Activation-inactivation of hormone binding sites of the oestradiol-17 beta receptor is a multiregulated process

J Steroid Biochem. 1986 Jan;24(1):39-43. doi: 10.1016/0022-4731(86)90029-4.

Abstract

The calf uterus oestradiol-17 beta receptor exists in a hormone binding form, which is phosphorylated on tyrosine, and in a non-hormone binding form, which is dephosphorylated. Two enzymes regulate the number of hormone binding sites of the receptor: a kinase which has been purified from cytosol and a phosphatase purified from nuclei. Recent and new findings on the regulation of this activation-inactivation process are reported. In vitro only a fraction (30-60%) of the receptor binding sites are inactivated by the phosphatase. Evidence is given suggesting that this is due to the production during the inactivation process of a powerful inhibitor of the phosphatase. Ca2+-calmodulin stimulates the kinase activity with a parallel increase of phosphorylation on tyrosine and hormone binding sites of the receptor. Nanomolar concentrations of oestradiol-17 beta also stimulate the kinase to activate hormone binding sites. These results suggest that in intact cells inactivation-activation of the oestradiol receptor is a multiregulated process.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Binding Sites
  • Calcium / pharmacology
  • Calmodulin / pharmacology
  • Cattle
  • Estradiol / metabolism*
  • Female
  • In Vitro Techniques
  • Phosphoric Monoester Hydrolases / antagonists & inhibitors
  • Phosphorylation
  • Protein Kinases / analysis
  • Receptors, Estradiol / metabolism*
  • Receptors, Estrogen / metabolism*
  • Tyrosine / metabolism

Substances

  • Calmodulin
  • Receptors, Estradiol
  • Receptors, Estrogen
  • Tyrosine
  • Estradiol
  • Protein Kinases
  • Phosphoric Monoester Hydrolases
  • Calcium