PMID: 15379634Sep 24, 2004Paper

Estrogen receptors as targets for drug development for breast cancer, osteoporosis and cardiovascular diseases

Current Cancer Drug Targets
Thresia ThomasT J Thomas

Abstract

Estrogen receptors (ERs) are proteins that mediate the action of estradiol and a series of natural and synthetic chemicals that mimic the estradiol structure. Estrogenic action was initially attributed to a single type of ER, now known as ERalpha, but ERbeta was discovered in 1995. Tissue specific distribution and the intensity of expression of these proteins determine the first response of tissues to estrogenic compounds. Estrogens and ERs play a major role in the origin and progression of breast cancer, and antiestrogens that block ER function are useful for breast cancer prevention and treatment. Estrogen mimetics, however, do not fall into distinct categories of agonists and antagonists, since their action is regulated by tissue-specific expression of a number of auxiliary proteins called coactivators or corepressors. In addition, small molecules such as polyamines, fattyacids, and thioredoxin may modulate ER function. Estrogenic functions encompass multiple organ systems, including the reproductive, skeletal, cardiovascular, and nervous system. Estrogens are critical for bone remodeling and mineralization so that estrogen replacement therapy is proven to strengthen bone health in post-menopausal women. Ideally, selective b...Continue Reading

Citations

Apr 28, 2007·Biochemistry and Cell Biology = Biochimie Et Biologie Cellulaire·Veena VijayanathanThresia Thomas
Apr 1, 2014·Journal of Pharmaceutical and Biomedical Analysis·P BourassaH A Tajmir-Riahi
Jul 1, 2006·Expert Opinion on Drug Discovery·Eric R ProssnitzTudor I Oprea
Dec 18, 2007·Frontiers in Neuroendocrinology·Nandini Vasudevan, Donald W Pfaff
Aug 29, 2006·The American Journal of Pathology·Domenico AlvaroEugenio Gaudio
Jun 13, 2006·The International Journal of Biochemistry & Cell Biology·Veena VijayanathanThresia Thomas
Sep 30, 2014·International Journal of Biological Macromolecules·P BourassaH A Tajmir-Riahi
Sep 30, 2016·Amino Acids·Enzo Agostinelli
Aug 9, 2005·Cancer Letters·Filippo Acconcia, Rakesh Kumar
Mar 14, 2018·Medical Sciences : Open Access Journal·T J Thomas, Thresia Thomas
Mar 21, 2017·Current Pharmaceutical Design·Rosa Perez-Gregorio, Jesus Simal-Gandara
Oct 5, 2006·Endocrine Reviews·Nandini Vasudevan, Donald W Pfaff
Jun 1, 2010·Toxicological Sciences : an Official Journal of the Society of Toxicology·Leon Earl GrayKevin M Crofton
Oct 3, 2008·Cancer Research·Shali JohnT J Thomas
Sep 9, 2020·European Journal of Medicinal Chemistry·Sudesh Rani, Kamaldeep Paul

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