Conformationally Homogeneous Heterocyclic Pseudotetrapeptides as Three-Dimensional Scaffolds for Rational Drug Design: Receptor-Selective Somatostatin Analogues

摘要

Many protein-protein interactions are mediated through the recognition of β-turn secondary structures. Consequently, small-molecule β-turn mimetics are invaluable as probes for assessing bioactive ligand conformations, establishing phar-macophoric requirements, and pursuing rational drug design. Although effective small-molecule drug scaffolds have been developed for the precise positioning of up to four functionalities primarily in two dimensions, an analogous rigid scaffold capable of the predictable juxtaposition of four amino acid side chains in three dimensions has required the use of pentameric or larger cyclopeptides.