The binding of estrogen and estrogen antagonists to the estrogen receptor

Arch Biochem Biophys. 1992 Aug 1;296(2):583-91. doi: 10.1016/0003-9861(92)90614-3.

Abstract

The model of the estrogen receptor as a dimer of identical, interacting subunits and data obtained by Sasson and Notides (1988, Mol. Endocrinol. 2, 307-312) were used to find the standard free energy changes that describe the binding of estradiol and 4-hydroxytamoxifen to the estrogen receptor. For the binding of estradiol or 4-hydroxytamoxifen to the estrogen receptor the data do not deviate systematically from the best fit to the model. The standard free energy change for binding of one molecule of estradiol at one site and one molecule of 4-hydroxytamoxifen at the second site of estrogen receptor indicates that 4-hydroxytamoxifen antagonizes the binding of estradiol to the estrogen receptor.

Publication types

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

MeSH terms

  • Binding, Competitive
  • Estradiol / metabolism*
  • Macromolecular Substances
  • Models, Biological
  • Protein Binding
  • Receptors, Estrogen / chemistry
  • Receptors, Estrogen / metabolism*
  • Tamoxifen / analogs & derivatives*
  • Tamoxifen / metabolism
  • Thermodynamics

Substances

  • Macromolecular Substances
  • Receptors, Estrogen
  • Tamoxifen
  • afimoxifene
  • Estradiol