Peptide inhibitors of a phosphotyrosine-binding domain...

Details Peptide inhibitors of a phosphotyrosine-binding domain... Peptide inhibitors of a phosphotyrosine-binding domain...

C - Chemistry, Metallurgy

07

K

C07K 7/08 (2006.01) A61K 38/08 (2006.01) A61K 38/10 (2006.01) A61K 38/12 (2006.01) C07K 7/06 (2006.01) C07K 7/64 (2006.01) C07K 14/71 (2006.01) C07K 14/715 (2006.01) A61K 38/00 (2006.01)

Patent

CA 2235756

A peptide of the formula (I): X1-A1-A2-X2-Asn-X3-X4-P.Tyr-X5-X6-X7-X8, wherein X1 represents Lys, Arg, His, Ser, Thr, Tyr, Asn, Leu, Val or Glu, A1 represents Trp, Leu, Ala, Ser, Ile, Glu, Met, Gly, Cys, Phe, Pro or Val, and A2 represents Ala, Val, Leu, Ile, Ser, Met, Phe, Gly, Cys, Trp or Pro, X2 represents Glu, Asn, Tyr, Thr, Ser, Asp or Ile, X3 represents Pro, Met, Trp, Phe, Ala, Lys, Val, Leu, Ile, Gly or Cys, X4 represents Leu, Ala, Glu, Gln, Asp, Asn, Tyr, Thr or Ser, X5 represents Phe, Trp, Pro, Leu, Ala, Val, Ile, Gly, Cys, Met, Arg or Ser, X6 represents Ser, Thr, Tyr, Asn, Glu, Met, Ala, Leu, Val or Gly, X7 represents Asp, Glu, Ala, Val, Leu, Ile, Gly, Cys, Phe, Trp, Met, Pro, Ser or Asn and X8 which may be present or absent represents Phe, Trp, Pro, Leu, Ala, Val, Ile, Gly, Cys, Met, Asp, Ser or Arg which interferes with the interaction of a PTB domain containing protein with a PTB domain binding site, and truncations and analogues of the peptide.

L'invention concerne un peptide de la formule (I): X?1¿-A?1¿-A?2¿-X?2¿-Asn-X?3¿-X?4¿-P.Tyr-X?5¿-X?6¿-X?7-¿X?8¿, dans laquelle X représente Lys, Arg, His, Ser, Thr, Tyr, Asn, Leu, Val ou Glu, A?1¿ représente Trp, Leu, Ala, Ser, Ile, Glu, Met, Gly, Cys, Phe, Pro ou Val, et A?2¿ représente Ala, Val, Leu, Ile, Ser, Met, Phe, Gly, Cys, Trp ou Pro, X?2¿ représente Glu, Asn, Tyr, Thr, Ser, Asp ou Ile, X?3¿ représente Pro, Met, Trp, Phe, Ala, Lys, Val, Leu, Ile, Gly ou Cys, X?4¿ représente Leu, Ala, Glu, Gln, Asp, Asn, Tyr, Thr ou Ser X?5¿ représente Phe, Trp, Pro, Leu, Ala, Val, Ile, Gly, Cys, Met, Arg ou Ser, X?6¿ représente Ser, Thr, Tyr, Asn, Glu, Met, Ala, Leu, Val ou Gly, X?7¿ représente Asp, Glu, Ala, Val, Leu, Ile, Gly, Cys, Phe, Trp, Met, Pro, Ser ou Asn et X?8¿, pouvant être présent ou absent, représente Phe, Trp, Pro, Leu, Ala, Val, Ile, Gly, Cys, Met, Asp, Ser ou Arg. Ce peptide perturbe l'interaction d'un domaine de liaison de phosphotyrosine (PTB) contenant une protéine avec un site de liaison de domaine (PTB). L'invention concerne également des troncatures et des analogues du peptide.

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