-terminal stabilizing peptide sequence. The analogues are particularly useful for the prophylaxis or treatment of stomach and bowel-related disorders and for ameliorating side effects of chemotherapy. Also disclosed are methods and kits for selecting a patient from populations suited for treatment with GLP-2 analogues.
    • 公开了GLP-2类似物,其包含与[hGly2] GLP-2相比更多的取代之一,并且其在体内的改善的生物活性和/或改善的化学稳定性,例如在体外稳定性测定中评估。 更具体地,本文公开的优选的GLP-2类似物包括在野生型GLP-2序列的8,16,24和/或28位的一个或多个位置上的取代,任选与第2位的进一步取代组合(如 引入)和位置3,5,7,10和11中的一个或多个,和/或缺失一个或多个氨基酸31至33和/或添加N-末端或C-末端稳定肽 序列。 类似物对于预防或治疗胃和肠相关疾病以及改善化学疗法的副作用特别有用。 还公开了用于从适合于用GLP-2类似物治疗的群体中选择患者的方法和试剂盒。