title: Novel concepts in androgen receptor blockade.
abstract: Androgen receptor blockade is a cornerstone of treatment for prostate cancer. Despite castrate levels of testosterone, activation of the androgen receptor remains an important mediator of disease progression in the androgen "independent" state. Thus, maximal blockade of androgen receptor signaling is a continual goal in the management of castration-resistant prostate cancer. In this review we will discuss how various aspects of androgen receptor signaling are being targeted for therapeutic development in castration-resistant prostate cancer. These include direct androgen receptor inhibitors, inhibitors of adrenal androgen synthesis, and a dual 5alpha-reductase isoenzyme inhibitor.
authors.affiliation: The Urologic Oncology Program, UCSF Comprehensive Cancer Center, University of California-San Francisco, San Francisco, CA 94143, USA.
authors.forename: Andrew C
authors.initials: AC
authors.lastname: Hsieh
authors.forename: Charles J
authors.initials: CJ
authors.lastname: Ryan
mesh_terms: D058891:5-alpha Reductase Inhibitors; D000311:Adrenal Glands / Q000187:drug effects / Q000378:metabolism; D000726:Androgen Antagonists / Q000494:pharmacology* / Q000627:therapeutic use*; D059002:Androgen Receptor Antagonists; D000736:Androstenes; D000737:Androstenols / Q000494:pharmacology / Q000627:therapeutic use; D000970:Antineoplastic Agents / Q000494:pharmacology* / Q000627:therapeutic use*; D001378:Azasteroids / Q000494:pharmacology / Q000627:therapeutic use; D000068538:Dutasteride; D004791:Enzyme Inhibitors / Q000494:pharmacology / Q000627:therapeutic use; D006801:Humans; D007654:Ketoconazole / Q000494:pharmacology / Q000627:therapeutic use; D008297:Male; D017430:Prostate-Specific Antigen / Q000097:blood; D011471:Prostatic Neoplasms / Q000188:drug therapy* / Q000276:immunology
chemical_list: D058891:5-alpha Reductase Inhibitors; D000726:Androgen Antagonists; D059002:Androgen Receptor Antagonists; D000736:Androstenes; D000737:Androstenols; D000970:Antineoplastic Agents; D001378:Azasteroids; D004791:Enzyme Inhibitors; D017430:Prostate-Specific Antigen; C089740:abiraterone; D000068538:Dutasteride; D007654:Ketoconazole