Figure 2.
FRET profiles for RyR1 and RyR2 over a range of Hit concentrations. The same FLT-detected FRET readout used in the primary HTS was measured at several Hit concentrations, using RyR1 and RyR2 samples. FRET dose-response of (a) suramin, (b) temsirolimus, (c) chloroxine, and (d) myricetin, measured at 30 nM Ca2+ using skeletal (green tones) and cardiac (red tones) SR membranes, in the presence of 5 mM GSSG (dark tones) or GSH (light tones). FRET efficiency in the presence of compound (E) was normalized to FRET efficiency in the presence of DMSO-only (E0). Data are presented as means ± SEM, n = 4. *P < 0.05 vs. DMSO by 2-sided Student’s unpaired T-test.