Characterization of steroid binding specificity of the androgen receptor in human foreskin fibroblasts

G. R. Cunningham, T. J. Lobl, C. Cockrell, T. C. Shao, D. J. Tindall

Research output: Contribution to journalArticle

8 Scopus citations

Abstract

Our objective was to evaluate a convenient in vitro model for measuring steroid affinities to the human androgen receptor. The ability3 of unlabeled analogues of dihydrotestosterone (DHT) to compete with [3H]DHT for binding to the receptor in human fibroblasts was measured and expressed relative to DHT. The C-3 ketone group and the planar configuration of the A and B rings were critical for binding. Absence of the 10β-methyl group increased affinity of the androstane compounds for the receptor. The 17β-hydroxyl group was also essential for high affinity binding and addition of a 17α -methyl group enhanced binding. Binding of steroids with a Δ4 double bond was consistently less than that of the 5α-reduced steroids. This was true of both the androstene and estrene series. We conclude that human foreskin fibroblasts offer a useful model for in vitro studies characterizing the effects of steroid structural modifications on binding to the human androgen receptor.

Original languageEnglish (US)
Pages (from-to)617-626
Number of pages10
JournalSteroids
Volume41
Issue number5
DOIs
StatePublished - May 1983

ASJC Scopus subject areas

  • Biochemistry
  • Molecular Biology
  • Endocrinology
  • Pharmacology
  • Clinical Biochemistry
  • Organic Chemistry

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    Cunningham, G. R., Lobl, T. J., Cockrell, C., Shao, T. C., & Tindall, D. J. (1983). Characterization of steroid binding specificity of the androgen receptor in human foreskin fibroblasts. Steroids, 41(5), 617-626. https://doi.org/10.1016/0039-128X(83)90027-2