# US 7,611,711 B2 · VEGFR-3 inhibitor materials and methods > Agents: this data is available as JSON from the patentgrep API and MCP server — see https://patentgrep.com/llms.txt - Number: US 7,611,711 B2 - Document ID: US7611711B2 - Status: Granted - Kind: B2 - Application number: 10/046,922 - Filed: 2002-01-15 - Published: 2002-11-07 - Granted: 2009-11-03 - Earliest claimed: 2001-01-17 - Assignees: Vegenics Limited - Inventors: Kari Alitalo; Erkki Koivunen; Hajime Kubo - Web page: https://patentgrep.com/patent/US7611711B2 ## CPC - C07K 14/52: Cytokines; Lymphokines; Interferons - A61P 35/00: Antineoplastic agents - C07K 14/71: for growth factors; for growth regulators - A61K 38/00: Medicinal preparations containing peptides (peptides containing beta-lactam rings A61K31/00; cyclic dipeptides not having in their molecule any other peptide link than those which form their ring, e.g. piperazine-2,5-diones, A61K31/00; ergot alkaloids of the cyclic peptide type A61K31/48; containing macromolecular compounds having statistically distributed amino acid units A61K31/74; medicinal preparations containing antigens or antibodies A61K39/00; medicinal preparations characterised by the non-active ingredients, e.g. peptides as drug carriers, A61K47/00) - C07K: PEPTIDES (peptides in foodstuffs A23; obtaining protein compositions for foodstuffs, working-up proteins for foodstuffs A23J; preparations for medicinal purposes A61K; peptides containing beta-lactam rings C07D; cyclic dipeptides not having in their molecule any other peptide link than those which form their ring, e.g. piperazine-2,5-diones, C07D; ergot alkaloids of the cyclic peptide type C07D519/02; macromolecular compounds having statistically distributed amino acid units in their molecules, i.e. when the preparation does not provide for a specific; but for a random sequence of the amino acid units, homopolyamides and block copolyamides derived from amino acids C08G69/00; macromolecular products derived from proteins C08H1/00; preparation of glue or gelatine C09H; single cell proteins, enzymes C12N; genetic engineering processes for obtaining peptides C12N15/00; compositions for measuring or testing processes involving enzymes C12Q; investigation or analysis of biological material G01N33/00) - A61P: SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS - A61K: PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES (devices or methods specially adapted for bringing pharmaceutical products into particular physical or administering forms A61J3/00; chemical aspects of, or use of materials for deodorisation of air, for disinfection or sterilisation, or for bandages, dressings, absorbent pads or surgical articles A61L; soap compositions C11D) ## Abstract The present invention relates to the diagnosis, evaluation, and therapeutic intervention of disorders mediated by the activity of cell surface receptor VEGFR-3, which activity often is stimulated by VEGFR-3 ligands VEGF-C and VEGF-D. More particularly, the present invention identifies novel methods and compositions for the inhibition of VEGF-C/D binding to VEGFR-3. The compositions of the present invention will be useful in the inhibition of angiogenesis and lymphangiogenesis. ## Claims ### Claim 1 An isolated peptide comprising the amino acid sequence set forth in any one of SEQ ID NOs: 35-66, wherein the peptide is 8 to 25 amino acids in length and binds to human Vascular Endothelial Growth Factor Receptor-3 (VEGFR-3). ### Claim 2 (depends on 1) The isolated peptide according to claim 1, wherein the peptide comprises amino- and carboxy-terminal cysteine residues. ### Claim 3 (depends on 1) The isolated peptide according to claim 1, comprising the amino acid sequence set forth in any one of SEQ ID NOs: 35-43 and 55-66. ### Claim 4 (depends on 1) The isolated peptide of claim 1, wherein said peptide comprises the sequence CGYWLTIWGC (SEQ ID NO: 35). ### Claim 5 (depends on 3, 4) The peptide of claim 3 or claim 4 wherein the peptide is 10-25 amino acids in length. ### Claim 6 An isolated peptide comprising the amino acid sequence set forth in SEQ ID NO: 34, wherein the peptide is 10 to 25 amino acids in length and binds to human Vascular Endothelial Growth Factor Receptor-3 (VEGFR-3). ### Claim 7 (depends on 6) The isolated peptide according to claim 6, wherein the peptide comprises amino- and carboxy-terminal cysteine residues. ### Claim 8 An isolated peptide comprising the amino acid sequence spanning amino acid residue 2 through amino acid residue 9 of any one of SEQ ID NOs: 35 and 55-58, wherein the peptide is 8 to 25 amino acids in length and binds to human Vascular Endothelial Growth Factor Receptor-3 (VEGFR-3). ### Claim 9 (depends on 8) The isolated peptide according to claim 8, wherein the peptide comprises amino- and carboxy-terminal cysteine residues. ### Claim 10 (depends on 8) The isolated peptide of claim 8 wherein the peptide is 10 to 20 amino acids in length. ### Claim 11 (depends on 1, 6) The isolated peptide according to claim 1, 6, or 8, wherein said peptide further comprises an intramolecular bond between amino acid residues to form a cyclic peptide. ### Claim 12 (depends on 11) The isolated peptide according to claim 11, wherein the peptide comprises amino- and carboxy-terminal cysteines, and the intramolecular bond comprises a disulfide bond between the cysteines. ### Claim 13 (depends on 1, 6) The isolated peptide according to claim 1, 6, or 8, wherein said peptide inhibits Vascular Endothelial Growth Factor C (VEGF-C) binding to the human VEGFR-3. ### Claim 14 (depends on 1, 6, 8) A peptide according to claim 1, 6 or 8, wherein the peptide is conjugated to a cytoxic agent or a label. ### Claim 15 (depends on 14) The peptide of claim 14, wherein the label is selected from the group consisting of a radionuclide, a dye, an enzyme, and an enzyme substrate. ### Claim 16 (depends on 14) The peptide according to claim 14, wherein the cytotoxic agent is a radioisotope. ### Claim 17 (depends on 14) The peptide according to claim 14, wherein the cytotoxic agent is an anti-neoplastic pro-drug. ### Claim 18 (depends on 1, 6, 8) A chimeric protein comprising a peptide according to claim 1, 6 or 8 attached to a tumor necrosis factor. ### Claim 19 (depends on 1, 6, 8) A chimeric protein comprising a peptide according to claim 1, 6 or 8 attached to an antibody or binding fragment thereof. ### Claim 20 (depends on 1, 6) The isolated peptide of claim 1, 6, or 8, wherein said peptide further comprises a modification to increase the circulating in-vivo half-life of the peptide in a mammal wherein the modification is glycosylation, pegylation or inclusion of non-hydrolyzable bond. ### Claim 21 (depends on 1, 6) A peptide dimer comprising first and second peptides according to claim 1, 6, or 8 wherein the peptide dimer binds to VEGFR-3. ### Claim 22 (depends on 21) The peptide dimer according to claim 21, wherein the first and second peptides comprise the same amino acid sequence. ### Claim 23 (depends on 1, 6) A composition comprising an isolated peptide according to claim 1, 6, or 8 in a pharmaceutically acceptable carrier.