Apelin, a bioactive peptide, is the endogenous ligand of APJ, a G protein-coupled receptor which is widely expressed in peripheral tissues and in the central nervous system. The apelin/APJ system is involved in the regulation of various physiological functions and is a therapeutic target in different pathologies; the development of APJ agonists and antagonists has thus increased. Area covered: This review focuses on the in vitro and in vivo metabolic effects of apelin in physiological conditions and in the context of metabolic diseases. Expert opinion: In experimental models, novel APJ agonists are efficient in vivo, to treat metabolic diseases and associated complications. However, more clinical trials are necessary to determine whether molecules that target APJ could become an alternative therapeutic strategy in the treatment of metabolic diseases and associated complications.
Keywords: Apelin; apelin/APJ system; energy metabolism; obesity; type 2 diabetes.