G-protein-coupled receptors (GPCRs) in the treatment of diabetes: Current view and future perspectives

被引：15

作者：

Sebastiani, Guido ^{[1
,2
]}

Ceccarelli, Elena ^{[1
]}

Castagna, Maria Grazia ^{[1
]}

Dotta, Francesco ^{[1
,2
]}

机构：

[1] Univ Siena, Dept Med Surg & Neurosci, Siena, Italy

[2] Fdn Umberto Di Mario ONLUS, Toscana Life Sci, Siena, Italy

来源：

BEST PRACTICE & RESEARCH CLINICAL ENDOCRINOLOGY & METABOLISM | 2018年 / 32卷 / 02期

关键词：

G-protein coupled receptors; type; 2; diabetes; incretin hormones; insulin secretion; GLUCAGON-LIKE PEPTIDE-1; IMPROVES GLUCOSE-TOLERANCE; LEUKOTRIENE B-4 RECEPTOR; INSULIN-SECRETION; CLINICAL DEVELOPMENT; THERAPEUTIC TARGET; GPR40; AGONISTS; BETA-CELLS; GLP-1; DISCOVERY;

D O I：

10.1016/j.beem.2018.02.005

中图分类号：

R5 [内科学];

学科分类号：

1002 ; 100201 ;

摘要：

G-protein coupled receptors (GPCRs) represent the largest receptor family in the genome and are of great interest for the design of novel drugs in a wide variety of diseases including neurologic disorders, obesity and Type 2 diabetes mellitus. The latter is a chronic disease characterized by insulin resistance and impaired insulin secretion, affecting >400 million patients worldwide. Here we provide an overview on: a) The molecular basis of GPCR signalling and of its involvement in the regulation of insulin secretion and of glucose homeostasis; b) the role of GPCRs in type 2 diabetes pathophysiology and as therapeutic targets of current and future glucose-lowering drugs. (C) 2018 Elsevier Ltd. All rights reserved.

引用

页码：201 / 213

页数：13

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