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

      1 , , ,

      Science (New York, N.Y.)

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          Abstract

          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 reduces the amount of chemical synthesis and time required for the discovery of high-affinity ligands and appears particularly useful in target-directed drug research.

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          Author and article information

          Journal
          Science
          Science (New York, N.Y.)
          0036-8075
          0036-8075
          Nov 29 1996
          : 274
          : 5292
          Affiliations
          [1 ] Pharmaceutical Discovery Division, Abbott Laboratories, Abbott Park, IL 60064, USA.
          Article
          8929414

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