Estrogen receptor binding assay

Figure 6.12 Assessment of the chance correlation in DF for ER232, an estrogenic dataset that contains 232 chemicals tested in an estrogen receptor binding assay.

Competitive Estrogen-Receptor Binding Assay Using Rat Uterine Cytosol... 

In our previous studies, DBM showed inhibitory effect on DMBA-induced covalent binding of [ H]DMBA to mammary gland DNA. Therefore, we subsequently evaluated its influence on hormonal mitogenic action toward tumor promotion. Because of the structural similarity between estradiol (Ea) and DBM, a competitive estrogen-receptor binding assay was used in our studies to examine the inhibitory effects of DBM on estradiol-dependent action. 

Estrogen receptor binding assay rat uterine cytosol (ER-RUC) Ex vivo... 

Fig. 7.3. A dot plot (on the left) showing the staining of cells from a human breast tumor for two intracellular proteins. Cytokeratin-positivity marks tumor cells in the suspension, and estrogen receptor positivity on these cells indicates superior prognosis. The plot on the right shows a correlation (in 27 breast tumors) between the intensity of estrogen receptor staining by flow cytometry and the level of estrogen receptor binding (by radioligand binding assay). Modified from Ian Brotherick et al. (1995).

Figure 6.8 Depiction of the recursive process used in our laboratory to develop QSAR models for predicting estrogen receptor binding. The process starts with data from an initial set of chemicals from the literature QSAR modeling. These preliminary QSAR models are used prospectively to define a set of chemicals that will further improve the model s robustness and predictive capability. The new chemicals are assayed, and these data are then used to challenge and refine the QSAR models. Vahdation of the model is critical. The process emphasizes the living model concept.

Akahori Y, Nakai M, Yamasaki K, Takatsuki M, Shimohigashi Y, Ohtaki M (2008) Relationship between the results of in vitro receptor binding assay to human estrogen receptor alpha and in vivo uterotrophic assay comparative study with 65 selected chemicals. Toxicol In Vitro 22(1) 225-231... 

In assay sytems, many of these phytoestrogens are able to bind more avidly to the estrogen receptor than estrogen itself. Why plant products should possess such avid estrogenic compounds is unclear, but it has been suggested that consumption of phytoestrogens by insects may result in alterations in the sex... 

Fig. 6.8 Breakthrough curves for ligands infused through an estrogen receptor p FAC assay. Slow tight-binding ligands (nafoxidine and tamoxifen) exhibit diffuse breakthrough curves, while ligands with rapid kinetics exhibit sharper curves (norethindrone). Dehydroisoandro-sterone, a ligand intermediate between norethindrone and nafoxidine, was undetected in this experiment.

Polybrominated Diphenyl Ethers. Results of in vitro estrogen receptor and thyroid hormone transport protein binding assays and in vivo studies of thyroid hormone homeostasis indicate that PBDEs have the potential to disrupt normal endocrine function. 

Harvey, J. M., Cark, G. M., Osborne, C. K., and Allred, D. C. 1991. Estrogen receptor status by immunohistochemistry is superior to the ligand-binding assay for predicting response to adjuvant endocrine therapy in breast cancer. J. Clin. Oncol. 27 1474-1481. 

Stoessel S, Leclercq G (1986) Competitive binding assay for estrogen receptor in monolayer culture measure of receptor activity potency. J Steroid Biochem 25 677-682... 

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