Estrogen receptor beta in health and disease.
Estrogens, acting through its two receptors, ESR1 (hereafter designated ER alpha) and ESR2 (hereafter designated ER beta), have diverse physiological effects in the reproductive system, bone, cardiovascular system, hematopoiesis, and central and peripheral nervous systems. Mice with inactivated ER alpha, ER beta, or both show a number of interesting phenotypes, including incompletely differentiated epithelium in tissues under steroidal control (prostate, ovary, mammary, and salivary glands) and defective ovulation reminiscent of polycystic ovarian syndrome in humans (in ER beta-/- mice), and obesity, insulin resistance, and complete infertility (both in male and female ER alpha-/- mice). Estrogen agonists and antagonists are frequently prescribed drugs with indications that include postmenopausal syndrome (agonists) and breast cancer (antagonists). Because the two estrogen receptors (ERs) have different physiological functions and have ligand binding pockets that differ enough to be selective in their ligand binding, opportunities now exist for development of novel ER subtype-specific selective-ER modulators.
Imamov
Otabek
O
Department of Biosciences and Medical Nutrition, Novum, Karolinska Institute, Karolinska University Hospital, Huddinge, SE-141 86 Sweden.
Shim
Gil-Jin
GJ
Warner
Margaret
M
Gustafsson
Jan-Ake
JA
D000818:Animals; D001327:Autoimmune Diseases / Q000209:etiology / Q000378:metabolism*; D047628:Estrogen Receptor alpha; D047629:Estrogen Receptor beta / Q000187:drug effects / Q000502:physiology*; D005260:Female; D006801:Humans; D015464:Leukemia, Myelogenous, Chronic, BCR-ABL Positive / Q000378:metabolism*; D008024:Ligands; D008297:Male; D019636:Neurodegenerative Diseases / Q000188:drug therapy / Q000378:metabolism* / Q000517:prevention & control; D011469:Prostatic Diseases / Q000378:metabolism / Q000473:pathology*
D047628:Estrogen Receptor alpha; D047629:Estrogen Receptor beta; D008024:Ligands