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胰岛素和GLP-1类似物长效化策略研究的最新进展

李承业, 黄文龙, 钱海

李承业, 黄文龙, 钱海. 胰岛素和GLP-1类似物长效化策略研究的最新进展[J]. 中国药科大学学报, 2018, 49(6): 660-670. DOI: 10.11665/j.issn.1000-5048.20180604
引用本文: 李承业, 黄文龙, 钱海. 胰岛素和GLP-1类似物长效化策略研究的最新进展[J]. 中国药科大学学报, 2018, 49(6): 660-670. DOI: 10.11665/j.issn.1000-5048.20180604
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LI Chengye, HUANG Wenlong, QIAN Hai. Advances in the research of long-acting strategy of insulin and GLP-1 analogs[J]. Journal of China Pharmaceutical University, 2018, 49(6): 660-670. DOI: 10.11665/j.issn.1000-5048.20180604
Citation: LI Chengye, HUANG Wenlong, QIAN Hai. Advances in the research of long-acting strategy of insulin and GLP-1 analogs[J]. Journal of China Pharmaceutical University, 2018, 49(6): 660-670. DOI: 10.11665/j.issn.1000-5048.20180604
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胰岛素和GLP-1类似物长效化策略研究的最新进展

  • 中国药科大学新药研究中心

基金项目: 国家自然科学基金资助项目(No.81673299)

Advances in the research of long-acting strategy of insulin and GLP-1 analogs

摘要

    摘要
  • 摘要: 胰岛素类似物和胰高血糖素样肽-1(glucagon-like peptide-1，GLP-1)类似物是糖尿病治疗领域的常用药物。胰岛素和GLP-1都属于内源性多肽，具有高效性和高选择性等优点。但传统胰岛素药物起效慢，作用时间短，且存在低血糖风险；而GLP-1因为肾脏清除和体内酶的代谢，半衰期很短，二者都不能稳定且持续地控制血糖。因此，对胰岛素和GLP-1进行长效化研究具有重要意义。本文从多肽药物长效化策略以及临床评估数据等方面出发，对已上市以及在研相关药物的研究进展进行综述，为新型长效化胰岛素和GLP-1类似物的设计提供理论参考。
    Abstract: Insulin as well as glucagon-like peptide 1(GLP-1)and its analogs are commonly used in treating type II diabetes. Both insulin and GLP-1 are endogenous peptides, and have advantages such as high efficiency and selectivity. However, there are some disadvantages to using regular insulin with slow effect, short-time effect and risk of hypoglycemia. Due to the elimination of kidneys and the metabolism of enzymes, the half-life of GLP-1 is so short that neither of them can stabilize glucose. Therefore, it is of great significance to study the long-acting strategy of insulin and GLP-1. Based on the long-acting strategy and pharmacological assessment of peptide drugs, this paper reviewed the latest progress of the related drugs that already on the market and under research to provide references for the design of novel long-acting insulin and GLP-1 analogs.
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  • 刊出日期:  2018-12-24

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