Free Fatty Acid Receptor 1 (FFAR1)

GPR40; FFA1R; G Protein-Coupled Receptor 40

SPN	T840
HGNC	4498
MGI	2684079
PubMed	23378609
RGD	628613
UniProt	O14842
Wiki	FFAR1

Free fatty acid receptor 1(FFA1) 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.

Reference

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J. Biol. Chem. 278:11303-11311(2003) [PubMed] [Europe PMC] [Abstract]

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J. Biol. Chem. 284:3529-3536(2009) [PubMed] [Europe PMC] [Abstract]

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"A novel antidiabetic drug, fasiglifam/TAK-875, acts as an ago-allosteric modulator of FFAR1."
PLoS ONE 8:E76280-E76280(2013) [PubMed] [Europe PMC] [Abstract]

"High-resolution structure of the human GPR40 receptor bound to allosteric agonist TAK-875."
Nature 513:124-127(2014) [PubMed] [Europe PMC] [Abstract]