# US 10,864,251 B2 · Peptides of syndecan-1 for inhibiting angiogenesis

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- Number: US 10,864,251 B2
- Document ID: US10864251B2
- Status: Granted
- Kind: B2
- Application number: 16/251,217
- Filed: 2019-01-18
- Published: 2019-05-16
- Granted: 2020-12-15
- Earliest claimed: 2006-06-09
- Assignees: Wisconsin Alumni Research Foundation
- Applicants: Wisconsin Alumni Research Foundation
- Inventors: Alan C. Rapraeger; DeannaLee M. Beauvais
- Web page: https://patentgrep.com/patent/US10864251B2

## CPC

- A61K 38/1709: {from mammals}
- A61K 45/06: Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
- A61P 43/00: Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
- C07K 7/06: having 5 to 11 amino acids
- C07K 7/08: having 12 to 20 amino acids (gastrins C07K14/595; somatostatins C07K14/655; melanotropins C07K14/68)
- C07K 14/4725: {Proteoglycans, e.g. aggreccan}
- C07K 14/705: Receptors; Cell surface antigens; Cell surface determinants {(tumour specific antigens C07K14/4748)}
- 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)
- 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
- 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)

## Abstract

The present invention provides a peptide derived from the extracellular domain of syndecan-1 that inhibits angiogenesis.

## Claims

### Claim 1

A method of inhibiting αvβ3 or αvβ5 integrin activation by syndecan-1, comprising contacting a cell expressing an αvβ3 or αvβ5 integrin molecule with a polypeptide segment consisting of 32 to 100 amino acid residues and comprising SEQ ID NO:21, whereby the αvβ3 or αvβ5 integrin activation is inhibited.

### Claim 2 (depends on 1)

The method of claim 1, wherein the polypeptide segment is 32 to 80 amino acid residues in length.

### Claim 3 (depends on 1)

The method of claim 1, wherein the polypeptide segment is 32 to 50 amino acid residues in length.

### Claim 4 (depends on 1)

The method of claim 1, wherein the polypeptide segment consists of SEQ ID NO:10.

### Claim 5 (depends on 1)

The method of claim 1, wherein the polypeptide segment comprises at least 35 contiguous amino acids from SEQ ID NO:10.

### Claim 6 (depends on 1)

The method of claim 1, wherein the polypeptide segment consists of SEQ ID NO:28.

### Claim 7 (depends on 1)

The method of claim 1, wherein the polypeptide segment consists of SEQ ID NO:21.

### Claim 8 (depends on 1)

The method of claim 1, wherein the step of contacting the cell with the polypeptide segment is accomplished by administering the polypeptide segment to a subject having a disease characterized by the activation of the αvβ3 or αvβ5 integrin, whereby the disease is treated.

### Claim 9 (depends on 8)

The method of claim 8, wherein the disease is a cancer in which the αvβ3 or αvβ5 integrin is upregulated.

### Claim 10 (depends on 9)

The method of claim 9, wherein the method inhibits the survival of cancerous tumor cells within the subject.

### Claim 11 (depends on 10)

The method of claim 10, wherein survival of the cancerous tumor cells is inhibited by inducing apoptosis in the cancerous tumor cells.

### Claim 12 (depends on 9)

The method of claim 9, wherein the method inhibits the migration of cancerous tumor cells within the subject.

### Claim 13 (depends on 9)

The method of claim 9, wherein the method inhibits the metastasis of cancerous tumor cells within the subject.

### Claim 14 (depends on 9)

The method of claim 9, wherein the method inhibits cancer-related angiogenesis within the subject.

### Claim 15 (depends on 14)

The method of claim 14, wherein the angiogenesis is inhibited by reducing the proliferation and migration of endothelial cells that are associated with angiogenesis.

### Claim 16 (depends on 14)

The method of claim 14, wherein the angiogenesis is inhibited by reducing the survival of endothelial cells that are associated with angiogenesis.

### Claim 17 (depends on 16)

The method of claim 16, wherein survival of the endothelial cells is reduced by increasing the susceptibility of the endothelial cells to apoptosis.

### Claim 18 (depends on 8)

The method of claim 8, wherein the disease is a noncancerous disease in which the αvβ3 or αvβ5 integrin is upregulated.

### Claim 19 (depends on 18)

The method of claim 18, wherein the noncancerous disease is a disease that is characterized by angiogenesis.

### Claim 20 (depends on 19)

The method of claim 19, wherein the method inhibits the disease-related angiogenesis within the subject.
