The action of Tamoxife is mediated by its binding to the estrogen receptors and

Question

The action of Tamoxife is mediated by its binding to the estrogen receptors and then it blocks the effect of estrogen on mammary epithelium. Tamoxifen is a nonsteroidal agent that binds to estrogen receptors, inducing a conformational change in the receptor. This results in a blockage or change in the expression of estrogen dependent genes. The prolonged binding of tamoxifen to the nuclear chromatin of these results in reduced DNA polymerase activity, impaired thymidine utilization, blockade of estradiol uptake, and decreased estrogen response. It is likely that tamoxifen interacts with other coactivators or corepressors in the tissue and binds with different estrogen receptors, ER-alpha or ER-beta, producing both estrogenic and antiestrogenic effects.

Explanation / Answer

[35 Marks] Q 2(a) Discuss in detail, with the aid of the scheme below, the mode of action of the anticancer prodrug, tamoxifen. CH3 CH 20% HO tamoxifen 4-hydroxytamoxifen

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