# US 2008/0188641 A1 · Methods for detecting and inhibiting angiogenesis

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- Number: US 2008/0188641 A1
- Document ID: US20080188641A1
- Status: Published application
- Kind: A1
- Application number: 11/743,008
- Filed: 2007-05-01
- Published: 2008-08-07
- Earliest claimed: 1998-05-08
- Assignees: University of California, San Diego
- Inventors: Judith A. Varner
- Web page: https://patentgrep.com/patent/US20080188641A1

## CPC

- C07K 16/2842: {against integrin beta1-subunit-containing molecules, e.g. CD29, CD49}
- A61K 38/08: Peptides having 5 to 11 amino acids {(A61K38/043 - A61K38/046 take precedence)}
- A61P 35/00: Antineoplastic agents
- C07K 16/2845: {against integrin beta2-subunit-containing molecules, e.g. CD11, CD18}
- A61K 2039/505: {comprising antibodies}
- C07K 2317/76: Antagonist effect on antigen, e.g. neutralization or inhibition of binding
- 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)
- 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)
- A61P: SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS

## Abstract

The present invention provides methods for reducing or inhibiting angiogenesis in a tissue, by contacting α5β1 integrin in the tissue with an agent that interferes with specific binding of the α5β1 integrin to a ligand expressed in the tissue; and methods of identifying angiogenesis in a tissue, by contacting the tissue with an agent that specifically binds α5β1 integrin, and detecting specific binding of the agent to α5β1 integrin associated with a blood vessel in the tissue. Also provided are methods of diagnosing a pathological condition characterized by angiogenesis in a tissue in an individual. The invention further provides methods of reducing or inhibiting angiogenesis in a tissue in an individual, by administering to the individual an agent that interferes with the specific binding of α5β1 integrin to a ligand expressed in the tissue; and methods of reducing the severity of a pathological condition associated with angiogenesis in an individual, by administering to the individual an agent that interferes with specific binding of α5β1 integrin to a ligand in a tissue associated with the pathological condition. The invention also provides methods of identifying an agent that reduces or inhibits angiogenesis associated with α5β1 integrin expression in a tissue by contacting a tissue exhibiting angiogenesis associated with α5β1 integrin expression with an agent, and detecting a reduction or inhibition of angiogenesis in the tissue.

## Claims

### Claim 1

A method of identifying an α5β1 integrin antagonist agent, said method comprising identifying an agent as reducing or inhibiting angiogensis associated with α5β1 integrin expression ina tissue by detecting said agent as interfering with α5β1 integrin binding to its ligand.

### Claim 2 (depends on 1)

The method of claim 1 wherein said ligand is fibronectin.

### Claim 3 (depends on 1)

The method of claim 1 wherein said agent is an antibody or a fragment thereof, or a peptide.

### Claim 4 (depends on 2)

The method of claim 2 wherin said agent is an antibody or a fragment thereof, or a peptide.

### Claim 5 (depends on 3)

The method of claim 3 wherein said agent is a peptide.

### Claim 6 (depends on 4)

The method of claim 4 wherein said agent is a peptide.

### Claim 7 (depends on 5)

The method of claim 5 wherein said peptide specifically binds α5β1 integrin.

### Claim 8 (depends on 6)

The method of claim 6 wherein said peptide specifically binds α5β1 integrin.

### Claim 9 (depends on 5)

The method of claim 5 wherein said peptide is a cyclic peptide.

### Claim 10 (depends on 6)

The method od claim 6 wherein said peptide is a cyclic peptide.

### Claim 11 (depends on 7)

The method of claim 7 wherein said peptide comprises a sequence represented by SEQ ID NO: 1 (CRRETAWAC).

### Claim 12 (depends on 8)

The method of claim 8 wherein said peptide comprises a sequence represented by SEQ ID NO: 1 (CRRETAWAC).

### Claim 13 (depends on 1)

The method of claim 1 wherein said identifying is by detecting the agent as intefering with α5β1 integrin binding to its ligand tissue.

### Claim 14 (depends on 13)

The method of claim 13 wherein said tissue exhibits angiogensis.

### Claim 15 (depends on 5)

A method of preparing a peptide that reduces or inhibits angiogenesis associated with α5β1 integrin expression in a tissue, said method comprising chemically synthesizing a peptide identified by the method of claim 5.

### Claim 16 (depends on 6)

A method of preparing a peptide that reduces or inhibits angigenesis associated with α5β1 integrin expression in a tissue, said method comprising chemically synthesizing a peptide identified by the method of claim 6.

### Claim 17

A method od preparing an α5β1 integrin antagonist peptide, said method comprising chemically synthesizing a peptide identified as reducing or inhibiting angiogenesis associated with α5β1 integrin expression in a tissue by said peptide's interference with α5β1 integrin binding to its ligand.

### Claim 18 (depends on 17)

The method of claim 17 wherein said peptide specifically binds α5β1 integrin.

### Claim 19

A method of determining a peptide to be ab α5β1 integrin antagonist peptide, said method comprising
contacting a peptide with α5β1 integrin and its ligand, and
determining said peptide to be an α5β1 integrin antagonist which interferes with α5β1 integrin expression in a tissue.

### Claim 20 (depends on 19)

The method of claim 19 wherein said peptide specifically binds α5β1 integrin.

### Claim 21 (depends on 19)

The method of claim 19 wherein said ligand is fibronectin.

### Claim 22 (depends on 19)

The method of claim 19 wherein said α5β1 integrin and its ligand are in a tissue.

### Claim 23 (depends on 22)

The method of claim 22 wherein said tissue exhibits angiogenesis.

### Claim 24 (depends on 13)

The method of claim 13 wherein said screening is for more than one peptide and said contacting comprises a plurality of peptides with α5β1 integrin and its ligand.

### Claim 25 (depends on 19)

A method of preparing a peptide that reduces or inhibits angiogenesis associated with α5↑1 integrin expression in a tissue, said method comprising chemically synthesizing an α5β1 integrin antagonist peptide determined by the method claim 19.

### Claim 26 (depends on 19)

A method of preparing a peptide that reduces or inhibits angiogenesis associated with α5β1 integrin expression in a tissue, said method comprising chemically synthesizing an α5β1 integrin antagonist peptide according to claim 19.

### Claim 27

A method of preparing an α5β1 integrin peptide, said method comprising chemically synthesizing an α5β1 integrin antagonist peptide that inteferes with α5β1 integrin binding to its ligand and reduces or inhibits angiogenesis associated with α5β1 integrin expression in a tissue.

### Claim 28 (depends on 26)

The method of claim 26 wherein said peptide specifically binds α5β1 integrin.

### Claim 29 (depends on 27)

The method of claim 27 wherein said peptide specifically binds α5β1 integrin.