Moderate GSK-3β inhibition improves neovascular architecture, reduces vascular leakage, and reduces retinal hypoxia in a model of ischemic retinopathy

Angiogenesis. 2010 Sep;13(3):269-77. doi: 10.1007/s10456-010-9184-y. Epub 2010 Sep 1.

Abstract

In ischemic retinopathies, unrelieved hypoxia induces the formation of architecturally abnormal, leaky blood vessels that damage retina and ultimately can cause blindness. Because these newly formed blood vessels are functionally defective, they fail to alleviate underlying hypoxia, resulting in more pathological neovascularization and more damage to retina. With an established model of ischemic retinopathy, we investigated inhibition of glycogen synthase kinase-3β (GSK-3β) as a means for improving the architecture and functionality of pathological blood vessels in retina. In vitro, hypoxia increased GSK-3β activity in retinal endothelial cells, reduced β-catenin, and correspondingly impaired integrity of cell/cell junctions. Conversely, GSK-3β inhibitors restored β-catenin, improved cell/cell junctions, and enhanced the formation of capillary cords in three-dimensional collagen matrix. In vivo, GSK-3β inhibitors, at appropriately moderate doses, strongly reduced abnormal vascular tufts, reduced abnormal vascular leakage, and improved vascular coverage and perfusion during the proliferative phase of ischemia-driven retinal neovascularization. Most importantly, these improvements in neovasculature were accompanied by marked reduction in retinal hypoxia, relative to controls. Thus, GSK-3β inhibitors offer a promising strategy for alleviating retinal hypoxia by correcting key vascular defects typically associated with ischemia-driven neovascularization.

Publication types

  • Research Support, N.I.H., Extramural
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Disease Models, Animal
  • Endothelial Cells / drug effects
  • Endothelial Cells / enzymology
  • Endothelial Cells / pathology
  • Glycogen Synthase Kinase 3 / antagonists & inhibitors*
  • Glycogen Synthase Kinase 3 / metabolism
  • Glycogen Synthase Kinase 3 beta
  • Humans
  • Hypoxia / complications
  • Hypoxia / drug therapy*
  • Hypoxia / pathology
  • Intercellular Junctions / drug effects
  • Intercellular Junctions / metabolism
  • Ischemia / complications
  • Ischemia / drug therapy*
  • Ischemia / pathology
  • Mice
  • Mice, Inbred C57BL
  • Morphogenesis / drug effects
  • Protein Kinase Inhibitors / pharmacology
  • Protein Kinase Inhibitors / therapeutic use*
  • Regional Blood Flow
  • Retina / drug effects
  • Retina / enzymology
  • Retina / metabolism
  • Retina / pathology*
  • Retinal Neovascularization / complications
  • Retinal Neovascularization / drug therapy*
  • Retinal Neovascularization / enzymology
  • Retinal Neovascularization / pathology
  • Vascular Diseases / complications
  • Vascular Diseases / drug therapy*
  • Vascular Diseases / pathology
  • beta Catenin / metabolism

Substances

  • Protein Kinase Inhibitors
  • beta Catenin
  • GSK3B protein, human
  • Glycogen Synthase Kinase 3 beta
  • Gsk3b protein, mouse
  • Glycogen Synthase Kinase 3