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Prostate Cancer
Volume 2011, Article ID 918707, 13 pages
Review Article

New Insights into the Androgen-Targeted Therapies and Epigenetic Therapies in Prostate Cancer

1Department of Pharmaceutical Sciences, Jefferson School of Pharmacy, Thomas Jefferson University, 130 South 9th Street, Edison Building, Suite 1510F, Philadelphia, PA 19107, USA
2Department of Pharmacology and Experimental Therapeutics, University of Maryland and School of Medicine, 685 West Baltimore Street, Baltimore, MD 21201-1559, USA
3Kimmel Cancer Center, Thomas Jefferson University, Philadelphia, PA 19107, USA

Received 22 June 2011; Accepted 27 July 2011

Academic Editor: Fazlul H. Sarkar

Copyright © 2011 Abhijit M. Godbole and Vincent C. O. Njar. This is an open access article distributed under the Creative Commons Attribution License, which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.


Prostate cancer is the most common cancer in men in the United States, and it is the second leading cause of cancer-related death in American men. The androgen receptor (AR), a receptor of nuclear family and a transcription factor, is the most important target in this disease. While most efforts in the clinic are currently directed at lowering levels of androgens that activate AR, resistance to androgen deprivation eventually develops. Most prostate cancer deaths are attributable to this castration-resistant form of prostate cancer (CRPC). Recent work has shed light on the importance of epigenetic events including facilitation of AR signaling by histone-modifying enzymes, posttranslational modifications of AR such as sumoylation. Herein, we provide an overview of the structure of human AR and its key structural domains that can be used as targets to develop novel antiandrogens. We also summarize recent findings about the antiandrogens and the epigenetic factors that modulate the action of AR.