Androgen receptor as a therapeutic target

Adv Drug Deliv Rev. 2010 Oct 30;62(13):1277-84. doi: 10.1016/j.addr.2010.08.002. Epub 2010 Aug 12.


Androgens function as sex hormone primarily via activation of a single androgen receptor (AR, or NR3C4). AR is an important therapeutic target for the treatment of diseases such as hypogonadism and prostate cancer. AR ligands of different chemical structures and/or pharmacological properties are widely used for these therapeutic applications, and all of the AR ligands currently available for therapy modulate AR function via direct binding to the ligand-binding pocket (LBP) of the receptor. In the past ten years, our understanding of AR structure and molecular mechanism of action has progressed extensively, which has encouraged the rapid development of newer generation of AR ligands, particularly tissue-selective AR ligands. With improved tissue selectivity, future generations of AR ligands are expected to greatly expand the therapeutic applications of this class of drugs. This review will provide an overview of the common therapeutic applications of currently available AR ligands, and discussion of the major challenges as well as novel therapeutic strategies proposed for future drug development.

Publication types

  • Review

MeSH terms

  • Androgen Receptor Antagonists / metabolism*
  • Androgen Receptor Antagonists / therapeutic use*
  • Androgens / metabolism
  • Humans
  • Ligands
  • Male
  • Molecular Targeted Therapy*
  • Prostatic Neoplasms / drug therapy*
  • Prostatic Neoplasms / metabolism
  • Receptors, Androgen / metabolism*
  • Structure-Activity Relationship


  • Androgen Receptor Antagonists
  • Androgens
  • Ligands
  • Receptors, Androgen