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. Author manuscript; available in PMC: 2020 Jul 17.
Published in final edited form as: J Am Chem Soc. 2019 Jul 8;141(28):11059–11070. doi: 10.1021/jacs.9b02679

Figure 2.

Figure 2.

Indenoisoquinolines can induce and stabilize MycG4. (A) Left: schematic of the FRET-quenching assay used for compound screening. The FRET-quenching (shown as fluorophore in black color) caused by MycG4 folding can be induced by K+ or MycG4-inducing compounds. Right: relative fluorescence intensities of the labeled MycG4 in the presence of DMSO, 100 mM K+, and indenoisoquinoline analogs as shown by FRET-quenching assay. Data shown are the average values of the two individual experiments. DMSO (negative control), 100 mM K+ (positive control), and six indenoisoquinolines used for further studies are highlighted and labeled. Conditions: 1 μM labeled DNA, 10 μM compound, 25 °C, 50 mM Tris·acetate, pH 7. (B) Thermal stabilization values (ΔTm) of MycG4 by indenoisoquinoline analogs as shown by FRET-melting assay. Data shown are the average values of the two individual experiments. The six representative indenoisoquinolines used for further studies are highlighted and labeled. Conditions: 150 nM labeled DNA, 1.5 μM compound, 25 °C, pH 7, 10 mM K+. (C) Correlation of FRET-quenching and FRET-melting data. The Pearson correlation coefficient (r) is shown.