A novel high-throughput screening assay is designed to identify inhibitors of the androgen receptor, which plays a critical role in the progression of prostate cancer. The assay could be used to identify new drugs to treat resistant forms of prostate cancer, as described in the peer-reviewed journal ASSAY and Drug Development Technologies.
Approximately 75% of patients with castrate-resistant prostate cancer express androgen receptor variants that lack the ligand binding domain. These forms of disease evade all forms of currently available androgen receptor-targeting treatment. The amino terminal domain (NTD) of the androgen receptor has been shown to be critical for the receptor’s function. Iain McEwan, from the University of Aberdeen, and co-authors developed a cell-based high-throughput assay for screening and identifying inhibitors of the androgen receptor-NTD.
“We demonstrate the suitability of the assay for high-throughput screening platforms and validate two initial hits emerging from a small, targeted, library screen in prostate cancer cells,” state the investigators.
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