SYNTHETIC, STABILIZED, THREE-DIMENSION POLYPEPTIDES

摘要

Methods for synthesizing three-dimensional stabilized peptides which mimic the three-dimensional configuration of the active site of a natural, biologically active protein are carried out by (1) noting the three-dimensional configuration of the active site of a known biologically active protein, (2) noting the amino acid sequence and the hydrogen bonds existing between amino acids which hydrogen bonds are capable of maintaining the three-dimensional configuration of the active site and (3) producing a synthetic three-dimensional peptide to mimic the structure of the active site. The synthetic peptide is synthesized so as to have the same or a similar amino acid sequence to the amino acid sequence of the active site of the biologically active polypeptide but with the stabilizing hydrogen bonds being replaced by a bridging divalent radical selected from the group consisting of -(N)-C(CH3)=N(H<+>)-CH2-(N)-; -(N)-C(CH3)=N(H<+>)-CH2-CH2-(N)-; and -(N)-N=CH-CH2-CH2-CH2-(C)-.