Free fatty acid receptor 3 (for GPR41) and Free fatty acid receptor 2 (for GPR43) (FFAR3 (GPR41), FFAR2 (GPR43))

Free fatty acid receptor 3 (FFAR3/GPR41) and free fatty acid receptor 2 (FFAR2/GPR43) are mammalian G protein-coupled receptors (GPCRs) primarily activated by short-chain fatty acids (SCFAs) such as acetate, propionate, and butyrate, which are produced by gut microbiota during the fermentation of dietary fiber. GPR41 and GPR43 are expressed in various tissues, notably adipocytes, colon epithelial cells, immune cells, and bone tissue. They play significant roles in mediating metabolic regulation, host-microbiome interactions, immune responses, and bone metabolism. Both receptors have been implicated in the pathogenesis and treatment of conditions like obesity, inflammatory diseases (such as colitis, arthritis, and asthma), and potentially cancer. GPR43, in particular, has shown protective effects in animal models of inflammatory diseases, and synthetic agonists targeting it are under investigation. The biological roles of these receptors are complex and context-dependent, with variable protective or causative effects reported depending on tissue type, specific disease model, and experimental conditions

Other names

Free fatty acid receptor 3FFAR3Free fatty acid receptor 2FFAR2SCFA receptorshort-chain fatty acid receptor

Drugs/agonists targeting GPR43/FFAR2 modulate immune and inflammatory responses through activation by short-chain fatty acids, notably acetate, propionate, and butyrate Activation can reduce severity of inflammatory diseases and impact metabolic signaling