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

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.