Estrogen binding

The concept that different ligands play an active role in ER function is apparent at the biochemical level. In addition to competitive inhibition of estrogen binding, antiestrogens induce unique conformations/stiuctures of both ERa and ER 3. This provides a structural basis for the unique biological activities displayed by the different compounds [1]. 

Donohoe, R.M. and Curtis, L.R. (1996). Estrogenic activity of chlordecone, o,p -DDT and o,p -DDE in juvenile rainbow trout Induction of vitellogenesis and interaction with hepatic estrogen binding sites. Aquatic Toxicology 36, 31-52. 

DOC Deoxycorticosterone TEBG Testosterone-estrogen-binding globulin... 

Hutchens, T. W., Gibbons, W. E., Besch, P. K. (1984). High-performance chromatofocusing and size-exclusion chromatography - separation of human uterine estrogen-binding proteins. J. Chromatogr. 297, 283-299. 

PCB diets were associated with reproductive impairment including anovulation, fetal resorption, delayed ovulation, increased gestation, and decreased litter size. Hepatic estrogen binding site concentrations decreased with increasing dietary PCB concentrations but not uterine estrogen receptor sites... 

Garcia T, Lehler S, Bloomer WD, Schachter B (1988) A variant estrogen receptor messenger ribonucleic acid is associated with reduced levels of estrogen binding in human mammary tumors. Mol Endocrinol 2 785... 

Estrogen receptors, in analogy with many other nuclear receptors, fill a double role, since they can be activated by kinase cascades independently of estrogens and of activation of the estrogen binding site by an estrogenic ligand (Fig. 3). 

Starlard-Davenport A, Xiong Y, Bratton S, et al. Phenylalanine(90) and phenyl-alanine(93) are crucial amino acids within the estrogen binding site of the human UDP-glucuronosyltransferase 1A10. Steroids 2007 72(l) 85-94. 

Tong, W.D., Perkins, R., Strelitz, R., Collantes, E.R., Keenan, S., Welsh, W.J., Branham, W.S., and Sheehan, D.M., Quantitative structure-activity relationships (QSARs) for estrogen binding to the estrogen receptor predictions across species, Environ. Health Perspect., 105, 1116-1124, 1997a. 

Because they are hydrophobic molecules, estrogens easily diffuse across cell membranes. When inside a cell, estrogens bind to highly specific, soluble receptor proteins. Estrogen receptors are members of a large family of proteins that act as receptors for a wide range of hydrophobic molecules, including other steroid hormones, thyroid hormones, and retinoids. 

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