The calcium/calmodulin-dependent protein phosphatase calcineurin is the major Elk-1 phosphatase

J Biol Chem. 1997 Nov 21;272(47):29415-8. doi: 10.1074/jbc.272.47.29415.

Abstract

The transcription factor Elk-1 is a component of ternary complex factor and regulates gene expression in response to a wide variety of extracellular stimuli. Phosphorylation of the C-terminal domain of Elk-1, especially at serine 383, is important for its transactivation activity. Recently mitogen-activated protein kinases, such as extracellular signal-regulated kinase, stress-activated protein kinase, and p38 mitogen-activated protein kinase have been demonstrated to be Elk-1 kinases. However, negative regulators of Elk-1, such as protein phosphatases, still remain to be identified. Here we report that COS cell lysates were able to dephosphorylate an extracellular signal-regulated kinase-phosphorylated glutathione S-transferase-Elkc fusion protein, including serine 383. The phosphatase activity was inhibited by cyclosporin A (a calcineurin inhibitor) but not by okadaic acid (a PP1 and PP2A inhibitor). Purified calcineurin also could efficiently dephosphorylate glutathione S-transferase-Elkc in vitro. Pretreatment of COS cells with cyclosporin A significantly enhanced epidermal growth factor-induced serine 383 Elk-1 phosphorylation whereas ionomycin inhibited the Elk-1 phosphorylation. These data provide both in vitro and in vivo evidence that calcineurin is the major Elk-1 phosphatase and plays a critical role in Elk-1 regulation. The identification of calcineurin as the major Elk-1 phosphatase may provide a mechanism for Elk-1 regulation by Ca2+ signals as well as a possible biochemical basis for the neurotoxicity and nephrotoxicity of the immunosuppressant drug cyclosporin A.

Publication types

  • Research Support, U.S. Gov't, P.H.S.

MeSH terms

  • Animals
  • COS Cells
  • Calcineurin / metabolism*
  • Calcineurin Inhibitors
  • Cyclosporine / pharmacology
  • DNA-Binding Proteins / metabolism*
  • Enzyme Inhibitors / pharmacology
  • Epidermal Growth Factor / pharmacology
  • Ionomycin / pharmacology
  • Ionophores / pharmacology
  • Mice
  • Okadaic Acid / pharmacology
  • Phosphorylation / drug effects
  • Proto-Oncogene Proteins / metabolism*
  • Receptor Protein-Tyrosine Kinases / metabolism*
  • Transcription Factors / metabolism*
  • ets-Domain Protein Elk-1

Substances

  • Calcineurin Inhibitors
  • DNA-Binding Proteins
  • Elk1 protein, mouse
  • Enzyme Inhibitors
  • Ionophores
  • Proto-Oncogene Proteins
  • Transcription Factors
  • ets-Domain Protein Elk-1
  • Okadaic Acid
  • Ionomycin
  • Epidermal Growth Factor
  • Cyclosporine
  • Receptor Protein-Tyrosine Kinases
  • Calcineurin