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    • 3. 发明公开
    • GLYCOSYLATED GLP-1 PEPTIDE
    • EP2298801A1
    • 2011-03-23
    • EP09766408.0
    • 2009-06-15
    • Otsuka Chemical Co., Ltd.
    • KAJIHARA, YasuhiroTSUJI, TakashiSAKAMOTO, IzumiNAMBU, YuriHAYASHI, NaohiroISHII, KazuyukiFUKAE, KazuhiroTEZUKA, KatsunariASAI, Hiroaki
    • C07K14/605A61K38/00A61P1/04A61P3/04A61P3/10C12N15/09
    • C07K14/605A61K38/00
    • An object of the present invention is to provide an oligosaccharide chain added GLP-1 peptide that has higher stability in blood than that of GLP-1 and, preferably, exhibits higher activity of controlling blood-sugar levels than that of GLP-1. The present invention provides an oligosaccharide chain added GLP-1 peptide having GLP-1 activity, wherein at least two amino acids are each substituted with an oligosaccharide chain added amino acid, in (a) GLP-1; (b) a peptide having the amino acid sequence of GLP-1 with deletion, substitution or addition of one or several amino acids; or (c) a GLP-1 analog. The present invention also provides an oligosaccharide chain added GLP-1 peptide having GLP-1 activity, wherein at least one amino acid is substituted with an oligosaccharide chain added amino acid, in the (a), (b) or (c) and the oligosaccharide chain is an oligosaccharide chain comprising oligo hyaluronic acid. In the oligosaccharide chain added amino acid, the oligosaccharide chain may be linked to the amino acid via a linker.
    • 本发明的目的在于提供一种与GLP-1相比血中稳定性更高且优选显示出比GLP-1更高的血糖控制活性的附加糖链的GLP-1肽。 在(a)GLP-1中,本发明提供具有GLP-1活性的附加糖链的GLP-1肽,其中至少两个氨基酸各自被添加了糖链的氨基酸取代; (b)具有缺失,取代或增加一个或几个氨基酸的具有GLP-1氨基酸序列的肽; 或(c)GLP-1类似物。 (a),(b)或(c)中,本发明还提供具有GLP-1活性的附加糖链的GLP-1肽,其中至少一个氨基酸被添加了糖链的氨基酸取代。 寡糖链是包含寡聚透明质酸的寡糖链。 在附加了糖链的氨基酸中,寡糖链可以通过接头与氨基酸连接。