An NMR-based antagonist induced dissociation assay for targeting the ligand-protein and protein-protein interactions in competition binding experiments.

@article{Krajewski2007AnNA,
  title={An NMR-based antagonist induced dissociation assay for targeting the ligand-protein and protein-protein interactions in competition binding experiments.},
  author={Marcin Krajewski and Ulli Rothweiler and Loyola D'Silva and Sudipta Majumdar and Christian Klein and Tad A. Holak},
  journal={Journal of medicinal chemistry},
  year={2007},
  volume={50 18},
  pages={4382-7}
}
We present an NMR-based antagonist induced dissociation assay (AIDA) for validation of inhibitor action on protein-protein interactions. As opposed to many standard NMR methods, AIDA directly validates the inhibitor potency in an in vitro NMR competition binding experiment. AIDA requires a large protein fragment (larger than 30 kDa) to bind to a small reporter protein (less than 20 kDa). We show here that a small fragment of a protein fused to glutathione S-transferase (GST) can effectively… CONTINUE READING