Free fatty acid receptor 4 (FFAR4) (FFAR4)

Free fatty acid receptor 4 (FFAR4), also known as GPR120, is a G protein-coupled receptor that serves as a primary sensor for long-chain fatty acids, particularly omega-3 polyunsaturated fatty acids (PUFAs) like DHA and EPA [11, 20]. It is highly expressed in adipose tissue, where it plays a critical role in promoting adipocyte maturation (adipogenesis) and regulating lipid metabolism [12, 20]. Activation of FFAR4 leads to potent anti-inflammatory effects by inhibiting macrophage-mediated inflammation and enhances insulin sensitivity, making it a significant therapeutic target for metabolic disorders [20, 30]. Dysregulation of FFAR4 signaling is associated with obesity and type 2 diabetes in humans [20]. Several small-molecule agonists, such as TUG-891 and PBI-4050, have been developed to target this receptor for the treatment of metabolic and inflammatory diseases [12, 27]. In addition to its metabolic roles, FFAR4 is involved in the regulation of appetite and the secretion of gut hormones like GLP-1 [17, 20]. Therapeutic strategies focusing on FFAR4 agonists aim to treat conditions such as nonalcoholic steatohepatitis (NASH) and cardiovascular disease by leveraging its anti-inflammatory and insulin-sensitizing properties [20, 31]. However, challenges remain in achieving high selectivity over related receptors like FFAR1 to avoid potential side effects [13, 20].

Other names

GPR120G-protein coupled receptor 120PGR4Omega-3 fatty acid receptor

Agonist