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International Union of Pharmacology. LXXI. Free fatty acid receptors FFA1, -2, and -3: pharmacology and pathophysiological functions.
Pharmacological Reviews ( IF 19.3 ) Pub Date : 2008-12-01 , DOI: 10.1124/pr.108.00802
Leigh A Stoddart 1 , Nicola J Smith , Graeme Milligan
Affiliation  

Identification of G protein-coupled receptors that are activated by free fatty acids has led to considerable interest in their pharmacology and function because of the wide range of normal physiology and disease states in which fatty acids have been implicated. Free fatty acid receptor (FFA) 1 is activated by medium- to long-chain fatty acids and is expressed in the insulin-producing beta-cells of the pancreas. Activation of FFA1 has been proposed to mediate fatty acid augmentation of glucose-stimulated insulin secretion although it is unclear whether the known long-term detrimental effects of beta-cell exposure to high levels of fatty acids are also mediated through this receptor. The related receptors FFA2 and FFA3 are both activated by short-chain fatty acids although they have key differences in the signaling pathways they activate and tissue expression pattern. The aim of this review is to provide a comprehensive overview of the current understanding of the pharmacology and physiological role of these fatty acid receptors.

中文翻译:

国际药理学联合会。六十一。游离脂肪酸受体 FFA1、-2 和 -3:药理学和病理生理学功能。

游离脂肪酸激活的 G 蛋白偶联受体的鉴定引起了对其药理学和功能的极大兴趣,因为脂肪酸涉及广泛的正常生理学和疾病状态。游离脂肪酸受体 (FFA) 1 被中长链脂肪酸激活,并在胰腺的产生胰岛素的 β 细胞中表达。已提议激活 FFA1 以介导葡萄糖刺激的胰岛素分泌的脂肪酸增加,尽管尚不清楚 β 细胞暴露于高水平脂肪酸的已知长期有害影响是否也通过该受体介导。相关受体 FFA2 和 FFA3 均由短链脂肪酸激活,尽管它们在激活的信号通路和组织表达模式方面存在关键差异。本综述的目的是全面概述目前对这些脂肪酸受体的药理学和生理学作用的理解。
更新日期:2019-11-01
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