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。
摘要:
The present invention provides an insulin molecule that provides a protracted, even basal duration of action. The insulin molecule comprises a modification at the N-terminus of the A-chain, optionally a modification at the N-terminus of the B-chain, a modification at a B-chain lysine, and optionally a modification at the C-terminus of the A-chain. The present invention also provides a method of treating diabetes mellitus comprising administering the insulin molecule.
摘要:
This invention relates the use of glucagon-like peptides such as GLP-1, a GLP-1 analog, or a GLP-1 derivative in methods and compositions for reducing body weight.
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。
摘要:
This invention relates the use of glucagon-like peptides such as GLP-1, a GLP-1 analog, or a GLP-1 derivative in methods and compositions for reducing body weight.