Figure 6: Real-time imaging of drug–target engagement in live cells.
From: In vivo imaging of specific drug–target binding at subcellular resolution
Normalized intensity and anisotropy as a function of time for HT1080 cells loaded with AZD2281–BODIPY FL and washed. Values are measured in both the cytoplasmic (a) and nuclear (b) regions of the cells in the absence (black circles) and presence (grey squares) of fivefold higher concentration of unlabelled AZD2281 (competition). Points in the graphs refer to a single experiment, average±s.d. (n=6 cells). Also shown at the right of each figure, average±s.d. at the end of the wash in the absence (black bars, n=42 cells, seven separate experiments) and presence (grey bars, n=36 cells, six separate experiments) of unlabelled AZD2281 (5 × ). Bars are representative of seven and six different experiments, respectively. Red arrows indicate switch from loading to washing. Fluorescence intensity refers to the sum of both perpendicular and parallel channels.
