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  • FFA4/GPR120: Pharmacology a...
    Milligan, Graeme; Alvarez-Curto, Elisa; Hudson, Brian D.; Prihandoko, Rudi; Tobin, Andrew B.

    Trends in pharmacological sciences (Regular ed.), September 2017, 2017-09-00, 20170901, Letnik: 38, Številka: 9
    Journal Article

    Free Fatty Acid receptor 4 (FFA4), also known as GPR120, is a G-protein-coupled receptor (GPCR) responsive to long-chain fatty acids that is attracting considerable attention as a potential novel therapeutic target for the treatment of type 2 diabetes mellitus (T2DM). Although no clinical studies have yet been initiated to assess efficacy in this indication, a significant number of primary publications and patents have highlighted the ability of agonists with potency at FFA4 to improve glucose disposition and enhance insulin sensitivity in animal models. However, the distribution pattern of the receptor suggests that targeting FFA4 may also be useful in other conditions, ranging from cancer to lung function. Here, we discuss and contextualise the basis for these ideas and the results to support these conclusions. Substantial focus on the therapeutic potential of FFA4/GPR120 is currently directed towards type 2 diabetes. Progress in the identification and characterisation of FFA4/GPR120 agonist ligands is apparent in both the primary scientific and patent literatures. In models of glucose handling, FFA4/GPR120 agonists appear highly effective. Recent indications provide support for consideration of FFA4/GPR120 ligands in areas of cancer treatment. High levels of expression of FFA4/GPR120 in the lung suggest utility in analysis of the potential therapeutic roles of FFA4/GPR120 ligands in both acute and chronic airway inflammatory conditions.