Figure 8.
Fluorescence displacement assay based on ligand-conjugated QDots for the drug discovery of allosteric antidepressants. (A) Targeted hSERTs bind to the QDot-tagged ligands, forming complexes that increase fluorescent signal along the membrane. When exposed to a potential drug that induces a conformational change in the binding site, the QDot-tagged ligands are displaced resulting in a decrease in fluorescence intensity. (B) Representative time-lapse fluorescent images show the effect of paroxetine on lhigand-hSERT displacement in the presence of PBS buffer (control), 10 µM, and 20 µM paroxetine. (Reprinted with permission from Ref 62. Copyright 2011 American Chemical Society)