Binding activity of indicated
concentrations of BODIPY FL vindoline
(20) in the TR-FRET assay after 30 min of incubation
with 5 nM Tb-anti-GST and other indicated assay components. (A) Interaction
of BODIPY FL vindoline (20) with 5 nM GST-hPXR-LBD and
5 nM Tb-anti-GST in the presence of either DMSO or TO901317 (1, 10 μM); interaction of BODIPY FL vindoline (20) with 5 nM Tb-anti-GST and DMSO with or without 5 nM GST
(without GST-hPXR-LBD). (B) Signal-to-background ratio of BODIPY FL
vindoline (20) interaction with 5 nM GST-hPXR-LBD and
5 nM Tb-anti-GST, where signal and background are defined as 10 000
× 520 nm/490 nm ratios obtained from DMSO and TO901317 (1, 10 μM), respectively. For each BODIPY FL vindoline
(20) concentration tested in both panels A and B, the
difference between DMSO and TO901317 (1, 10 μM)
was substantial and statistically significant (p <
0.0001).