Discovery of nonsteroidal androgens

James T. Dalton, Arnab Mukherjee, Zixin Zhu, Leonid Kirkovsky, Duane Miller

Research output: Contribution to journalArticle

168 Citations (Scopus)

Abstract

Nonsteroidal androgens have not been reported. During studies to identify affinity ligands for the androgen receptor in our laboratory, we synthesized several electrophilic nonsteroidal ligands for the androgen receptor and examined their receptor binding affinity and ability to stimulate receptor-mediated transcriptional activation. We found that three of these ligands (1) bound the androgen receptor with affinity similar to that of dihydrotestosterone (the endogenous ligand) and (2) mimicked the effects of dihydrotestosterone on receptor-mediated transcriptional activation (i.e., they were receptor agonists). These studies demonstrate that nonsteroidal ligands can be structurally modified to produce agonist activity. These ligands thus represent the first members of a novel class of androgens with potential therapeutic applications in male fertility and hormone replacement therapy.

Original languageEnglish (US)
Pages (from-to)1-4
Number of pages4
JournalBiochemical and Biophysical Research Communications
Volume244
Issue number1
DOIs
StatePublished - Mar 6 1998

Fingerprint

Androgens
Androgen Receptors
Ligands
Dihydrotestosterone
Transcriptional Activation
Chemical activation
Hormone Replacement Therapy
Fertility
Hormones

All Science Journal Classification (ASJC) codes

  • Biophysics
  • Biochemistry
  • Molecular Biology
  • Cell Biology

Cite this

Discovery of nonsteroidal androgens. / Dalton, James T.; Mukherjee, Arnab; Zhu, Zixin; Kirkovsky, Leonid; Miller, Duane.

In: Biochemical and Biophysical Research Communications, Vol. 244, No. 1, 06.03.1998, p. 1-4.

Research output: Contribution to journalArticle

Dalton, James T. ; Mukherjee, Arnab ; Zhu, Zixin ; Kirkovsky, Leonid ; Miller, Duane. / Discovery of nonsteroidal androgens. In: Biochemical and Biophysical Research Communications. 1998 ; Vol. 244, No. 1. pp. 1-4.
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