Inhibitors of alpha integrin in beta 6

摘要

The invention relates to novel peptides of formula (I) Ac-Arg-X<1>-Asp-X<2>-X<3>-X<4>-X<5>-X<6>-NH2 which are biologically active as ligands of the integrin alpha v beta 6, wherein: Ac represents Acetyl, X<1> represents Ser, Gly, Thr, Asp, Arg, Val, Tyr, His or Ala; X<2> represents Leu, Ile, Nle, Val or Phe; X<3> represents Asp, Glu, Lys, Phe, Aib, Nal, Gly, Ala, Bgl or Phg; X<4> represents Gly, Ala, Ser, beta -Ala or omega -Abu; X<5> represents Leu, Ile, Nle, Val or Phe, and; X<6> represents Arg, Har, Lys, Leu, Orn, Phe, Ala, Tyr, Gly, Ser or Asp, whereby the aforementioned amino acids can be derivatized. The amino acid radicals are linked to one another in a peptide-like manner via the alpha -amino groups and the alpha -carboxy groups. The dextrorotatory forms and the levorotatory forms of the optically active amino acid radicals are contained as well as the salts of said peptides. Ac-Arg-Thr-Asp-Leu-Asp-Ser-Leu-Arg-NH2 is excluded. The inventive peptides can also be used as effective inhibitors of the alpha v beta 6 integrin receptor and thus for treating different diseases and pathological findings.