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    • 6. 发明申请
    • SELECTIVE GLUCAGON-LIKE-PEPTIDE-2 (GLP-2) ANALOGUES
    • 选择性GLUCAGON-LIKE-PEPTIDE-2(GLP-2)ANALOGUES
    • WO2008056155A1
    • 2008-05-15
    • PCT/GB2007/004273
    • 2007-11-08
    • ZEALAND PHARMA A/SLARSEN, Bjarne DuePETERSEN, Yvette Miata
    • LARSEN, Bjarne DuePETERSEN, Yvette Miata
    • C07K14/605A61K38/26
    • C07K14/605A61K38/26A61K45/06
    • GLP-2 analogues are disclosed which comprise one of more substitutions as compared to h[Gly2]GLP-2 and which may have the property of an increased small intestine/colon and stomach/colon selectivity. More particularly, preferred GLP-2 analogues disclosed herein comprise substitutions at one or more of positions (11, 16, 20, 24) and/or (28) of the wild-type GLP-2 sequence, optionally in combination with further substitutions at position (2) and one or more of positions (3, 5, 7), and (10), 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.
    • GLP-2类似物被公开,其包含与h [Gly2] GLP-2相比更多的取代,并且其可具有增加的小肠/结肠和胃/结肠选择性的性质。 更具体地,本文公开的优选的GLP-2类似物在野生型GLP-2序列的一个或多个位置(11,16,20,24)和/或(28)处包含取代,任选地与 位置(2)和位置(3,5,7)和(10)中的一个或多个,和/或一个或多个氨基酸(31)至(33)的缺失和/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。