Integration of G-protein coupled receptor signaling pathways for activation of a transcription factor (EGR-3)

Genomics Proteomics Bioinformatics. 2003 Aug;1(3):173-9. doi: 10.1016/s1672-0229(03)01022-2.

Abstract

We recently reported the use of a gene-trapping approach to isolate cell clones in which a reporter gene had integrated into genes modulated by T-cell activation. We have now tested a panel of clones from that report and identified the one that responds to a variety of G-protein coupled receptors (GPCR). The beta-lactamase tagged EGR-3 Jurkat cell was used to dissect specific GPCR signaling in vivo. Three GPCRs were studied, including the chemokine receptor CXCR4 (Gi-coupled) that was endogenously expressed, the platelet activation factor (PAF) receptor (Gq-coupled), and beta2 adrenergic receptor (Gs-coupled) that was both stably transfected. Agonists for each receptor activated transcription of the beta-lactamase tagged EGR-3 gene. Induction of EGR-3 through CXCR4 was blocked by pertussis toxin and PD58059, a specific inhibitor of MEK (MAPK/ERK kinase). Neither of these inhibitors blocked isoproterenol or PAF-mediated activation of EGR-3. Conversely, beta2- and PAF-mediated EGR-3 activation was blocked by the p38, specific inhibitor SB580. In addition, both beta2- and PAF-mediated EGR-3 activation could be synergistically activated by CXCR4 activation. This combined result indicates that EGR-3 can be activated through distinct signal transduction pathways by different GPCRs and that signals can be integrated and amplified to efficiently tune the level of activation.

Publication types

  • Review

MeSH terms

  • Culture Media
  • DNA-Binding Proteins / metabolism*
  • Early Growth Response Protein 3
  • Gene Expression Regulation
  • Genes, Reporter
  • Humans
  • Jurkat Cells
  • MAP Kinase Signaling System
  • Receptors, CXCR4 / metabolism
  • Receptors, G-Protein-Coupled / metabolism*
  • Signal Transduction*
  • Transcription Factors / metabolism*
  • beta-Lactamases / metabolism

Substances

  • Culture Media
  • DNA-Binding Proteins
  • Receptors, CXCR4
  • Receptors, G-Protein-Coupled
  • Transcription Factors
  • Early Growth Response Protein 3
  • beta-Lactamases