Arginine-rich anti-vascular endothelial growth factor...

Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Peptide containing doai

Reexamination Certificate

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C530S329000

Reexamination Certificate

active

09913956

ABSTRACT:
Disclosed are novel peptides inhibitory of the activity of vascular endothelial growth factor (VEGF) and their use in the treatment of angiogenesis-related diseases, including cancer. A combinatorial library of peptides consisting of six amino acid residues were chemically synthesize and, from the library, specific amino acid residues for each amino acid position were screened by comparing their inhibitory activity against VEGF binding to the cell surface receptor. The novel peptide sequences thus obtained bind to VEGF and block the binding of VEGF to its receptors present on the surface of vascular endothelial cells, thereby inhibiting the hormonal activity of VEGF. The peptides inhibit the angiogenesis induced by VEGF and human cancer cells. Also, the peptides inhibit growth and metastasis of human cancer cells transplanted to mice. Thus, the peptides can be used to treat angiogenesis-related diseases, including cancer, diabetic retinopathy, rheumatoid arthritis, etc.

REFERENCES:
patent: 19724793 (1998-12-01), None
patent: 9702554 (1999-11-01), None
patent: WO 00/74701 (2000-12-01), None
Kim et al. Inhibition of vascular endothelial growth factor-induced angiogenesis . . . Nature. Apr. 29, 1993, vol. 362, pp. 841-844.
Borgstrom et al. Complete inhibition of angiogenesis . . . Cancer Research. Sep. 1996, vol. 56, pp. 4032-4039.
Ferrer-Montiel et al. Selected peptides targeted to the NMDA receptor channel . . . Nature Biotechnology. Mar. 1998, vol. 16, pp. 286-291.
Iida et al. Macrophage Activation And Host Augmentation . . . International Journal of Immunopharmacology. 1989, vol. 11, No. 3, pp. 249-258.
Bae D G et al: “Arginine-rich anti-vascular endothelial growth factor peptides inhibit tumor growth and metastasis by blocking angiogenesis”; The Journal of Biological Chemistry; United States May 5, 2000; vol. 275, No. 18, pp. 13588-13596.
Supplementary Partial European Search Report, dated Jan. 27, 2004, Examiner O. Lechner.

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