Perspectives in GLP-1 Research: New Targets, New Receptors

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• 作者：Giulia Cantini¹ ; ^{giulia.cantini@unifi.it" class="auth_mail" title="E-mail the corresponding author} ; Edoardo Mannucci¹ ; ² ; Michaela Luconi¹ ; ^{michaela.luconi@unifi.it" class="auth_mail" title="E-mail the corresponding author}
• 关键词：glucagon-like peptide-1 ; GLP-1 receptor agonists ; incretins ; cardioprotection
• 刊名：Trends in Endocrinology & Metabolism
• 出版年：2016
• 出版时间：June 2016
• 年：2016
• 卷：27
• 期：6
• 页码：427-438
• 全文大小：2216 K

文摘

The incretin hormone glucagon-like peptide-1 (GLP-1) binds to and activates its G-protein-coupled-receptor GLP-1R to reduce glycaemia through the stimulation of insulin and suppression of pancreatic glucagon secretion. Recently, GLP-1 effects unrelated to glucose homeostasis have been discovered in myocardium, bone, adipose tissue, and other target organs, which appear to be mainly mediated by GLP-1R-independent pathways. Here, we summarize knowledge on GLP-1R agonists (GLP-1RAs) as they relate to the improvement of glucose control, and focus on the most recently described effects, discussing the preclinical evidence of the involvement of alternative receptors and signalling mechanisms. It is now evident that the universe of GLP-1RAs is expanding further from the initial incretin effect, opening new unforeseen avenues for research and clinical applications.