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胰高血糖素样肽-1 受体激动剂的发现和研发。

The Discovery and Development of Glucagon-Like Peptide-1 Receptor Agonists.

机构信息

School of Environmental and Chemical Engineering, Shanghai University, China.

School of Life Sciences, Shanghai University, China.

出版信息

Curr Med Chem. 2024;31(20):2921-2943. doi: 10.2174/0929867330666230416153301.

DOI:10.2174/0929867330666230416153301
PMID:37062063
Abstract

Diabetes mellitus has become a serious life-threatening disease. As one of the new drugs for the treatment of diabetes, GLP-1 receptor agonists have attracted a lot of attention. Compared with traditional hypoglycemic drugs, GLP-1 receptor agonists have good safety and tolerability. To a certain extent, they overcome the problem of the short half-life of natural GLP-1 and can exist stably in patients for a long time, achieving good results in the treatment of diabetes, as well as improving the symptoms of some complications. The GLP-1 receptor agonists in the market are all peptide drugs. Compared with peptide drugs, small molecule agonists have the advantages of low cost and oral administration. In this article, we review the recent research progress of GLP-1 receptor agonists.

摘要

糖尿病已成为一种严重威胁生命的疾病。GLP-1 受体激动剂作为治疗糖尿病的新药之一,受到了广泛关注。与传统的降糖药物相比,GLP-1 受体激动剂具有良好的安全性和耐受性。在一定程度上克服了天然 GLP-1 半衰期短的问题,可以在患者体内稳定存在很长时间,在治疗糖尿病方面取得了良好的效果,同时改善了一些并发症的症状。目前市场上的 GLP-1 受体激动剂均为肽类药物。与肽类药物相比,小分子激动剂具有成本低、可口服的优点。本文就 GLP-1 受体激动剂的研究进展作一综述。

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本文引用的文献

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Diabetes Obes Metab. 2023 Mar;25(3):805-814. doi: 10.1111/dom.14928. Epub 2022 Dec 19.
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Effect of polyethylene Glycol Loxenatide (long-acting GLP-1RA) on lipid, glucose levels and weight in type 2 diabetes mellitus patients with obesity.聚乙二醇洛塞那肽(长效 GLP-1RA)对肥胖 2 型糖尿病患者的血脂、血糖和体重的影响。
Eur Rev Med Pharmacol Sci. 2022 Nov;26(21):7996-8003. doi: 10.26355/eurrev_202211_30153.
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N Engl J Med. 2022 Dec 15;387(24):2245-2257. doi: 10.1056/NEJMoa2208601. Epub 2022 Nov 2.
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The metabolic effects of adding exenatide to basal insulin therapy when targeting remission in early type 2 diabetes in a randomized clinical trial.在一项随机临床试验中,针对早期 2 型糖尿病缓解目标,添加 exenatide 到基础胰岛素治疗的代谢效应。
Nat Commun. 2022 Oct 16;13(1):6109. doi: 10.1038/s41467-022-33867-9.
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Nat Med. 2022 Oct;28(10):2083-2091. doi: 10.1038/s41591-022-02026-4. Epub 2022 Oct 10.
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