Figure 5
From: KRAS oncogene repression in colon cancer cell lines by G-quadruplex binding indolo[3,2-c]quinolines
KRAS promoter activity is decreased following exposure of HEK293T cells lines to equitoxic (IC50) concentrations of compounds TMPyP4, 2d, 3d and 3e.
Cells were co-transfected with pGL3-basic vector (empty vector control), or with KRAS promoter luciferase reporter construct PGL-Ras0.5, or PGL-Ras2.0, together with pRL-TK. Twenty-four h later, cells were replated in 96 wells plates, at 5000 cells per well. Subsequently, 24 h after replating, cells were exposed to IC50 equitoxic concentration of test compounds IQcs and TMPyP4 and vehicle (DMSO). KRAS promoter activity levels were evaluated by Dual-Luciferase assay 72 h after compound exposure. Results are expressed as the luciferase signal ratio of pGL-Ras2.0 or pGL-Ras0.5 to pGL3-basic vector transfected cells, after normalization with Renilla Luciferase. The results are expressed as the mean ± SEM fold-change compared to DMSO exposure, from three independent experiments. *p < 0.05 and § p < 0.01 from DMSO vehicle control.
