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发明公开
CN109384839A 胰高血糖素样肽-1类似物及其用途 有权

胰高血糖素样肽-1类似物及其用途
摘要：
本发明提供了一种胰高血糖素样肽-1类似物的前体多肽或其药学上可接受的盐，所述前体多肽具有以下通式Ⅰ所示的氨基酸序列；通式ⅠHX1X2GTFTSDVSSYLEEX3AAX4EFIX5WLVKX6X7X8X9；其中，所述X1、X2、X3、X4、X5、X6、X7、X8和X9表示任意的氨基酸。本发明还提供一种胰高血糖素样肽-1类似物或其药学上可接受的盐。本发明的胰高血糖素样肽-1类似物由基于内源性GLP-1(7-36/37)序列优化后的多肽和特定结构的聚乙二醇缀合而得，具有更强的降血糖活性，可减少用药剂量，而且体内半衰期显著延长，有望提高临床依从性，并且本发明提供的前体多肽序列与内源性GLP-1(7-36/37)高度同源，可以降低免疫原性，因此具有更好的作为药物开发应用的潜力。
摘要（英）：

The present invention provides a precursor polypeptide or a pharmaceutically acceptable salt of a glucagon-like peptide-1 analogue, wherein the precursor polypeptide has an amino acid sequence represented by the following general formula I HX1X2GTFTSDVSSYLEEX3AAX4EFIX5WLVKX6X7X8X9, and X1, X2, X3, X4, X5, X6, X7, X8 and X9 represent arbitrary amino acids. The present invention further provides a glucagon-like peptide-1 analog or a pharmaceutically acceptable salt thereof. According to the present invention, the glucagon-like peptide-1 analog is obtained by conjugating a polypeptide optimized based on an endogenous GLP-1 (7-36/37) sequence and polyethylene glycol having a specific structure, has strong blood glucose lowering activity so as to reduce the dosage, and has significantly-prolonged half-life in vivo so as to be expected to improve clinical compliance; and the precursor polypeptide and the endogenous GLP-1 (7-36/37) are highly homologous in the sequence so as to reduce the immunogenicity, such that the precursor polypeptide has good potential in the drug development application.

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