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.

Fig. 1

Steroids derivatives.

Fig. 2

Benzopyran derivatives 16–22.

Fig. 3

Cyclohexylphenol 23, cyclopentylene 24, and diphenylmethane derivative 25.

Fig. 4

Structure of ERB-041 26, KB9520 27 and chloroindazole 28.

Fig. 5

Separate enantiomers of DPN.

Fig. 6

Tetrahydrofluorenone derivatives.

Fig. 7

β-LGND1 and β-LNGD2 compounds.

Fig. 8

Schiff base derivatives: oximes (36–39) and imines (40–41).

Fig. 9

Carborane derivatives.

Fig. 10

Phytoestrogen compounds 44–53.

Fig. 11

ERβ selective ligands useful for PET studies.