# US 10,766,942 B2 · Fragments of syndecan-2 having anti-angiogenic activity

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- Number: US 10,766,942 B2
- Document ID: US10766942B2
- Status: Granted
- Kind: B2
- Application number: 15/520,149
- Filed: 2015-10-20
- Published: 2017-11-09
- Granted: 2020-09-08
- Earliest claimed: 2014-10-20
- Assignees: Queen Mary University of London
- Applicants: Queen Mary University of London
- Inventors: James Whiteford; Giulia De Rossi
- Web page: https://patentgrep.com/patent/US10766942B2

## CPC

- C07K 14/705: Receptors; Cell surface antigens; Cell surface determinants {(tumour specific antigens C07K14/4748)}
- A61P 3/10: for hyperglycaemia, e.g. antidiabetics
- A61P 7/00: Drugs for disorders of the blood or the extracellular fluid
- A61P 9/00: Drugs for disorders of the cardiovascular system
- A61P 9/10: for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
- A61P 11/06: Antiasthmatics
- A61P 17/06: Antipsoriatics
- A61P 19/02: for joint disorders, e.g. arthritis, arthrosis
- A61P 27/02: Ophthalmic agents
- A61P 27/06: Antiglaucoma agents or miotics
- A61P 35/00: Antineoplastic agents
- A61P 37/06: Immunosuppressants, e.g. drugs for graft rejection
- A61P 43/00: Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
- C07K 14/78: Connective tissue peptides, e.g. collagen, elastin, laminin, fibronectin, vitronectin or cold insoluble globulin [CIG]
- 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 14/00: Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
- 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 provides an anti-angiogenic peptide comprising an amino acid sequence having at least 70% identity to amino acid residues 123-140 of SEQ ID NO 1 or amino acid residues 24-141 of SEQ ID NO 2. The invention also provides nucleic acid constructs encoding such peptides, and vectors and cells comprising such nucleic acid constructs. The invention further provides pharmaceutical compositions comprising the peptides or nucleic acid constructs of the invention, and the use of peptides, nucleic acid constructs or pharmaceutical compositions of the invention to treat diseases associated with angiogenesis.10

## Claims

### Claim 1

An anti-angiogenic peptide consisting of up to 25 amino acids comprising a) amino acid residues 123-140 of SEQ ID NO 1 or amino acid residues 124-141 of SEQ ID NO 2, or b) amino acid residues 123-140 of SEQ ID NO 1 and having conservative amino acid substitutions at one or more positions selected from the group consisting of E125, E126, D127, N129, and S138, or amino acid residues 124-141 of SEQ ID NO 2 and having conservative amino acid substitutions at one or more positions selected from the group consisting of I126, K127, S128, D130, and N139.

### Claim 2 (depends on 1)

The anti-angiogenic peptide according to claim 1, wherein the peptide consists of 18 or 19 amino acids and includes a) amino acid residues 123-140 of SEQ ID NO 1 or amino acid residues 124-141 of SEQ ID NO 2, or b) amino acid residues 123-140 of SEQ ID NO 1 and having conservative amino acid substitutions at one or more positions selected from the group consisting of E125, E126, D127, N129, and S138, or amino acid residues 124-141 of SEQ ID NO 2 and having conservative amino acid substitutions at one or more positions selected from the group consisting of I126, K127, S128, D130, and N139.

### Claim 3 (depends on 1)

The anti-angiogenic peptide according to claim 1, wherein the peptide comprises up to 25 consecutive amino acid residues selected from: a) amino acid residues 120-144 of SEQ ID NO 1 or amino acid residues 121-145 of SEQ ID NO 2, or b) amino acid residues 120-144 of SEQ ID NO 1 and having conservative amino acid substitutions at one or more positions selected from the group consisting of E125, E126, D127, N129, and S138, or amino acid residues 121-145 of SEQ ID NO 2 and having conservative amino acid substitutions at one or more positions selected from the group consisting of I126, K127, S128, D130, and N139.

