Octapeptide bombesin analogs

Details Octapeptide bombesin analogs Octapeptide bombesin analogs

1994-11-10

1999-03-02

Davenport, Avis M.

Chemistry: natural resins or derivatives; peptides or proteins;

Peptides of 3 to 100 amino acid residues

8 to 10 amino acid residues in defined sequence

530323, C07K 500, C07K 700, C07K 706, A61K 3800

Patent

active

058772774

ABSTRACT:
A linear (i.e., non-cyclic) analog of biologically active amphibian bombesin, mammalian gastrin-releasing peptide (GRP), or mammalian growth hormone releasing factor (GRF), having an active site and a binding site responsible for the binding of the peptide to a receptor on a target cell. Cleavage of a peptide bond in the active site of naturally occurring bombesin, GRP, or GRF is unnecessary for in vivo biological activity. The analog has one of the following modifications: (a) a deletion of an amino acid residue within the active site and a modification of an amino acid residue outside of the active site, (b) a replacement of two amino acid residues within the active site with a synthetic amino acid, a .beta.-amino acid, or a .gamma.-amino acid residue, or (c) a non-peptide bond instead of a peptide bond between an amino acid residue of the active site and an adjacent amino acid residue.

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Camble et al., Peptides: Chemistry, Structure and Biology "ICI 216140 and other potent in vivo antagonist analogs of bombesin/gastrin-releasing peptide" 174-176, 1990.
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