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Apelin is an endogenous peptide capable of binding to the apelin receptor (APJ), which was originally described as an unprimed G protein-coupled receptor. Apelin and APJ are widely expressed in a variety of tissues and organ systems. They are implicated in different key physiological processes, such as angiogenesis, cardiovascular function, cell proliferation and regulation of energy metabolism. On the other hand, this ligand receptor is also involved in several pathologies including diabetes, obesity, cardiovascular disease and cancer.