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. Click here to read the article now.
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 coauthors, 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.
“McEwan and coworkers endeavor to address a clear, unmet medical need in prostate cancer. The impact on translation of new chemical hits and drug repurposing and repositioning for this type of prostate cancer will be quite high, highlighting the importance of new assay development,” says ASSAY and Drug Development Technologies Editor-in-Chief Bruce Melancon, PhD, Director of Medicinal Chemistry at the Warren Center for Neuroscience Drug Discovery at Vanderbilt University.
About the Journal
ASSAY and Drug Development Technologies is an authoritative peer-reviewed journal published 10 times a year online with open access options and in print. Led by Editor-in-Chief Bruce Melancon, PhD, Director of Medicinal Chemistry at the Warren Center for Neuroscience Drug Discovery at Vanderbilt University, the Journal provides early-stage screening techniques and tools that enable identification and optimization of novel targets and lead compounds for new drug development. Complete tables of content and a sample issue may be viewed on the ASSAY and Drug Development Technologies website.
About the Publisher
Mary Ann Liebert, Inc., publishers is known for establishing authoritative peer-reviewed journals in many promising areas of science and biomedical research. Its biotechnology trade magazine, GEN (Genetic Engineering & Biotechnology News), was the first in its field and is today the industry’s most widely read publication worldwide. A complete list of the firm’s more than 100 journals, books, and newsmagazines is on the Mary Ann Liebert, Inc., publishers website.
Assay and Drug Development Technologies
Method of Research
Subject of Research
Development of a High-Throughput Screening Assay for Small-Molecule Inhibitors of Androgen Receptor Splice Variants