Phosphorylation and nuclear translocation of integrin β4 induced by a chemical small molecule contribute to apoptosis in vascular endothelial cells

Apoptosis. 2013 Sep;18(9):1120-31. doi: 10.1007/s10495-013-0860-4.

Abstract

Integrin β4 and its Y-1494 phosphorylation play an important role in cell signaling. We found a small molecule, ethyl1-(3-(4-chlorophenoxy)-2-hydroxypropyl)-3-(4-chlorophenyl)-1H-pyrazole-5-carboxylate (ECPC), that could elevate the levels of KIT ligand (KITLG), interleukin 8 (IL-8), prostaglandin-endoperoxide synthase 2 (PTGS2) and activating transcription factor 3 (ATF3) and promote apoptosis in vascular endothelial cells (VECs) through integrin β4. We investigated the underlying mechanism of integrin β4 participating in this process. ECPC treatment increased the phosphorylation of Y-1494 in the integrin β4 cytoplasmic domain via a well-known receptor tyrosine kinase, fibroblast growth factor receptor 1 (FGFR1), and integrin β4 translocated from the cytoplasm to nucleus. With suppression of Y-1494 phosphorylation by FGF-2 or siRNA of FGFR1, ECPC failed to promote integrin β4 nuclear translocation and could not increase the expression of KITLG, IL-8, PTGS2 or ATF3. Y-1494 phosphorylation and nuclear translocation of integrin β4 may be important during ECPC-induced apoptosis in VECs.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Activating Transcription Factor 3 / genetics
  • Activating Transcription Factor 3 / metabolism
  • Amino Acid Motifs
  • Apoptosis* / drug effects
  • Cell Nucleus / drug effects
  • Cell Nucleus / genetics
  • Cell Nucleus / metabolism*
  • Cell Survival / drug effects
  • Endothelial Cells / cytology*
  • Endothelial Cells / drug effects
  • Endothelial Cells / metabolism*
  • Fibroblast Growth Factor 2 / metabolism
  • Humans
  • Integrin beta4 / chemistry
  • Integrin beta4 / genetics
  • Integrin beta4 / metabolism*
  • Phosphorylation / drug effects
  • Receptor, Fibroblast Growth Factor, Type 1 / genetics
  • Receptor, Fibroblast Growth Factor, Type 1 / metabolism
  • Small Molecule Libraries / chemical synthesis
  • Small Molecule Libraries / pharmacology*

Substances

  • ATF3 protein, human
  • Activating Transcription Factor 3
  • Integrin beta4
  • Small Molecule Libraries
  • Fibroblast Growth Factor 2
  • Receptor, Fibroblast Growth Factor, Type 1