Formation of a fluorescent glucocorticoid receptor-steroid complex in HTC cell cytosol

J Steroid Biochem. 1985 Sep;23(3):267-73. doi: 10.1016/0022-4731(85)90404-2.

Abstract

An intensely fluorescent rhodamine derivative of dexamethasone (i.e. Dex-C2-Rho) was synthesized. Dex-C2-Rho possessed high affinity for HTC cell glucocorticoid receptors in cell-free systems. Whole cell activity and receptor affinity of Dex-C2-Rho were both much lower, apparently due to problems with cell permeability and/or metabolism. A specific, fluorescent receptor-steroid complex at concentrations as low as 1 X 10(-9) M could readily be observed with crude HTC cell receptors after removal of the free Dex-C2-Rho. This appears to be the first report of a fluorescent glucocorticoid receptor-steroid complex.

MeSH terms

  • Animals
  • Binding, Competitive
  • Cell-Free System
  • Culture Techniques
  • Cytosol / metabolism
  • Dexamethasone / analogs & derivatives*
  • Dexamethasone / metabolism
  • Liver Neoplasms, Experimental / metabolism*
  • Rats
  • Receptors, Glucocorticoid / metabolism*
  • Rhodamines / metabolism*
  • Spectrometry, Fluorescence
  • Xanthenes / metabolism*

Substances

  • Receptors, Glucocorticoid
  • Rhodamines
  • Xanthenes
  • Dexamethasone
  • N-(dexamethasone 21-S-ethyl-2'-amino)tetramethylrhodamine