Application of a mathematical model for two component receptor binding to two high affinity oestrogen binding sites in nuclei from DMBA rat mammary tumours

J Steroid Biochem. 1988 Apr;29(4):375-80. doi: 10.1016/0022-4731(88)90245-2.

Abstract

Saturation binding of [3H]oestradiol has been determined using exchange conditions, on nuclei from DMBA tumours from rats treated prior to sacrifice with oestradiol and tamoxifen alone or in combination. Application of a model to the binding data enabled the amounts (C2) and apparent dissociation constants (Kdapp) of a second lower affinity binding component to be determined as well as the amount of a higher affinity site (C1) and its dissociation constant (Kd1). Kdapp did not change significantly with any pretreatment but 2 h after oestradiol (5 micrograms) and after tamoxifen alone there was a significant decrease in Kd compared with control. It is suggested that the difference in Kd of the higher affinity binding sites in control and 2 h oestradiol treated animals may be due to the loss of an essential co-factor, possibly cytosolic, when nuclei are isolated in the absence of ligand.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • 9,10-Dimethyl-1,2-benzanthracene
  • Animals
  • Binding Sites
  • Cell Nucleus / metabolism
  • Estradiol / metabolism
  • Mammary Neoplasms, Experimental / metabolism*
  • Mathematics
  • Models, Theoretical
  • Rats
  • Receptors, Estrogen / metabolism*
  • Tamoxifen / metabolism

Substances

  • Receptors, Estrogen
  • Tamoxifen
  • Estradiol
  • 9,10-Dimethyl-1,2-benzanthracene