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FFA4/GPR120: Pharmacology and Therapeutic Opportunities
Trends in Pharmacological Sciences ( IF 13.8 ) Pub Date : 2017-07-19 , DOI: 10.1016/j.tips.2017.06.006
Graeme Milligan 1 , Elisa Alvarez-Curto 1 , Brian D Hudson 1 , Rudi Prihandoko 1 , Andrew B Tobin 1
Affiliation  

Free Fatty Acid receptor 4 (FFA4), also known as GPR120, is a G-protein-coupled receptor (GPCR) responsive to long-chain fatty acids that is attracting considerable attention as a potential novel therapeutic target for the treatment of type 2 diabetes mellitus (T2DM). Although no clinical studies have yet been initiated to assess efficacy in this indication, a significant number of primary publications and patents have highlighted the ability of agonists with potency at FFA4 to improve glucose disposition and enhance insulin sensitivity in animal models. However, the distribution pattern of the receptor suggests that targeting FFA4 may also be useful in other conditions, ranging from cancer to lung function. Here, we discuss and contextualise the basis for these ideas and the results to support these conclusions.



中文翻译:

FFA4/GPR120:药理学和治疗机会

游离脂肪酸受体 4 (FFA4),也称为 GPR120,是一种对长链脂肪酸有反应的 G 蛋白偶联受体 (GPCR),作为治疗 2 型糖尿病的潜在新型治疗靶点引起了广泛关注糖尿病(T2DM)。尽管尚未启动临床研究来评估该适应症的功效,但大量的主要出版物和专利强调了具有 FFA4 效力的激动剂在动物模型中改善葡萄糖处置和增强胰岛素敏感性的能力。然而,受体的分布模式表明,靶向 FFA4 也可能在其他情况下有用,从癌症到肺功能。在这里,我们讨论和背景化这些想法的基础和支持这些结论的结果。

更新日期:2017-07-19
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