Estrogen receptors alpha (ERα) and beta (ERβ): subtype-selective ligands and clinical potential

Steroids. 2014 Nov;90:13-29. doi: 10.1016/j.steroids.2014.06.012. Epub 2014 Jun 24.

Abstract

Estrogen receptors alpha (ERα) and beta (ERβ) are nuclear transcription factors that are involved in the regulation of many complex physiological processes in humans. Modulation of these receptors by prospective therapeutic agents is currently being considered for prevention and treatment of a wide variety of pathological conditions, such as, cancer, metabolic and cardiovascular diseases, neurodegeneration, inflammation, and osteoporosis. This review provides an overview and update of compounds that have been recently reported as modulators of ERs, with a particular focus on their potential clinical applications.

Keywords: Agonists; Antagonists; Estrogen receptor subtype α; Estrogen receptor subtype β; Modulators; Therapeutic applications.

Publication types

  • Research Support, N.I.H., Extramural
  • Research Support, Non-U.S. Gov't
  • Review

MeSH terms

  • Estrogen Receptor alpha / agonists
  • Estrogen Receptor alpha / antagonists & inhibitors
  • Estrogen Receptor alpha / metabolism*
  • Estrogen Receptor beta / agonists
  • Estrogen Receptor beta / antagonists & inhibitors
  • Estrogen Receptor beta / metabolism*
  • Estrogens / metabolism*
  • Humans
  • Models, Chemical
  • Selective Estrogen Receptor Modulators / pharmacology

Substances

  • Estrogen Receptor alpha
  • Estrogen Receptor beta
  • Estrogens
  • Selective Estrogen Receptor Modulators