FFA4/GPR120: Pharmacology and Therapeutic Opportunities.
FFA4/GPR120: Pharmacology and Therapeutic Opportunities.
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DOI：
10.1016/j.tips.2017.06.006
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发表时间：
2017-09
影响因子：
13.8
通讯作者：
Tobin AB
中科院分区：
文献类型：
--
作者：
Milligan G;Alvarez-Curto E;Hudson BD;Prihandoko R;Tobin AB
游离脂肪酸受体4(FFA4)，又称GPR120，是一种G蛋白偶联受体，对长链脂肪酸有反应，作为治疗2型糖尿病的新靶点正受到人们的广泛关注。虽然目前还没有临床研究来评估这一适应症的有效性，但相当数量的主要出版物和专利已经强调了在动物模型中具有FFA4活性的激动剂能够改善葡萄糖代谢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在其他情况下也可能有用，从癌症到肺功能。在这里，我们讨论这些想法的基础和支持这些结论的结果，并将其与背景联系起来。目前，对FFA4/GPR120治疗潜力的大量关注针对的是2型糖尿病。在鉴定和表征FFA4/GPR120激动剂配体方面的进展在初级科学文献和专利文献中都是显而易见的。在葡萄糖处理模型中，FFA4/GPR120激动剂似乎非常有效。最近的迹象为FFA4/GPR120配体在癌症治疗领域的考虑提供了支持。FFA4/GPR120在肺中的高水平表达提示在分析FFA4/GPR120配体在急性和慢性呼吸道炎症条件下的潜在治疗作用方面是有用的。
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. Substantial focus on the therapeutic potential of FFA4/GPR120 is currently directed towards type 2 diabetes. Progress in the identification and characterisation of FFA4/GPR120 agonist ligands is apparent in both the primary scientific and patent literatures. In models of glucose handling, FFA4/GPR120 agonists appear highly effective. Recent indications provide support for consideration of FFA4/GPR120 ligands in areas of cancer treatment. High levels of expression of FFA4/GPR120 in the lung suggest utility in analysis of the potential therapeutic roles of FFA4/GPR120 ligands in both acute and chronic airway inflammatory conditions.
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DOI：
10.1074/jbc.m116.754887
发表时间：
2016-12-30
期刊：
The Journal of biological chemistry
影响因子：
--
作者：
Alvarez-Curto E;Inoue A;Jenkins L;Raihan SZ;Prihandoko R;Tobin AB;Milligan G
通讯作者：
Milligan G
影响因子：
4.2
作者：
Agarwal, Sameer;Sasane, Santosh;Desai, Ranjit C.
通讯作者：
Desai, Ranjit C.
影响因子：
5.2
作者：
Belchior, Thiago;Paschoal, Vivian A.;Festuccia, William
通讯作者：
Festuccia, William
影响因子：
3.6
作者：
Christiansen, Elisabeth;Watterson, Kenneth R.;Ulven, Trond
通讯作者：
Ulven, Trond
DOI：
10.1074/jbc.m114.568816
发表时间：
2014-06-27
期刊：
The Journal of biological chemistry
影响因子：
--
作者：
Butcher AJ;Hudson BD;Shimpukade B;Alvarez-Curto E;Prihandoko R;Ulven T;Milligan G;Tobin AB
通讯作者：
Tobin AB