### Claim 4 (depends on 3)

The anti-angiogenic peptide according to claim 3, wherein the peptide consists of amino acid residues 123-140 of SEQ ID NO 1 or amino acid residues 124-141 of SEQ ID NO 2.

### Claim 5 (depends on 1)

The anti-angiogenic peptide according to claim 1 wherein the peptide is fused to a heterologous peptide.

### Claim 6 (depends on 1)

A nucleic acid construct encoding the anti-angiogenic peptide according to claim 1.

### Claim 7 (depends on 6)

A vector comprising a nucleic acid construct according to claim 6.

### Claim 8 (depends on 6)

A cell comprising a nucleic acid construct according to claim 6.

### Claim 9 (depends on 1)

A pharmaceutical composition comprising a pharmaceutically acceptable carrier and an anti-angiogenic peptide according to claim 1 or a nucleic acid construct encoding an anti-angiogenic peptide according to claim 1.

### Claim 10 (depends on 9)

A pharmaceutical composition according to claim 9 further comprising an anti-angiogenic compound.

### Claim 11 (depends on 10)

A pharmaceutical composition according to claim 10 wherein the anti-angiogenic compound is selected from the group consisting of suramin, sorafenib and sunitinib.

### Claim 12 (depends on 1)

A method for the treatment of a disease associated with angiogenesis comprising administering to a subject in need thereof a therapeutically effective amount of an anti-angiogenic peptide according to claim 1, or a nucleic acid construct encoding an anti-angiogenic peptide according to claim 1.

### Claim 13 (depends on 12)

The method according to claim 12 wherein the disease is cancer, arthritis, psoriasis, asthma, atherosclerosis or an ocular disease.

### Claim 14 (depends on 1)

A kit comprising an anti-angiogenic peptide according to claim 1, or a nucleic acid construct encoding an anti-angiogenic peptide according to claim 1.

### Claim 15 (depends on 7)

A cell comprising a vector according to claim 7.

### Claim 16 (depends on 9)

A method for the treatment of a disease associated with angiogenesis comprising administering to a subject in need thereof a therapeutically effective amount of a pharmaceutical composition according to claim 9.

### Claim 17 (depends on 13)

The method according to claim 13 wherein the ocular disease is selected from the group consisting of diabetic retinopathy, exudative (wet) or nonexudative (dry) macular degeneration (AMD), corneal graft rejection, corneal neovascularisation, retinopathy of prematurity (ROP), retinal artery or vein occlusion, neovascular glaucoma, and sickle cell retinopathy.

### Claim 18 (depends on 9)

A kit comprising a pharmaceutical composition according to claim 9.

### Claim 19

An anti-angiogenic peptide consisting of up to 25 amino acids comprising: a) amino acid residues 123-140 of SEQ ID NO 1 or amino acid residues 124-141 of SEQ ID NO 2, or b) amino acid residues 123-140 of SEQ ID NO 1 and having one conservative amino acid substitution therein, or amino acid residues 124-141 of SEQ ID NO 2 and having one conservative amino acid substitution therein.

### Claim 20 (depends on 19)

The anti-angiogenic peptide according to claim 19, wherein the peptide consists of 18 or 19 amino acids and includes: a) amino acid residues 123-140 of SEQ ID NO 1 or amino acid residues 124-141 of SEQ ID NO 2, or b) amino acid residues 123-140 of SEQ ID NO 1 and having one conservative amino acid substitution therein or amino acid residues 124-141 of SEQ ID NO 2 and having one conservative amino acid substitution therein.

### Claim 21 (depends on 19)

The anti-angiogenic peptide according to claim 19, wherein the peptide comprises up to 25 consecutive amino acid residues selected from: a) amino acid residues 120-144 of SEQ ID NO 1 or amino acid residues 121-145 of SEQ ID NO 2, or b) amino acid residues 120-144 of SEQ ID NO 1 and having one conservative amino acid substitution therein or amino acid residues 121-145 of SEQ ID NO 2 and having one conservative amino acid substitution therein.