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GLP-1 analogs useful for diabetes treatment

机译:GLP-1类似物可用于糖尿病治疗

摘要

The invention provides effective analogs of the active GLP-1 peptides, 7-34, 7-35, 7-36, and 7-37, which have improved characteristics for treatment of diabetes Type II. These analogs have amino acid substitutions at positions 7-10 and/or are truncated at the C-terminus and/or contain various other amino acid substitutions in the basic peptide. The analogs may either have an enhanced capacity to stimulate insulin production as compared to glucagon or may exhibit enhanced stability in plasma as compared to GLP-1 (7-37) or both. Either of these properties will enhance the potency of the analog as a therapeutic. Analogs having D-amino acid substitutions in the 7 and 8 positions and/or N-alkylated or N-acylated amino acids in the 7 position are particularly resistant to degradation in vivo.
机译:本发明提供了活性GLP-1肽的有效类似物7-34、7-35、7-36和7-37,它们具有改善的II型糖尿病治疗特性。这些类似物在7-10位具有氨基酸取代和/或在C末端被截短和/或在碱性肽中含有各种其他氨基酸取代。与胰高血糖素相比,这些类似物可能具有增强的胰岛素产生能力,或者与GLP-1(7-37)相比,它们可以在血浆中表现出增强的稳定性,或者二者兼有。这些性质中的任何一种都将增强类似物作为治疗剂的效力。在7和8位具有D-氨基酸取代和/或在7位具有N-烷基化或N-酰化氨基酸的类似物对体内降解特别抗性。

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