Figure 1: PDGF-induced change in conformation and phosphorylation of AKT are inhibited upon treatment with 2-O-Bn-InsP5.
From: A Small Molecule Inhibitor of PDK1/PLCγ1 Interaction Blocks Breast and Melanoma Cancer Cell Invasion
(A) The increase in FRET efficiency upon PDGF treatment indicates a change in conformation of AKT that is prevented upon pre-treatment with the inhibitor. Box and whiskers plots of FRET efficiencies are displayed for the indicated conditions. Each cell is represented by a red symbol. A Mann-Whitney test was used to calculate the P values shown on the graph (n = 3 experiments; **p = 0.0016, ***p = 0.0001). (B) Cells were left untreated or treated with 2-O-Bn-InsP5 prior to PDGF stimulation and phosphorylation of AKT at residues Threonine 308 (pT308) and Serine 473 (pS473) was assessed by Western blotting. (C,D) Results from densitometry analysis of Western blotting showing significant decrease in the normalized phosphorylation of AKT at T308 and S473 from 4 independent experiments (**p = 0.002, *p = 0.007 respectively).
