The binding of estrogen and estrogen antagonists to the estrogen receptor

Jeffrey P. Bond, Shlomo Sasson, Angelo C. Notides*

*Corresponding author for this work

Research output: Contribution to journalArticlepeer-review

5 Scopus citations

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.

Original languageEnglish
Pages (from-to)583-591
Number of pages9
JournalArchives of Biochemistry and Biophysics
Volume296
Issue number2
DOIs
StatePublished - 1 Aug 1992

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