Androgen receptor antagonists steroidal

Snyder BW, Winneker RC, Batzold FH. Endocrine profile of Win 49596 in the rat a novel androgen receptor antagonist. J Steroid Biochem 1989 33 1127-1132. 

The mechanisms of action of steroid hormones on lymphoid, mammary, and prostatic cancer have been partially clarified. Specific cell surface receptors have been identified for estrogen, progesterone, corticosteroids, and androgens in neoplastic cells in these tissues. As in normal cells, steroid hormones also form an intracellular steroid-receptor complex that ultimately binds directly to nuclear proteins associated with DNA to activate transcription of a broad range of cellular genes involved in cell growth and proliferation (see Chapter 39 Adrenocorticosteroids Adrenocortical Antagonists). 

Steroid hormone receptors (for gonadal steroids and adrenocortical steroids) are complex proteins inside the target cell. The steroid penetrates, is bound and translocates into the cell nucleus, which is the principal site of action and where RNA/protein synthesis occurs. Compounds that occupy the receptor without causing translocation into the nucleus or the replenishment of receptors act as antagonists, e.g. spironolactone to aldosterone, cyproterone to androgens, clomiphene to oestrogens. 

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