Androgens, mediated by the Androgen Receptor (AR), play a crucial role in prostate cancer. Current treatments are focused on anti-androgenic drugs competing with natural androgens and antagonizing the transcriptional activity of the AR. Although widely used, these drugs have shown significant side effects and in addition, tumors have become resistant suggesting mutations of the receptor. Regulation of gene expression by AR requires the binding to androgens or to its natural ...
Androgens, mediated by the Androgen Receptor (AR), play a crucial role in prostate cancer. Current treatments include antiandrogens competing with natural androgens and antagonize AR transcriptional activity. Although widely used, antiandrogens have shown significant side effects. Regulation of gene expression by AR requires the binding to its natural ligand, dihydrotestosterone (DHT), and assembly of coregulatory proteins (CoR). The blockage of the interaction between DHT-liganded AR and CoR by small molecules ...
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