Role of free fatty acid receptors in the regulation of energy metabolism

Functions of omega-3 fatty acids and FFA4 (GPR120) in macrophages

“…Completion of the human genome project revealed the sequences of 865 GPCR genes, and many known signaling molecules (ligands) were found to utilize orphan GPCRs as receptors (Davenport et al, 2013;Fredriksson et al, 2003;Im, 2002Im, , 2004. Several GPCRs have been reported for free fatty acids (FFA) and these were renamed by the International Union of Basic and Clinical Pharmacology Committee on receptor nomenclature and drug classification (NC-IUPHAR), as FFA1, FFA2, FFA3, and FFA4 (formerly known as GPR40, GPR43, GPR41, and GPR120, respectively) (Davenport et al, 2013;Im, 2004Im, , 2013, which recognize and respond to short chain (FFA2 and FFA3), medium long chain (FFA1), and unsaturated long chain fatty acids (FFA4) (Hara et al, 2013;Talukdar et al, 2011). Additionally, GPR84 and GPR119 have also been reported to function as receptors for medium chain fatty acids and fatty acid derivatives, respectively (Im, 2013;Overton et al, 2006;Wang et al, 2006).…”

10-oxo-12(Z)-octadecenoic acid, a linoleic acid metabolite produced by gut lactic acid bacteria, potently activates PPARγ and stimulates adipogenesis

“…Long-chain fatty acids (LCFAs) work both as essential nutrients and signaling molecules [14,15]. Several molecules have been identified to work as fatty acid receptors including nuclear receptors and G-protein-coupled receptors, many of which have been shown to play an important role in the regulation of whole-body energy metabolisms physiologically [14,15].…”

“…Several molecules have been identified to work as fatty acid receptors including nuclear receptors and G-protein-coupled receptors, many of which have been shown to play an important role in the regulation of whole-body energy metabolisms physiologically [14,15]. Peroxisome proliferatoractivated receptors (PPARs; PPARa, PPARg, and PPARd) are members of the nuclear receptor superfamily of transcription factors that are activated by the binding of small hydrophilic ligands, including LCFAs [14,16e18].…”

SIRT1 prevents pulmonary thrombus formation induced by arachidonic acid via downregulation of PAF receptor expression in platelets

“…Many GPCRs recognize specific phospholipids and free fatty acids [31,32], which suggested that the elucidation of the involved mechanism could provide useful therapeutic clues for the treatment of lipid-mediated diseases. It has been established that PAFR specifically recognizes PAF, but no evidence has been reported upon the relationship between PAFR and other lipids.…”