The present invention relates to a peptide having the sequence from N-terminus to C-terminus X-2X-1ZX1X2X3X4X5 whereinZ is tyrosine, phosphotyrosine or a non-natural analogue of phosphotyrosine, such as phosphonodifluoromethyl phenylalanine (F2Pmp)X-2 is a hydrophobic amino acid, such as Leu, Ile, Val, Phe, Tyr, Trp and MetX-1 is any amino acidX1 is a hydrophobic amino acid, such as Ile, Leu, Val, Phe, Tyr, Trp and MetX3 is a hydrophobic amino acid, such as Leu, Ile, Val, Phe, Tyr, Trp and MetX5 is a hydrophobic amino acid, such as Trp, Ile, Val, Phe, Tyr, and MetX2 and X4 are anionic amino acids, preferably each independently is Asp or Glu.The peptide inhibits protein-protein interactions of the Src homology 2 domain-containing phosphatase 2 (SHP2), for the treatment of cancer and RASopathies and as a biomedical research tool.

Stella, L., Biondi, B., Bocchinfuso, G., Martinelli, S., Tartaglia, M. (2020). Peptides targeting shp2 and uses thereof.

Peptides targeting shp2 and uses thereof

Lorenzo Stella;Gianfranco BOCCHINFUSO;
2020-01-01

Abstract

The present invention relates to a peptide having the sequence from N-terminus to C-terminus X-2X-1ZX1X2X3X4X5 whereinZ is tyrosine, phosphotyrosine or a non-natural analogue of phosphotyrosine, such as phosphonodifluoromethyl phenylalanine (F2Pmp)X-2 is a hydrophobic amino acid, such as Leu, Ile, Val, Phe, Tyr, Trp and MetX-1 is any amino acidX1 is a hydrophobic amino acid, such as Ile, Leu, Val, Phe, Tyr, Trp and MetX3 is a hydrophobic amino acid, such as Leu, Ile, Val, Phe, Tyr, Trp and MetX5 is a hydrophobic amino acid, such as Trp, Ile, Val, Phe, Tyr, and MetX2 and X4 are anionic amino acids, preferably each independently is Asp or Glu.The peptide inhibits protein-protein interactions of the Src homology 2 domain-containing phosphatase 2 (SHP2), for the treatment of cancer and RASopathies and as a biomedical research tool.
Università degli Studi di Roma Tor Vergata (81%)
Ospedale Pediatrico Bambino Gesù (19%)
Patent Cooperation Treaty (PCT)
2020
Italian patent n. 102020000004849 -
Settore CHIM/02
Settore CHEM-02/A - Chimica fisica
English
Stella, L; Biondi, B; Bocchinfuso, G; Martinelli, S; Tartaglia, M
Brevetti
Stella, L., Biondi, B., Bocchinfuso, G., Martinelli, S., Tartaglia, M. (2020). Peptides targeting shp2 and uses thereof.
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Utilizza questo identificativo per citare o creare un link a questo documento: https://hdl.handle.net/2108/393491
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