Endothelin-1 stimulates c-fos mRNA expression in C6 glioma cells via MAP kinase pathway

Peptides. 1999;20(8):907-14. doi: 10.1016/s0196-9781(99)00080-7.

Abstract

Exposure of C6 glioma cells to endothelin-1 (ET-1) caused dose-dependent (10(-11) M to 10(-7) M) increments in intracellular calcium concentration ([Ca2+]i) and c-fos mRNA expression (4.5-fold) that were abolished by the endothelinA receptor antagonist, BQ610, and by inhibition of phospholipase C with U73122. ET-1 stimulated c-fos mRNA expression was also inhibited by protein kinase C inhibition (chelerythrine) and by the MAP kinase kinase inhibitor PD98059, but not by inhibitors of tyrosine kinases, protein kinase A type I or II, calmodulin kinase II, or calcium channel blockade. C6 cells treated with ET-1 demonstrated a significant increase in MAP kinase activity as evidenced by Western blotting. These results indicate a mechanism of long-term signaling by ET-1 involving an ET(A) receptor-mediated, phospholipase C(beta)-linked pathway that is dependent on protein kinase C and MAP kinase activation.

MeSH terms

  • Alkaloids
  • Benzophenanthridines
  • Calcium-Calmodulin-Dependent Protein Kinases / metabolism*
  • Endothelin-1 / pharmacology*
  • Enzyme Activation
  • Enzyme Inhibitors / pharmacology
  • Estrenes / pharmacology
  • Flavonoids / pharmacology
  • Gene Expression Regulation / drug effects*
  • Genes, fos*
  • Glioma / enzymology
  • Glioma / genetics*
  • Glioma / pathology
  • Oligopeptides / pharmacology
  • Phenanthridines / pharmacology
  • Phosphorylation
  • Pyrrolidinones / pharmacology
  • RNA, Messenger / genetics*
  • Tumor Cells, Cultured

Substances

  • Alkaloids
  • Benzophenanthridines
  • Endothelin-1
  • Enzyme Inhibitors
  • Estrenes
  • Flavonoids
  • Oligopeptides
  • Phenanthridines
  • Pyrrolidinones
  • RNA, Messenger
  • 1-(6-((3-methoxyestra-1,3,5(10)-trien-17-yl)amino)hexyl)-1H-pyrrole-2,5-dione
  • BQ 610
  • chelerythrine
  • Calcium-Calmodulin-Dependent Protein Kinases
  • 2-(2-amino-3-methoxyphenyl)-4H-1-benzopyran-4-one