| abstract |
Linear (i.e. non-cyclic) analog of bombesin of a biologically active peptide from mammalian, gastrin-releasing (GRP), and bombesin of amphibians, having an active site and a binding site responsible for binding the peptide to a receptor of a target cell; cleavage of a peptide bond in the active site of natural bombesin or GRP is not necessary to obtain biological activity in vivo. This analog has one of the following modifications: (a) deletion of a residue in the active site and modification of a residue outside the active site, or (b) replacement of one or two residues in the active site by a synthetic amino acid. This analog can bind to the receptor and, through this bond, plays the role of competitive inhibitor of the natural peptide; however, thanks to one of the modifications, it does not exhibit the in vivo biological activity of the natural peptide. |