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

• Estrogens exert both beneficial and negative actions in humans.
• The actions of estrogens are mediated by two receptor subtypes (ERα and ERβ).
• The ligand binding pockets of ERα and ERβ are highly similar.
• The most promising ER-ligands for new clinical uses are ERβ-selective agonists.
• So far, no ERβ-selective agonists have been successfully introduced into the clinic.

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.

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