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. 2023 Oct 20;299(12):105369. doi: 10.1016/j.jbc.2023.105369

Figure 5.

Figure 5

Concentration-response curves of representative hits. Samples are excited at 473 nm or 532 nm, with the 473 nm data plotted as normalized FRET efficiency (E/EDMSO) and the 532 nm data plotted as the change in the acceptor lifetime compared to DMSO (Delta lifetime). To help guide the eye, data were fit to a hill equation when the data exceeded a 10% change from baseline and was not biphasic. Clinofibrate, Enoxaparin sodium, Erlotinib, Lumiracoxib decrease the FLT-FRET between FMAL-actin and TMR-cC0-C2 (donor-acceptor (DA)_cardiac). Fenticonazole nitrate increases FLT-FRET between FMAL-actin and PKA-phosphorylated TMR-cC0-C2 (DA_cardiac_PKA) but does not have any effect on cC0-C2 (DA_cardiac) or fC1-C2 (DA_skeletal). Erthromycin estolate has a biphasic effect on FRET between FMAL-actin and TMR-cC0-C2/PKA-phosphorylated-TMR-cC0-C2/TMR-fC1-C2. Erlotinib increases TMR-cC0-C2 FLT for all samples, and Erthromycin estolate decreases them. Fenticonazole nitrate slightly decreases FLT of TMR-cC0-C2 (acceptor (A)_cardiac) and PKA-phosphorylated-TMR-cC0-C2 (A_cardiac_PKA) but does not affect TMR-fC1-C2 (A_skeletal). Data are collected from three independent preparations of actin and TMR-cC0-C2 and TMR-fC1-C2. N = 3, n = 9. The effects on FLT-FRET and FLT values at 60 μM compound concentration are summarized in Table 1, Table 2, Table 3. All values are in average ± SD.