Process for the preparation of therapeutic peptides

摘要

A process is described for the preparation of a linear (that is non-cyclic) bombesine analogue from biologically active mammalian gastrin releasing peptide (GRP) and amphibian bombesine with an active site and a binding site responsible for binding the peptide to a target cell receptor; the cutting of a peptide link at the active site in the naturally produced bombesine or GRP is not necessary for biological activity in vivo. The analogue has one of the following modifications: a) elimination of a residue in the active site and modification of a residue outside the active site, or b) substitution of one or two residues in the active site with a synthetic acid amine. The analogue is capable of binding and acts as a competitive inhibitor for the naturally produced peptide in binding at the receptor, and because of one of the modifications fails to exhibit the biological activity in vivo of the naturally produced peptide.