Unravelling the roles of the apelin system: prospective therapeutic applications in heart failure and obesity

Trends Pharmacol Sci. 2006 Apr;27(4):190-4. doi: 10.1016/j.tips.2006.02.006. Epub 2006 Mar 13.


The apelin receptor was initially classed as an orphan G-protein-coupled receptor, and little was known about its physiological functions until apelin, the endogenous ligand, was identified. Similarities between the structure and anatomical distribution of apelin and its receptor and that of angiotensin II and the angiotensin AT1 receptor provide clues about the physiological functions of this novel signal-transduction system. Now, roles have been established for the apelin system in lowering blood pressure, as a potent cardiac inotrope, in modulating pituitary hormone release and food and water intake, in stress activation, and as a novel adipokine that is excreted from fat cells and regulates insulin. Given its broad array of physiological roles, apelin has attracted much interest as a target for novel therapeutic research and drug design.

Publication types

  • Review

MeSH terms

  • Adipocytes / drug effects*
  • Adipocytes / metabolism
  • Adipokines
  • Animals
  • Anti-Obesity Agents / pharmacology*
  • Apelin
  • Apelin Receptors
  • Blood Pressure / drug effects*
  • Cardiac Output, Low / drug therapy
  • Cardiac Output, Low / physiopathology
  • Cardiotonic Agents / pharmacology*
  • Carrier Proteins / metabolism
  • Carrier Proteins / pharmacology
  • Cell Line
  • Disease Models, Animal
  • Humans
  • Hypertension / drug therapy
  • Hypertension / physiopathology
  • Insulin / metabolism
  • Intercellular Signaling Peptides and Proteins / pharmacology*
  • Intercellular Signaling Peptides and Proteins / physiology*
  • Obesity / drug therapy
  • Obesity / metabolism
  • Receptors, G-Protein-Coupled / drug effects
  • Receptors, G-Protein-Coupled / metabolism
  • Signal Transduction
  • Vasodilator Agents / pharmacology*


  • APLN protein, human
  • APLNR protein, human
  • Adipokines
  • Anti-Obesity Agents
  • Apelin
  • Apelin Receptors
  • Apln protein, mouse
  • Apln protein, rat
  • Aplnr protein, mouse
  • Aplnr protein, rat
  • Cardiotonic Agents
  • Carrier Proteins
  • Insulin
  • Intercellular Signaling Peptides and Proteins
  • Receptors, G-Protein-Coupled
  • Vasodilator Agents