Apelin signalling: a promising pathway from cloning to pharmacology

Cell Signal. 2005 Apr;17(4):415-26. doi: 10.1016/j.cellsig.2004.09.018.


The discovery of new signalling pathways is always followed by the development of pharmacological agents as drugs that can be used in the treatment of diseases resulting from a dysfunction of the signalling pathway in question. Apelin signalling plays a role in the central and peripheral regulation of the cardiovascular system, in water and food intake, and possibly in immune function. Up-regulation of ligand and receptor is also associated with pathophysiological states such as cardiac dysfunction and neovascularisation. Finally, the apelin receptor is a coreceptor for the entry of several HIV-1 and SIV strains. In view of these features, the apelin receptor constitutes a very interesting target for the design of new drugs for treating the prime causes of human mortality.

Publication types

  • Review

MeSH terms

  • Animals
  • Apelin
  • Apelin Receptors
  • Cardiovascular System / metabolism
  • Carrier Proteins / chemistry
  • Carrier Proteins / genetics*
  • Central Nervous System / physiology
  • Cloning, Molecular
  • Drug Design
  • Humans
  • Intercellular Signaling Peptides and Proteins
  • Mice
  • Rats
  • Receptors, G-Protein-Coupled / antagonists & inhibitors
  • Receptors, G-Protein-Coupled / chemistry
  • Receptors, G-Protein-Coupled / genetics*
  • Signal Transduction* / drug effects
  • Structure-Activity Relationship


  • APLN protein, human
  • APLNR protein, human
  • Apelin
  • Apelin Receptors
  • Carrier Proteins
  • Intercellular Signaling Peptides and Proteins
  • Receptors, G-Protein-Coupled