Linear analog of biologically active mammalian grp or...

C - Chemistry – Metallurgy – 07 – K

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C07K 7/08 (2006.01) A61K 38/08 (2006.01) A61K 38/10 (2006.01) C07K 7/06 (2006.01)

Patent

CA 2008454

Abstract of the Disclosure In general the invention features a linear (i.e., non-cyclic) bomoesin analog of biologically active mammalian gastrin-releasing peptide (GRP) and amphibian bombesin, 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 or GRP is unnecessary for in vivo biological activity. The analog has one of the following modifications: (a) a deletion of a residue within the active site and a modification of a residue outside of the active site, or (b) a replacement of one or two residues within the active site with a synthetic amino acid. The analog is capable of binding to the receptor and acting as a competitive inhibitor of the naturally occurring peptide by binding to the receptor and, by virtue of one of the modifications, failing to exhibit the in vivo biological activity of the naturally occurring peptide.

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