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Sex Hormones (Male): Analogs and Antagonists


  1. Robert W. Brueggemeier

Published Online: 15 SEP 2006

DOI: 10.1002/3527600906.mcb.200500066

Reviews in Cell Biology and Molecular Medicine

Reviews in Cell Biology and Molecular Medicine

How to Cite

Brueggemeier, R. W. 2006. Sex Hormones (Male): Analogs and Antagonists. Reviews in Cell Biology and Molecular Medicine. .

Author Information

  1. The Ohio State University, Columbus, OH, USA

Publication History

  1. Published Online: 15 SEP 2006

This is not the most recent version of the article. View current version (5 OCT 2015)


The steroid testosterone is the major circulating sex hormone of the male and serves as the prototype for the androgens, the anabolic agents, and androgen antagonists. The endogenous androgens are biosynthesized from cholesterol in various tissues in the body; the majority of the circulating androgens are made in the testes under the stimulation of the gonadotropin LH. The reduction of testosterone to dihydrotestosterone is necessary for the androgenic actions of testosterone in androgen target tissues such as the prostate; the oxidation of testosterone by the enzyme aromatase produces estrogens. The androgenic actions of testosterone are due to the binding of dihydrotestosterone to its nuclear receptor, followed by dimerization of the receptor complex and binding to a specific DNA sequence. This binding of the homodimer to the androgen response element leads to gene expression, stimulation of the synthesis of new mRNA, and subsequent protein biosynthesis. The synthetic androgens and anabolics were prepared to impart oral activity to the androgen molecule, to separate the androgenic effects of testosterone from its anabolic effects and to improve upon its biological activities. Drug preparations are used for the treatment of various androgen-deficient diseases, for the therapy of diseases characterized by muscle wasting and protein catabolism, for postoperative adjuvant therapy, and for the treatment of certain hormone-dependent cancers. The two major categories of androgen antagonists are the antiandrogens, which block interactions of androgens with the androgen receptor, and the inhibitors of androgen biosynthesis and metabolism. Such compounds have therapeutic potential in the treatment of acne, virilization in women, hyperplasia and neoplasia of the prostate, and baldness, and for male contraception.


  • Anabolics;
  • Androgens;
  • Antiandrogens;
  • Dihydrotestosterone;
  • 5α-Reductase Inhibitors;
  • Selective Androgen Receptor Modulators;
  • Testosterone