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胰高血糖素样肽-1类似物:概述

Glucagon-like peptide-1 analogues: An overview.

作者信息

Gupta Vishal

机构信息

Department of Endocrinology, Jaslok Hospital and Research Centre, 15 - Dr. Deshmukh Marg, Pedder Road, Mumbai, Maharashtra, India.

出版信息

Indian J Endocrinol Metab. 2013 May;17(3):413-21. doi: 10.4103/2230-8210.111625.

Abstract

Abnormalities of the incretin axis have been implicated in the pathogenesis of type 2 diabetes mellitus. Glucagon-like peptide-1 (GLP-1) and gastroinhibitory intestinal peptide constitutes >90% of all the incretin function. Augmentation of GLP-1 results in improvement of beta cell health in a glucose-dependant manner (post-prandial hyperglycemia) and suppression of glucagon (fasting hyperglycemia), amongst other beneficial pleiotropic effects. Native GLP-1 has a very short plasma half-life and novel methods have been developed to augment its half life, such that its anti-hyperglycemic effects can be exploited. They can be broadly classified as exendin-based therapies (exenatide, exenatide once weekly), DPP-4-resistant analogues (lixisenatide, albiglutide), and analogues of human GLP-1 (liraglutide, taspoglutide). Currently, commercially available analogues are exenatide, exenatide once weekly, and liraglutide. This review aims to provide an overview of most GLP-1 analogues.

摘要

肠促胰岛素轴异常与2型糖尿病的发病机制有关。胰高血糖素样肽-1(GLP-1)和胃抑制性肠肽构成了所有肠促胰岛素功能的90%以上。GLP-1的增加以葡萄糖依赖的方式(餐后高血糖)改善β细胞健康,并抑制胰高血糖素(空腹高血糖),以及产生其他有益的多效性作用。天然GLP-1的血浆半衰期非常短,现已开发出新方法来延长其半衰期,以便能够利用其降血糖作用。它们大致可分为基于艾塞那肽的疗法(艾塞那肽、每周一次的艾塞那肽)、二肽基肽酶-4(DPP-4)抗性类似物(利司那肽、阿必鲁肽)和人GLP-1类似物(利拉鲁肽、塔司鲁肽)。目前,市售的类似物有艾塞那肽、每周一次的艾塞那肽和利拉鲁肽。本综述旨在概述大多数GLP-1类似物。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/61d9/3712370/4dc5e4264903/IJEM-17-413-g001.jpg

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