This atomic-level model of part of the human androgen receptor shows the target for a potential drug against prostate cancer. New research has determined the three-dimensional, atom-by atom structure of the target. The drug would bind to the receptor, interrupting its activity which drives the disease.
Scientists have determined the precise molecular structure of a potential new target for treating prostate cancer, a disease driven in part by abnormal testosterone activity. The target is part of the androgen receptor, a protein essential for testosterone to function in human cells. Prostate cancer is the most common cancer among men.
The androgen receptor and testosterone – technically, 5-alpha dihydrotestosterone – each drive prostate cancer at different stages of the disease. A common prostate cancer treatment uses drugs that compete with testosterone, blocking its ability to bind with the androgen receptor and so reducing the hormone’s effect. But cancer tends to become resistant to these drugs. The new research provides a novel strategy to block activation of both the androgen receptor and testosterone.
UCSF scientists determined the atom-by-atom topography of the pocket where proteins known as coactivators bind to the human androgen receptor to enable testosterone to trigger gene activity. Knowing the detailed shape greatly boosts the likelihood of developing a drug to block this binding and turn off androgen receptor activity, the scientists report.
Wallace Ravven | EurekAlert!
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