Figure 2 | Scientific Reports

Figure 2

From: GLUT3 inhibitor discovery through in silico ligand screening and in vivo validation in eukaryotic expression systems

Figure 2

Effect of compounds identified from TBVS on GLUT3 transport activity. (A) GLUT3 relative transport activity in the presence of 50 µM compound concentration, at 3 mM glucose concentration. Glucose transport activity of GLUT3 expressed in hxt0 yeast cells EBY.S7 was measured as C14-glucose uptake in whole cells (see “Materials and methods” for details). The compounds are identified by the ChemNavigator Structure ID. Six compounds, G3iA–G3iF (ChemNavigator Structure ID number underlined), inhibited GLUT3 relative activity by more than 60%. Initial screening at 100 µM concentration for all 193 tested compounds (listed in Supplementary Table S1) is shown in Supplementary Fig. S2. (B–G) Dose response curves for G3iA-G3iF inhibition of GLUT3 relative transport activity. Standard deviations for experimental points come from at least three independent measurements. Graphs, data analysis, and IC50 values were generated with GraphPad (https://www.graphpad.com).

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