Discovering high-affinity ligands for proteins: SAR by NMR.

  title={Discovering high-affinity ligands for proteins: SAR by NMR.},
  author={Suzanne Beckham Shuker and Philip J. Hajduk and Robert P. Meadows and Stephen W. Fesik},
  volume={274 5292},
A nuclear magnetic resonance (NMR)-based method is described in which small organic molecules that bind to proximal subsites of a protein are identified, optimized, and linked together to produce high-affinity ligands. The approach is called "SAR by NMR" because structure-activity relationships (SAR) are obtained from NMR. With this technique, compounds with nanomolar affinities for the FK506 binding protein were rapidly discovered by tethering two ligands with micromolar affinities. The method… CONTINUE READING
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