通过糖基化扫描取代鉴定具有延长降血糖活性的糖基化 exendin-4 类似物。
Identification of glycosylated exendin-4 analogue with prolonged blood glucose-lowering activity through glycosylation scanning substitution.
机构信息
Discovery Research Laboratories, Shionogi and Co., Ltd, Fukushima-ku, Osaka, Japan.
出版信息
Bioorg Med Chem Lett. 2010 Aug 1;20(15):4631-4. doi: 10.1016/j.bmcl.2010.06.002. Epub 2010 Jun 4.
Exendin-4, a glucagon-like peptide 1 receptor agonist, is a potent therapeutic xenopeptide hormone for the treatment of type 2 diabetes. In order to further improve in vivo activity, we examined the introduction of sialyl N-acetyllactosamine (sialyl LacNAc) to exendin-4. The glycosylated analogue having sialyl LacNAc at position 28 was found to have improved in vivo activity with prolonged glucose-lowering activity.
Exendin-4，一种胰高血糖素样肽 1 受体激动剂，是一种治疗 2 型糖尿病的有效治疗性异源肽激素。为了进一步提高体内活性，我们研究了在 Exendin-4 中引入唾液酸化 N-乙酰乳糖胺（sialyl LacNAc）。结果发现，在 28 位具有唾液酸化 LacNAc 的糖基化类似物具有改善的体内活性和延长的降血糖活性。
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