Estrogen's role in cell growth and proliferation has long been appreciated both in the normal development of secondary sexual characteristics and in diseased states in cancers of the breast, ovaries and uterus. We are beginning to appreciate estrogen's expanded role in maintaining such diverse functions as the skin's elasticity, the health of the central nervous system, bone density and cardiac health. Estrogen plays out its roles in varied tissues by binding to two major ligand activated nuclear receptors, estrogen receptor alpha (ER-a) and estrogen receptor beta (ER-b). The interrelationship of the two receptors plays a role in the responsiveness of certain breast cancers to drug treatment. Though the ligand binding sites of the two receptors differ by only two amino acids, the overall degree of homology between ER-a and ER-b is low. The body uses the receptor selectivity to its advantage by dispersing the receptors in varying ratios to different tissues. Of these actions ER-a is thought to be responsible for the majority with ER-b playing a minor role in all and having more significance in the cardiovascular and skeletal systems. Small molecules have been identified which bind to one or the other receptors with differing binding affinities. These selective estrogen receptor modulators (SERMs) hold the potential to be pharmacologically effective in treating diseases specific to one type of estrogen receptor while not affecting the other. For example, ER-a and ER-b are both present in breast tissue, and the ratio of beta to alpha is being examined as one indicator in determining the likelihood of successful treatment of breast cancer by certain drugs. Here we use changes in the fluorescence polarization to calculate binding affinities for each of several small molecules to ER-a and ER-b.
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