Testosterone-estradiol binding globulin binds to 2-methoxyestradiol with greater affinity than to testosterone

James F. Dunn, George R. Merriam, Charles Eil, Shinzo Kono, D. Lynn Loriaux, Bruce C. Nisula

Research output: Contribution to journalArticlepeer-review

54 Scopus citations


This report describes the unexpected observation that testosterone-estradiol binding globulin (TeBG) binds 2-methoxyestradiol better than it binds either testosterone or 17β-estradiol. As determined by competitive displacement of3H-testosterone from TeBG adsorbed onto a solid phase matrix of Con A-Sepharose, the relative binding activities of 2-methoxyestradiol, testosterone and 17β-estradiol for TeBG were 2.0, 1.0 and 0.32, respectively. In contrast, 2-methoxyestradiol, which is known to bind with low affinity to estrogen receptors, had only low affinity binding to the androgen receptor, as determined by competitive displacement of3H-dihydrotestosterone using 64-24 rat mammary tumor cells. 2-Methoxyestradiol is the first example of a naturally occurring steroid which binds with high affinity to TeBG but with low affinity to both androgen and estrogen receptors.

Original languageEnglish (US)
Pages (from-to)404-406
Number of pages3
JournalJournal of Clinical Endocrinology and Metabolism
Issue number2
StatePublished - Aug 1980
Externally publishedYes

ASJC Scopus subject areas

  • Endocrinology, Diabetes and Metabolism
  • Biochemistry
  • Endocrinology
  • Clinical Biochemistry
  • Biochemistry, medical


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