| 摘要 |
A description is given of a process for the preparation of therapeutic peptides, which are linear (i.e. non- cyclic) analogues of the biologically active bombesin of amphibians or of the gastrin releasing peptide (GRP) of mammals, which has an active site and a binding site, responsible for binding the peptide to the target cell receptor. Cleavage of a peptide bond in the active site of bombesin and GRP, which occurs naturally, is unnecessary for biological activity in vivo. The analogues have one of the following modifications: (a) loss of an amino acid residue in the active site and modification of an amino acid residue outside the active site, (b) replacement of two amino acid residues in the active site by a synthetic amino acid, β-amino acid or γ-amino acid residue, or (c) a non-peptide bond instead of a peptide bond between an amino acid residue of an active site and an adjacent amino acid residue.
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