THERAPEUTIC PEPTIDES
    3.
    发明授权
    THERAPEUTIC PEPTIDES 失效
    肽药物

    公开(公告)号:EP0438519B1

    公开(公告)日:1998-05-06

    申请号:EP89912292.3

    申请日:1989-10-13

    IPC分类号: C07K7/02 C07K14/595 A61K38/16

    摘要: In general, the invention features a linear (i.e., non-cyclic) bombesin analog of biologically active mammalian gastrin-releasing peptide (GRP) and amphibian bombesin, having an active site and a binding site responsable for the binding of the peptide to a receptor on a target cell; cleavage of a peptide bond in the active site of naturally occuring bombesin or GRP is unnecessary for in vivo bilogical 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 remplacement 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.