关键词：前列腺癌；雄激素；细胞（生物学）；临床医学
摘 要：The goal of this research is to verify the specificity of the inhibition of AR-p52 interaction by small molecule AR/p52 inhibitors (selected from prior high throughput screen) in cell culture and AR/p52 activity assays, and determine the efficacy of the compounds against castration resistant prostate cancer cell / xenograft growth. Data from this research will establish the AR-p52 interaction as a viable new target for preventing progression to castration resistant prostate cancer (PCa) and identify lead compound(s) to be further developed for preclinical toxicity testing and clinical trials for PCa that fall beyond the scope of this proposal. During the first year of the research a lead compound has been established with evidence of specificity for AR-p52 interaction and significant inhibition of both castration resistant and androgen-dependent PCa cell growth, and preliminary evidence of efficacy of the lead compound administered at MTD oral regimen against a castration resistant PCa xenograft model.