Free fatty acid receptors as therapeutic targets for the treatment of diabetes.
Free fatty acid receptors as therapeutic targets for the treatment of diabetes.
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DOI：
10.3389/fphar.2014.00236
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发表时间：
2014
影响因子：
5.6
通讯作者：
Kimura I
中科院分区：
文献类型：
--
作者：
Ichimura A;Hasegawa S;Kasubuchi M;Kimura I
营养调节能量平衡;然而，能量平衡失调可导致代谢紊乱，如肥胖和糖尿病。脂肪酸是调节各种细胞过程和生理功能的必需能量来源和信号分子。最近，几个孤儿G蛋白偶联受体被确定为游离脂肪酸受体（FFARs）。GPR 40/FFAR 1和GPR 120/FFAR 4被中链和/或长链脂肪酸激活，而GPR 41/FFAR 3和GPR 43/FFAR 2被短链脂肪酸激活。FFAR被认为是治疗代谢紊乱如肥胖和2型糖尿病的新型药物的靶标，因为最近的研究表明这些受体参与各种组织（包括脂肪、肠和免疫组织）中的能量代谢。在这篇综述中，我们总结了FFARs的生理作用，提供了一个全面的概述FFARs的能量调节，并讨论了治疗代谢紊乱的新前景。
Nutrition regulates energy balance; however, dysfunction of energy balance can cause metabolic disorders, such as obesity and diabetes. Fatty acids are an essential energy source and signaling molecules that regulate various cellular processes and physiological functions. Recently, several orphan G protein-coupled receptors were identified as free fatty acid receptors (FFARs). GPR40/FFAR1 and GPR120/FFAR4 are activated by medium- and/or long-chain fatty acids, whereas GPR41/FFAR3 and GPR43/FFAR2 are activated by short-chain fatty acids. FFARs are regarded as targets for novel drugs to treat metabolic disorders, such as obesity and type 2 diabetes, because recent studies have showed that these receptors are involved in the energy metabolism in various tissues, including adipose, intestinal, and immune tissue. In this review, we summarize physiological roles of the FFARs, provide a comprehensive overview of energy regulation by FFARs, and discuss new prospects for treatment of metabolic disorders.
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