Subcellular localization of coagulation factor II receptor-like 1 in neurons governs angiogenesis

Nat Med. 2014 Oct;20(10):1165-73. doi: 10.1038/nm.3669. Epub 2014 Sep 14.

Abstract

Neurons have an important role in retinal vascular development. Here we show that the G protein-coupled receptor (GPCR) coagulation factor II receptor-like 1 (F2rl1, previously known as Par2) is abundant in retinal ganglion cells and is associated with new blood vessel formation during retinal development and in ischemic retinopathy. After stimulation, F2rl1 in retinal ganglion cells translocates from the plasma membrane to the cell nucleus using a microtubule-dependent shuttle that requires sorting nexin 11 (Snx11). At the nucleus, F2rl1 facilitates recruitment of the transcription factor Sp1 to trigger Vegfa expression and, in turn, neovascularization. In contrast, classical plasma membrane activation of F2rl1 leads to the expression of distinct genes, including Ang1, that are involved in vessel maturation. Mutant versions of F2rl1 that prevent nuclear relocalization but not plasma membrane activation interfere with Vegfa but not Ang1 expression. Complementary angiogenic factors are therefore regulated by the subcellular localization of a receptor (F2rl1) that governs angiogenesis. These findings may have implications for the selectivity of drug actions based on the subcellular distribution of their targets.

Publication types

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

MeSH terms

  • Active Transport, Cell Nucleus
  • Angiopoietin-1 / genetics
  • Angiopoietin-1 / metabolism
  • Animals
  • HEK293 Cells
  • Humans
  • Mice
  • Mice, Inbred C57BL
  • Mice, Knockout
  • Microtubules / metabolism
  • Mutant Proteins / genetics
  • Mutant Proteins / metabolism
  • Neovascularization, Pathologic
  • Neovascularization, Physiologic* / genetics
  • Neurons / metabolism*
  • Promoter Regions, Genetic
  • Receptor, PAR-2 / deficiency
  • Receptor, PAR-2 / genetics
  • Receptor, PAR-2 / metabolism*
  • Retinal Ganglion Cells / metabolism
  • Retinal Vessels / growth & development
  • Retinal Vessels / metabolism
  • Sorting Nexins / metabolism
  • Sp1 Transcription Factor / metabolism
  • Subcellular Fractions / metabolism
  • Vascular Endothelial Growth Factor A / genetics
  • Vascular Endothelial Growth Factor A / metabolism

Substances

  • Angiopoietin-1
  • Angpt1 protein, mouse
  • Mutant Proteins
  • Receptor, PAR-2
  • Sorting Nexins
  • Sp1 Transcription Factor
  • Vascular Endothelial Growth Factor A
  • vascular endothelial growth factor A, mouse