Identification of a potent heterocyclic ligand to somatostatin receptor subtype 5 by the synthesis and screening of beta-turn mimetic libraries

The experimental procedures for the parallel synthesis of medium-ring heterocyclic beta-turn mimetics are described. The innovative method involves the rapid generation of libraries of mimetics for the identification of small molecule ligands to receptors. The method has been applied to the synthesis of mimetics with a wide range of amino acid side chains. The development of the 87 nM ligand, a human somatotropin receptor 5, is also described.