Polymer-based delivery of glucagon-like Peptide-1 for the treatment of diabetes.
Polymer-based delivery of glucagon-like Peptide-1 for the treatment of diabetes.
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DOI：
10.5402/2012/340632
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发表时间：
2012
期刊：
影响因子：
--
通讯作者：
Kim SW
中科院分区：
文献类型：
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作者：
Kim PH;Kim SW
肠促胰岛素激素，胰高血糖素样肽-1 （GLP-1）及其受体激动剂（exendin-4），众所周知具有葡萄糖稳态、胰岛素调节作用以及减肥和食物摄入作用。然而，由于GLP-1被二肽基肽酶- iv （DPP-IV）酶快速降解和exendin-4的肾脏消除，它们的临床应用受到限制。虽然exendin-4的半衰期比GLP-1长，但仍需要频繁注射以维持治疗糖尿病的疗效。近几十年来，各种聚合物递送系统已经被开发出来，用于递送GLP-1和exendin-4基因或肽，用于它们的长期作用和异位组织中的额外生产。在此，我们讨论了表达盒和肽的长期生产和分泌天然肽的修饰。此外，描述了用于递送修饰GLP-1或exendin-4的非病毒或病毒系统的特性。此外，还讨论了近年来通过化学偶联与各种智能聚合物进行化学偶联以提高GLP-1或延伸蛋白-4肽生物半衰期的研究进展。
The incretin hormones, glucagon-like peptide-1 (GLP-1) and its receptor agonist (exendin-4), are well known for glucose homeostasis, insulinotropic effect, and effects on weight loss and food intake. However, due to the rapid degradation of GLP-1 by dipeptidylpeptidase-IV (DPP-IV) enzyme and renal elimination of exendin-4, their clinical applications have been restricted. Although exendin-4 has longer half-life than GLP-1, it still requires frequent injections to maintain efficacy for the treatment of diabetes. In recent decades, various polymeric delivery systems have been developed for the delivery of GLP-1 and exendin-4 genes or peptides for their long-term action and the extra production in ectopic tissues. Herein, we discuss the modification of the expression cassettes and peptides for long-term production and secretion of the native peptides. In addition, the characteristics of nonviral or viral system used for a delivery of a modified GLP-1 or exendin-4 are described. Furthermore, recent efforts to improve the biological half-life of GLP-1 or exendin-4 peptide via chemical conjugation with various smart polymers via chemical conjugation compared with native peptide are discussed.