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Estrogen receptor competitive binding

Fulvestrant is an estrogen receptor competitive antagonist that binds to the estrogen receptor with comparable affinity to that of estradiol. Fulvestrant downregulates the estrogen receptor in human breast cancer cells. It is marketed for treatment of hormone-dependent breast cancer (Figure 8.76). °... [Pg.328]

B. RU 486 acts as a competitive progesterone antagonist and blocks progesterone binding at its receptors. It has no activity at estrogenic receptors. [Pg.714]

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... [Pg.113]

BPA, at levels greater than 2pgH, was found to be estrogenic in cultured human mammary cancer cells (MCF-7). Some of the reported effects of BPA in MCF-7 cells include induction of progesterone receptors in MCF-7 cells at a potency of 5000 times less than 17-/i-estradiol, increased rate of cell proliferation, and competition with estradiol for estrogen receptor binding sites. [Pg.316]

Tamoxifen competitively blocks estradiol binding to the estrogen receptor. [Pg.2525]

Estrogen Receptor (ER) competitive binding assays, which measures the binding affinity of a chemical for the estrogen receptor (Fang et al., 2000). [Pg.372]

Nonsteroidal estrogen receptor antagonist competitively binds to estrogen receptors on estrogen-dependent breast cells... [Pg.2313]

This congener did not competitively bind in vitro to recombinant human estrogen receptors a and... [Pg.404]

Fulvestrant is an antiestrogen. Fulvestrant competitively binds to the estrogen receptor and downregulates me estrogen receptor protein in human breast cancer cells. It is indicated in the treatment of hormone receptor-positive metastatic breast cancer in postmenopausal women wim disease progression following antiestrogen merapy. [Pg.287]

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Binding competition

Estrogen receptor

Estrogen receptor binding

Estrogen receptor competitive binding assays

Estrogens binding

Receptor binding

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