Therapeutic activation of endothelial sphingosine-1-phosphate receptor 1 by chaperone-bound S1P suppresses proliferative retinal neovascularization

EMBO Mol Med. 2023 May 8;15(5):e16645. doi: 10.15252/emmm.202216645. Epub 2023 Mar 13.

Abstract

Sphingosine-1-phosphate (S1P), the circulating HDL-bound lipid mediator that acts via S1P receptors (S1PR), is required for normal vascular development. The role of this signaling axis in vascular retinopathies is unclear. Here, we show in a mouse model of oxygen-induced retinopathy (OIR) that endothelial overexpression of S1pr1 suppresses while endothelial knockout of S1pr1 worsens neovascular tuft formation. Furthermore, neovascular tufts are increased in Apom-/- mice which lack HDL-bound S1P while they are suppressed in ApomTG mice which have more circulating HDL-S1P. These results suggest that circulating HDL-S1P activation of endothelial S1PR1 suppresses neovascular pathology in OIR. Additionally, systemic administration of ApoM-Fc-bound S1P or a small-molecule Gi-biased S1PR1 agonist suppressed neovascular tuft formation. Circulating HDL-S1P activation of endothelial S1PR1 may be a key protective mechanism to guard against neovascular retinopathies that occur not only in premature infants but also in diabetic patients and aging people.

Keywords: Sphingosine-1-phosphate (S1P); neovascularization; vascular retinopathy.

Publication types

  • Research Support, N.I.H., Extramural

MeSH terms

  • Animals
  • Lipoproteins, HDL
  • Lysophospholipids
  • Mice
  • Receptors, Lysosphingolipid / agonists
  • Receptors, Lysosphingolipid / genetics
  • Retinal Neovascularization*
  • Sphingosine
  • Sphingosine-1-Phosphate Receptors

Substances

  • Sphingosine-1-Phosphate Receptors
  • sphingosine 1-phosphate
  • Receptors, Lysosphingolipid
  • Lipoproteins, HDL
  • Sphingosine
  • Lysophospholipids