Therapeutic potential of interfering with apelin signalling.
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).
Sorli
S Caroline
SC
IFR31, Unité INSERM U-589, CHU Rangueil, Bât. L3, BP84225, 1 avenue Jean-Poulhès, 31432-Toulouse Cédex 4, France.
van den Berghe
Loïc
L
Masri
Bernard
B
Knibiehler
Bernard
B
Audigier
Yves
Y
D000075244:Apelin Receptors; D015195:Drug Design; D004730:Endothelium, Vascular / Q000187:drug effects / Q000503:physiopathology; D006801:Humans; D009389:Neovascularization, Pathologic / Q000503:physiopathology / Q000517:prevention & control; D043562:Receptors, G-Protein-Coupled / Q000037:antagonists & inhibitors / Q000502:physiology*; D015398:Signal Transduction / Q000187:drug effects / Q000502:physiology*
C104575:APLNR protein, human; D000075244:Apelin Receptors; D043562:Receptors, G-Protein-Coupled