The apelinergic system: a promising therapeutic target.
BACKGROUND
Apelin is a bioactive peptide known as the ligand of the G-protein-coupled receptor APJ. In recent years, there has been a growing body of evidence regarding the importance of apelin and APJ in the pathophysiology of cardiovascular, metabolic and gastrointestinal diseases, brain signalling, HIV infection and tumor angiogenesis. Therefore, the apelinergic system is involved in the pathogenesis of several diseases that represent a major burden to our society.


METHODS
The goal of this paper is to give an up-to-date review of existing information on apelin/APJ since the discovery of apelin in 1998, with particular focus on their involvement in the regulation of human body systems and potential therapeutic applications.


RESULTS
An overview of the most important physiological functions of the apelinergic system and the diseases that may benefit in the future from its modulation as a therapeutic target.


CONCLUSIONS
Today, the established biological effects of apelin involve major cardiovascular actions, neoangiogenesis, immunologic modulation and insulinemia control as well as body fluid and glucose homeostasis. However, the physiological and pathophysiological role of endogenous apelin is still unsettled and a better and profound knowledge of this system in humans is necessary for the development of novel apelinergic-based therapeutic targets.
Falcão-Pires
Inês
I
University of Porto, Department of Physiology, Cardiovascular R&D Unit, Faculty of Medicine, Alameda Professor Hernâni Monteiro, 4200-319, Porto, Portugal.
Ladeiras-Lopes
Ricardo
R
Leite-Moreira
Adelino F
AF
D000818:Animals; D000073861:Apelin; D000075244:Apelin Receptors; D016503:Drug Delivery Systems; D015195:Drug Design; D006801:Humans; D036341:Intercellular Signaling Peptides and Proteins / Q000378:metabolism*; D008024:Ligands; D043562:Receptors, G-Protein-Coupled / Q000378:metabolism*
C115436:APLN protein, human; C104575:APLNR protein, human; D000073861:Apelin; D000075244:Apelin Receptors; D036341:Intercellular Signaling Peptides and Proteins; D008024:Ligands; D043562:Receptors, G-Protein-Coupled