In many breast cancers, ER (alpha) activation by estrogens is generally considered responsible for enhanced proliferation, whereas that is counteracted by the presence of ER (beta),which exerts an antiproliferative effect. Please devise a strategy targeting both receptors for the treatment of this disease. •This question relates to the selectivity of different drugs for the treatment of Ovarian Cancer.The expression of the two Estrogen Receptors subtypes, ERa and ERß, was investigated in twohuman ovarian cancer cell lines, A and B, using Western Blotting of the whole cell fraction (Figure 1).The inhibitory effect on the cellular growth of the natural hormone estradiol (E2) and two different drugs (KB9520 and PPT) was studiedfor both cell lines using a Trypan Blue assay. Figure 2 shows a plot of the inhibition of cell proliferation versus control of the compoundsE2, KB9520 and PPT at increasing concentrations. A full agonist is expected to exert 100% inhibition of the cell proliferation for both celllinesA BERaERBTubulinFigure 1 - Western Blot% inhibition versus control6050403020100-10-20-30-40-50Cell line Aс 0,1 nM1 nM 5 nM 10 nMKB9520 E2 OPPT% inhibition versus control6050403020100-10CCell line B0,1 nM1 nM■KB952010 nM5 nME2 OPPTFigure 2 - Inhibition of cell proliferation for cell lines A and B under treatment with KB9520, E2 or PPT

In breast cancers, the activation of estrogen receptor alpha (ERα) by estrogens is often associated…

In many breast cancers, ER (alpha) activation by estrogens is generally considered responsible for enhanced proliferation, whereas that is counteracted by the presence of ER (beta),which exerts an antiproliferative effect. Please devise a strategy targeting both receptors for the treatment of this disease.

In many breast cancers, ER (alpha) activation by estrogens is generally considered responsible for enhanced proliferation, whereas that is counteracted by the presence of ER (beta),which exerts an antiproliferative effect. Please devise a strategy targeting both receptors for the treatment of this disease.

Biology 2e

2nd Edition

ISBN:9781947172517

Author:Matthew Douglas, Jung Choi, Mary Ann Clark

Publisher:Matthew Douglas, Jung Choi, Mary Ann Clark

Chapter17: Biotechnology And Genomics

Section: Chapter Questions

Problem 3VCQ: Figure 17.15 In 2011, the United States Preventative Services Task Force recommended against using...

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