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. 2017 May 26;8(2):138–150. doi: 10.4331/wjbc.v8.i2.138

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©The Author(s) 2017. Published by Baishideng Publishing Group Inc. All rights reserved.

Open-Access: This article is an open-access article which was selected by an in-house editor and fully peer-reviewed by external reviewers. It is distributed in accordance with the Creative Commons Attribution Non Commercial (CC BY-NC 4.0) license, which permits others to distribute, remix, adapt, build upon this work non-commercially, and license their derivative works on different terms, provided the original work is properly cited and the use is non-commercial. See: http://creativecommons.org/licenses/by-nc/4.0/

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Screening for neuron-selective androgen receptor inhibitors. A: AR conformation change can be monitored by the CFP-AR-YFP FRET reporter (top). Screening for compounds that affect AR conformation change in GT1-7 cells was accomplished in 96 well plates; B: Hits were assessed for a dose response in the same assay. Shown is the dose response to NSC285116 (siomycin A); C, D: Hits were then assessed for agonist or antagonist activity in the indicated cell lines in a FRET or an androgen-responsive luciferase reporter assay. Siomycin A demonstrated antagonist activity in GT1-7 neuron cells but not C2C12 muscle cells and was therefore selected for further analysis. AR: Androgen receptor.