GPR43/FFA2: physiopathological relevance and therapeutic prospects

Bindels, Laure B. [UCL] Dewulf, Evelyne M. [UCL] Delzenne, Nathalie M. [UCL]

Research interest in free fatty acid-binding receptors has been growing during the past decade, with an aim to better understand the modulation of host physiology in response to nutrition. G-protein-coupled receptor 43 (GPR43), also called free fatty acid receptor 2 (FFA2/FFAR2), binds short-chain fatty acids (SCFAs) produced by the microbial fermentation of carbohydrates and has shown promising therapeutic potential. This review presents current knowledge regarding the pharmacological properties of GPR43 and addresses its functions in selected organs (adipose tissue, intestine and immune cells). Furthermore, the demonstration of GPR43 involvement in several pathological conditions such as obesity, inflammatory disease, and cancer suggests new fields of interest related to this receptor. Finally, GPR43 could be a key player in gut microbes-host crosstalk, although further research is needed to clearly evaluate its role in the management of host health by nutrients or treatments targeting the gut microbiota.