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窖蛋白-1在 GLP-1 作用中的新角色。

Emerging Role of Caveolin-1 in GLP-1 Action.

机构信息

Department of Internal Medicine and Medical Specialties, University of Genoa, Genoa, Italy.

出版信息

Front Endocrinol (Lausanne). 2021 Apr 14;12:668012. doi: 10.3389/fendo.2021.668012. eCollection 2021.

DOI:10.3389/fendo.2021.668012
PMID:33935978
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC8079975/
Abstract

Glucagon-like peptide-1 (GLP-1) is a gut hormone mainly produced in the intestinal epithelial endocrine L cells, involved in maintaining glucose homeostasis. The use of GLP-1 analogous and dipeptidyl peptidase-IV (DPP-IV) inhibitors is well-established in Type 2 Diabetes. The efficacy of these therapies is related to the activation of GLP-1 receptor (GLP-1R), which is widely expressed in several tissues. Therefore, GLP-1 is of great clinical interest not only for its actions at the level of the beta cells, but also for the extra-pancreatic effects. Activation of GLP-1R results in intracellular signaling that is regulated by availability of downstream molecules and receptor internalization. It has been shown that GLP-1R co-localizes with caveolin-1, the main component of caveolae, small invagination of the plasma membrane, which are involved in controlling receptor activity by assembling signaling complexes and regulating receptor trafficking. The aim of this review is to outline the important role of caveolin-1 in mediating biological effects of GLP-1 and its analogous.

摘要

胰高血糖素样肽-1（GLP-1）是一种主要由肠道上皮内分泌 L 细胞产生的肠激素，参与维持葡萄糖内稳态。GLP-1 类似物和二肽基肽酶-4（DPP-4）抑制剂在 2 型糖尿病中的应用已得到充分证实。这些治疗方法的疗效与 GLP-1 受体（GLP-1R）的激活有关，GLP-1R 广泛表达于几种组织中。因此，GLP-1 不仅因其在β细胞水平的作用，而且因其在胰腺外的作用而具有重要的临床意义。GLP-1R 的激活导致细胞内信号转导，其受下游分子的可用性和受体内化的调节。已经表明，GLP-1R 与 caveolin-1 共定位，caveolin-1 是 caveolae 的主要成分，caveolae 是质膜的小凹陷，通过组装信号复合物和调节受体运输来控制受体活性。本综述的目的是概述 caveolin-1 在介导 GLP-1 及其类似物的生物学效应中的重要作用。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/2715/8079975/0abe9f3c556c/fendo-12-668012-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/2715/8079975/0abe9f3c556c/fendo-12-668012-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/2715/8079975/0abe9f3c556c/fendo-12-668012-g001.jpg

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New Insights into Beta-Cell GLP-1 Receptor and cAMP Signaling.β细胞胰高血糖素样肽-1 受体和 cAMP 信号转导的新见解
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