Tamoxifen

Question 1

Class

Answer 1

Oestrogen receptor

agonist but also angonist on the transcripon factors at the promotor region

Question 2

Clinical use

Answer 2

Breast cancer

Question 3

Adverse effects

Answer 3

Hot flushes
GIT disturbances
Headache
Menstrual
irregularities

Question 4

Actions

Answer 4

Prevents cell activation

and proliferation

Question 5

Mechanism of action

Answer 5

Competes with
endogenous oestrogen for
the oestrogen receptor

Question 6

what is Tamoxifen

Answer 6

A selective estrogen receptor modulator .can have both estogenic and antiestrogenic effects

Question 7

mode of action of Tamoxifen

Answer 7

binding to the estrogen receptor (ER), leading to a conformational change in the receptor and therefore altering the expression of estrogen dependent genes

Question 8

what happens when there is a prolonged binding of Tamoxifen to the nuclear chromatin

Answer 8

reduces DNA polymerase activity, impairs thymidine utilization, blocks estradiol uptake, and decreases estrogen response

Question 9

what can tamoxifen bind to

Answer 9

bind either the ER-a or Erb receptors

Question 10

how can Taxoxifen have estrogenic or antiestrogenic effects

Answer 10

bind either the ER-a or Erb receptors, and most likely will interact with multiple co-repressors, or co-activators leading