Targeting Ligand-Dependent and Ligand-Independent Androgen Receptor Signaling in Prostate Cancer
Technical Report,30 Sep 2014,29 Sep 2015
University of Texas, Southwestern Medical Center at Dallas Dallas United States
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Last year, we made significant progress in testing over a hundred analogues of our lead compound targeting ligand-dependent androgen receptor signaling in Prostate Cancer. We had overcome problems with solubility, off-target effects, toxicity and formulation. However, on rigorous evaluation, we found that we could not be sure that these agents were targeting specifically the interaction between the androgen receptor and coregulators. Towards this end, we developed a novel in vivo FRET assay, that validated the activity of our compounds in blocking the Androgen receptor interaction with specific coregulators.