2015
DOI: 10.1016/j.ejphar.2015.06.028
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FFA4 receptor (GPR120): A hot target for the development of anti-diabetic therapies

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Cited by 38 publications
(25 citation statements)
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“…Hence supplementation with such molecules or finding agonists that target pathways associated with these lipids, such as GPR120 signaling (240,241), could help reduce lipid-induced metaflammation in a variety of immunometabolic diseases, including obesity and diabetes. The -3 fatty acids are further metabolized into resolvins, which are involved in resolution of inflammation (169), a persistent process in diabetes.…”
Section: Bioactive Lipids and Regulation Of Inflammationmentioning
confidence: 99%
“…Hence supplementation with such molecules or finding agonists that target pathways associated with these lipids, such as GPR120 signaling (240,241), could help reduce lipid-induced metaflammation in a variety of immunometabolic diseases, including obesity and diabetes. The -3 fatty acids are further metabolized into resolvins, which are involved in resolution of inflammation (169), a persistent process in diabetes.…”
Section: Bioactive Lipids and Regulation Of Inflammationmentioning
confidence: 99%
“…Indeed, the FFA1 agonist fasiglifam entered phase III clinical trials; although it was clearly able to regulate glycemia and to produce clinically relevant lowering of hemoglobin A1c levels in patients with type 2 diabetes Poitout, 2013, 2015;Kaku et al, 2015), it was withdrawn from further trials because of concerns of possible liver toxicity. Although FFA4 is expressed in the pancreas (Stone et al, 2014;Suckow et al, 2014), where it may play roles in the regulation of glucagon production (Suckow et al, 2014), it is also expressed in various enteroendocrine cells (Parker et al, 2009;Iwasaki et al, 2015;Liu et al, 2015), adipocytes (Oh et al, 2010(Oh et al, , 2014Liu et al, 2015) and macrophages (Oh et al, 2010(Oh et al, , 2014Im, 2015;Liu et al, 2015). Potential combinations of effects on the release of incretins and/or satiety-regulating hormones in the gut, differentiation of and uptake of glucose by adipocytes, and control of the release of inflammatory mediators by macrophages have suggested that FFA4 might also be a useful therapeutic target to modulate insulin resistance and glucose homeostasis Oh et al, 2014;Liu et al, 2015;Milligan et al, 2015).…”
Section: Introductionmentioning
confidence: 99%
“…Since then, not least because essential and other polyunsaturated ω -3 fatty acids with health-promoting properties are among the most potent fatty acid activators of this receptor (Hirasawa et al, 2005; Christiansen et al, 2015), there has been strong interest in better understanding the biologic functions of FFA4 and in its potential as a therapeutic target (Liu et al, 2015; Li et al, 2016). Because reported effects of FFA4 activation include regulation of glucose homeostasis (Oh et al, 2014; Azevedo et al, 2016), regulation of release of incretins and satiety-regulating hormones (Hirasawa et al, 2005), modulation of insulin sensitivity (Oh et al, 2010, 2014; Azevedo et al, 2016), and potential effects on weight gain (Ichimura et al, 2012; Mo et al, 2013; Azevedo et al, 2016), a large focus of studies on FFA4 has centered on the possibility that agonists of this receptor might be useful antidiabetic agents (Cornall et al, 2014; Zhang and Leung, 2014; Moran et al, 2016).…”
Section: Introductionmentioning
confidence: 99%