Supplementary Figure 5: Small-molecule G4 ligands stimulate retrotransposition of the human L1RP element in HeLa cells.
From: G-quadruplex structures within the 3′ UTR of LINE-1 elements stimulate retrotransposition
(a) Growth inhibition properties of the small molecules. GI50 values of growth inhibition were determined using the cell viability assay CellTiter-GloTM after 4 days of incubation (data represent mean values ± s.d.; n = 3 independent cell cultures). (b) Representative FACS profiles of HeLa cells transfected with either pL1RPWT or pL1RP∆G4 and treated with the different quadruplex ligands PDS, PhenDC3, 12459 and PDC12. PDC20 and HgS were used as negative and positive controls respectively. (c) Percentage of EGFP positive cells for the different treatments. The blue and red lines report the mean values of the percentages of EGFP positive cells transfected with pL1RPWT or pL1RP∆G4 mock treated with DMSO. (d) Percentage of EGFP positive cells fold changes compared to mock treatment. (e-g) The small molecule PDC12 stimulates the retrotransposition of the human L1RP element in HeLa cells in a concentration dependent manner. (e) Representative FACS profiles of HeLa cells transfected with either L1RPWT or L1RP∆G4 and treated with an increasing concentration of PDC12. (f) Percentage of EGFP positive cells for different doses of PDC12. The blue and red lines report the mean values of the percentages of EGFP positive cells transfected with L1RPWT or L1RP∆G4 in the absence of PDC12 respectively. (g) EGFP positive cells fold changes compared to mock treatment (DMSO) for different doses of PDC12. The individual frames in c, d, f and g represent the mean values ± s.d. for n = 3 independent experiments.
