Therapeutic potential of interfering with apelin signalling

Drug Discov Today. 2006 Dec;11(23-24):1100-6. doi: 10.1016/j.drudis.2006.10.011. Epub 2006 Nov 2.


The apelin receptor is a G protein-coupled receptor activated by several apelin fragments. Its tissue distribution suggests that apelin signalling is involved in a broad range of physiological functions. Endothelial cells, which express high levels of apelin receptors, respond to apelin through the phosphorylation of key intracellular effectors associated with cell proliferation and migration. In addition, apelin is a mitogen for endothelial cells and exhibits angiogenic properties in matrigel experiments. This review focuses on the therapeutic potential of apelin signalling, which is associated with pathologies that result from decreased vascularisation (ischemias) or neovascularisation (retinopathies and solid tumors).

Publication types

  • Research Support, Non-U.S. Gov't
  • Review

MeSH terms

  • Apelin Receptors
  • Drug Design
  • Endothelium, Vascular / drug effects
  • Endothelium, Vascular / physiopathology
  • Humans
  • Neovascularization, Pathologic / physiopathology
  • Neovascularization, Pathologic / prevention & control
  • Receptors, G-Protein-Coupled / antagonists & inhibitors
  • Receptors, G-Protein-Coupled / physiology*
  • Signal Transduction / drug effects
  • Signal Transduction / physiology*


  • APLNR protein, human
  • Apelin Receptors
  • Receptors, G-Protein-Coupled