Copyright
©The Author(s) 2017.
World J Biol Chem. May 26, 2017; 8(2): 138-150
Published online May 26, 2017. doi: 10.4331/wjbc.v8.i2.138
Published online May 26, 2017. doi: 10.4331/wjbc.v8.i2.138
Figure 1 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.
- Citation: Otto-Duessel M, Tew BY, Vonderfecht S, Moore R, Jones JO. Identification of neuron selective androgen receptor inhibitors. World J Biol Chem 2017; 8(2): 138-150
- URL: https://www.wjgnet.com/1949-8454/full/v8/i2/138.htm
- DOI: https://dx.doi.org/10.4331/wjbc.v8.i2.138