p42/p44 MAP kinase module plays a key role in the transcriptional regulation of the vascular endothelial growth factor gene in fibroblasts

J Biol Chem. 1998 Jul 17;273(29):18165-72. doi: 10.1074/jbc.273.29.18165.

Abstract

Vascular Endothelial Growth Factor (VEGF) is a potent mitogen for vascular endothelial cells that has been implicated in tumor neovascularization. We show that, in hamster fibroblasts (CCL39 cells), VEGF mRNAs are expressed at low levels in serum-deprived or exponentially growing cells, whereas it is rapidly induced after stimulation of quiescent cells with serum. CCL39 derivatives, transformed with Polyoma virus or with active members of the p42/p44 mitogen-activated protein (MAP) kinase pathway, Gly/Val point mutant of Ras at position 12 (Ras-Val12), MKK1 in which Ser218 and Ser222 were mutated to Asp (MKK1-SS/DD)), express very high levels of VEGF mRNA. To analyze the contribution of the p42/p44MAP kinase in this induction, we used the CCL39-derived cell line (Raf-1:ER) expressing an estradiol-activable Raf-1. We show a time and an estradiol dose-dependent up-regulation of VEGF mRNA clearly detectable after 2 h of stimulation. The induction of VEGF mRNA in response to conditioned activation of Raf-1 is reverted by an inhibitor of MKK1, PD 098059, highlighting a specific role for the p42/p44 MAP kinase pathway in VEGF expression. Interestingly, hypoxia has an additive effect on VEGF induction in CCL39 cells stimulated by serum or in Raf-1:ER cells stimulated by estradiol. In contrast to VEGF, the isoforms VEGF-B and VEGF-C are poorly regulated by growth and oncogenic factors. We have identified a GC-rich region of the VEGF promoter between -88 and -66 base pairs which contains all the elements responsible of its up-regulation by constitutive active Ras or MKK1-SS/DD. By mutation of the putative binding sites and electrophoretic mobility supershift experiments, we showed that the GC-rich region constitutively binds Sp1 and AP-2 transcription factors. Furthermore, following activation of the p42/p44 MAP kinase module, the binding of Sp1 and AP-2 is increased in the complexes formed in this region of the promoter. Altogether, these data suggest that hypoxia and p42/p44 MAP kinase independently play a key role in the regulation of the VEGF expression.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Calcium-Calmodulin-Dependent Protein Kinases / metabolism*
  • Cells, Cultured
  • Core Binding Factor Alpha 1 Subunit
  • Cricetinae
  • DNA-Binding Proteins / metabolism
  • Endothelial Growth Factors / genetics*
  • Endothelial Growth Factors / metabolism
  • Fibroblasts / metabolism
  • Gene Expression Regulation
  • Lymphokines / genetics*
  • Mice
  • Mice, Nude
  • Mitogen-Activated Protein Kinase 1 / metabolism*
  • Mitogen-Activated Protein Kinase 3
  • Mitogen-Activated Protein Kinases*
  • Promoter Regions, Genetic
  • Proto-Oncogene Proteins c-raf / genetics
  • Proto-Oncogene Proteins c-raf / metabolism
  • RNA, Messenger / metabolism
  • Sodium-Hydrogen Exchangers / metabolism
  • Sp1 Transcription Factor / metabolism
  • Transcription Factor AP-2
  • Transcription Factors / metabolism
  • Transcription, Genetic*
  • Vascular Endothelial Growth Factor A
  • Vascular Endothelial Growth Factor B
  • Vascular Endothelial Growth Factor C
  • Vascular Endothelial Growth Factors

Substances

  • Core Binding Factor Alpha 1 Subunit
  • DNA-Binding Proteins
  • Endothelial Growth Factors
  • Lymphokines
  • RNA, Messenger
  • Runx2 protein, mouse
  • Sodium-Hydrogen Exchangers
  • Sp1 Transcription Factor
  • Transcription Factor AP-2
  • Transcription Factors
  • Vascular Endothelial Growth Factor A
  • Vascular Endothelial Growth Factor B
  • Vascular Endothelial Growth Factor C
  • Vascular Endothelial Growth Factors
  • growth factor-activatable Na-H exchanger NHE-1
  • Proto-Oncogene Proteins c-raf
  • Calcium-Calmodulin-Dependent Protein Kinases
  • Mitogen-Activated Protein Kinase 1
  • Mitogen-Activated Protein Kinase 3
  • Mitogen-Activated Protein Kinases