Synthesis and Biological Evaluation of Mixed β2/β3-Dipeptides as Somatostatin Analogs

Abstract

A symposium report. The synthesis and specific binding to the five cloned human somatostatin receptors of b2/b3-mixed dipeptides as mimics of the crucial b-turn region present in somatostatin are reported. The central Lys and Trp residues in somatostatin are a prerequisite for high biol. activity. The 1H NMR and CD spectra have shown that mixed (S)-b2/(S)-b3-dipeptide can fold into a turn-type structure, thus mimicking a natural cyclo-a-peptide with high biol. activity. This result clearly demonstrates the potential of b-peptides as peptidomimetics. [on SciFinder (R)]