estrogen receptor (ER). You are evaluating the pharmacological
properties of Raloxifene and comparing them to
Estradiol.
The human estrogen receptor has two different isoforms,
alpha and beta. To understand the effect of Raloxifene and
Estradiol and their selectivity, you quantify the expression of a
reporter gene selective to either ER or ER using a luminescence
assay (Figures 1 and 2).
- This Question Relates To The Biological Activity Of The Estrogen Receptor Er You Are Evaluating The Pharmacological P 1 (118.96 KiB) Viewed 12 times
- This Question Relates To The Biological Activity Of The Estrogen Receptor Er You Are Evaluating The Pharmacological P 2 (119.67 KiB) Viewed 12 times
raloxifene on ER or ER. already
answered
b) Explain the pharmacological effect of estradiol and
raloxifene on ER or ER. already
answered
- This Question Relates To The Biological Activity Of The Estrogen Receptor Er You Are Evaluating The Pharmacological P 3 (108.27 KiB) Viewed 12 times
then studied. For this purpose, the reporter gene expression was
monitored in cells treated with 0.5nM estradiol and with increasing
concentrations of Raloxifene (Figure 3).
- This Question Relates To The Biological Activity Of The Estrogen Receptor Er You Are Evaluating The Pharmacological P 4 (276.09 KiB) Viewed 12 times
mediated reporter gene expression of cells treated with 0.5nM
estradiol and increasing concentrations of Raloxifene
d) With reference to the data represented in Figures 1-3, how
does the data for both estradiol and raloxifene relate to the known
biological activity of the estrogen receptor ( 100 words
min)
The tissue distribution of ER or ER is not uniform, with
high ER/ER ratios in breast cancer cells, and low ER/ER ratios
found in bone cells. Overactivation of ER receptors in the breast
may lead to the development of tumours, while their activation of
bone cells has been found to prevent osteoporosis.
e) Reflecting on the experimental data and the known ER/ER
ratios in different tissue, what are the benefits of the
prescription of raloxifene or estradiol analogues for the treatment
of osteoporosis? (100 words min )
please could you help answer d and e
Thank you
180 160 alpha beta 140 120 100 Gene expression (LU) 80 60 40 20 0 1e-11 1e-10 TTTTT 1e-09 1e-08 Estradiol concentration (M) 1e-07 1e-06
30 • alpha beta 25 20 Gene expression (LU) 15 10 5 0 MT 1e-07 MT 1e-06 1e-11 1e-10 1e-09 1e-08 Raloxifene concentration (M)
DATE ER EC5o For ER alpha is 1e-09. Emax for alpha 160 LU b) estrogen is increasing the level of both ER alpha and ER beta the tissue. but , Raloxifene is increasing only only ERalpha but not the expoession of Er beta. c) Estogen Theive appooximately equal selectivity for ER alpha and But rcloxifene is highly selective for Erbete only. Erbeta
140 • alpha beta 120 100 Gene expression (LU) 80 60 40 20 TIMIT 1e-06 1e-11 1e-10 1e-09 1e-08 1e-07 Raloxifene concentration (M)