(a) Overview of the workflow employed to identify FOXO3 inhibitors. (b) Interactions between FOXO3-DBD and the 13 bp DNA strand were represented as pharmacophore features. DNA is shown as sticks and …
FPAs were performed with 125 nM FOXO3-DBD and 25 nM FAM-labeled IRE-oligonucleotide as described in Materials and methods. Compound concentration was 1 μM. mP value of freely rotating IRE-FAM …
Recombinant FOXO1-DBD (159 - 272) FOXO4-DBD (82-207) and FOXO6-DBD (87 - 200) were prepared as described for FOXO3-DBD in Materials and methods. FPAs to measure binding of FAM-labeled IRE …
(a) 1D 1H STD-NMR experiments for S9OX compound in the presence of the 15 µM FOXO3-DBD. The reference spectrum of S9OX is shown in black, the corresponding STD-NMR spectrum is shown in red. …
(a) 1D 1 H STD-NMR experiments for S9 compound in the presence of the 15 µM FOXO3-DBD. The reference spectrum of S9 is shown in black, the corresponding STD-NMR spectrum is shown in red. Chemically …
The comparison of chemical shift perturbation (CSP) obtained for 100 μM FOXO1- DBD (red), FOXO3-DBD (blue) and FOXO4-DBD (yellow) in the presence of 3 mM S9OX. Lines indicate changes greater than …
(a) Heatmaps of Affymetrix microarray analyses (U133 plus 2.0 expression profiling chips). Total RNA was prepared of SH-EP/FOXO3 cells treated with 100 nM 4OHT alone or in combination with 50 µM S9 …
SH-EP/FOXO3 cells were treated for eight hours (a,b) or 24 hr (c,d) with 100 nM 4OHT alone or in combination with 50 µM S9 or S9OX. Cell lysates were subjected to immunoblot analyses using …
SH-EP cells expressing a conditionally activated FOXO3(A3)-ERtm-H212R mutant or FOXO(A3)-ERtm were analyzed by immunoblot, treated with 20 nM 4OHT with or without 50 µM S9 or S9OX and subjected to …
SH-EP/FOXO3 cells were treated either for four hours with 100 nM 4OHT (a) or for two hours with 20 µg/ml etoposide (b). 50 µM S9 or S9OX were pre-incubated for 15 min. ROS accumulation was analyzed …
Synthesis of S9 and S9OX.
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