Androgen receptor has been shown to promote prostate cell growth and carcinogenesis of prostate cancer by
up-regulating its target genes. Testosterone and dihydrotestosterone are two major hormones which bind to and activate
androgen receptor. Targeting both the androgen receptor and the enzymes catalyzing the biosynthesis of testosterone and
dihydrotestosterone has been shown to be clinically beneficial in the treatment of prostate cancer. Prostate cancer can
become castration-resistant after long term treatment with chemo drugs, so efforts in finding compounds with improved
efficiency to castration-resistant prostate cancer are urgently needed. In this review we summarized the studies on recent
progress in the development of small molecular AR antagonists for the treatment of prostate cancer.
Keywords: Androgen receptor, castration-resistant prostate cancer, prostate cancer.
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