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

Steroids. 1983 May;41(5):617-26. doi: 10.1016/0039-128x(83)90027-2.

Abstract

Our objective was to evaluate a convenient in vitro model for measuring steroid affinities to the human androgen receptor. The ability 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 10 beta-methyl group increased affinity of the androstane compounds for the receptor. The 17 beta-hydroxyl group was also essential for high affinity binding and addition of a 17 alpha-methyl group enhanced binding. Binding of steroids with a delta 4 double bond was consistently less than that of the 5 alpha-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.

Publication types

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

MeSH terms

  • Binding, Competitive
  • Cells, Cultured
  • Dihydrotestosterone / analogs & derivatives
  • Dihydrotestosterone / metabolism*
  • Fibroblasts / metabolism
  • Humans
  • Kinetics
  • Male
  • Receptors, Androgen / metabolism*
  • Receptors, Steroid / metabolism*
  • Skin / metabolism*

Substances

  • Receptors, Androgen
  • Receptors, Steroid
  • Dihydrotestosterone