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G protein-coupled receptors (GPCR) represent a large family of proteins that share a unique membrane topology made of seven transmembrane segments. These receptors are an evolutionary success as they constitute more than 1% of the genoma. In addition, the same structural archetype has been selected to recognize a large variety of ligands and to activate multiple intracellular cascades via the coupling to different G proteins. Accordingly, G protein-coupled receptors participate in a wide range of physiological functions. The corollary of this physiological importance is that many pathologies are linked to a dysfunction of these signalling pathways. Indeed, half of the pharmacological drugs used to treat human diseases corresponds to molecules which interact with this family of receptors. In this context, the discovery of new receptors not only has an evident physiological interest, but also represents a therapeutic potential by the development of new pharmacological agents. The discovery and history of apelin signalling provides the best example of the close relationship between basic research and its pharmacoclinical implications.

Apelin Signalling: Lineage Marker and Functional Actor of Blood Vessel Formation