# US 2013/0157338 A1 · Rhamm binding peptides

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- Number: US 2013/0157338 A1
- Document ID: US20130157338A1
- Status: Published application
- Kind: A1
- Application number: 13/701,240
- Filed: 2011-05-31
- Published: 2013-06-20
- Earliest claimed: 2010-05-31
- Assignees: London Health Sciences Centre Research Inc.
- Inventors: Leonard G. Luyt; Eva A. Turley; Kenneth Virgel Esguerra
- Web page: https://patentgrep.com/patent/US20130157338A1

## CPC

- C07K 7/08: having 12 to 20 amino acids (gastrins C07K14/595; somatostatins C07K14/655; melanotropins C07K14/68)
- A61K 49/0043: {Fluorescein, used in vivo}
- A61K 49/0056: {Peptides, proteins, polyamino acids}
- A61K 51/088: {conjugates with carriers being peptides, polyamino acids or proteins (antibodies A61K51/10)}
- A61P 17/02: for treating wounds, ulcers, burns, scars, keloids, or the like
- A61P 35/00: Antineoplastic agents
- A61P 35/02: specific for leukemia
- A61P 35/04: specific for metastasis
- 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 14/47: from mammals
- C07K 14/705: Receptors; Cell surface antigens; Cell surface determinants {(tumour specific antigens C07K14/4748)}
- G01N 33/5011: {for testing antineoplastic activity}
- G01N 33/5759: {involving compounds localised on the membrane of tumour or cancer cells}
- G01T 1/249: {specially adapted for use in SPECT or PET (SPECT imaging G01T1/1642; PET imaging G01T1/2985; detecting prohibited goods, e.g. weapons, explosives, hazardous substances, contraband or smuggled objects G01V5/20)}
- 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)
- G01N 2333/70596: Molecules with a "CD"-designation not provided for elsewhere in G01N2333/705
- 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
- G01N: INVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES (measuring or testing apparatus or processes other than immunoassay, involving enzymes or microorganisms C12M, C12Q)
- G01T: MEASUREMENT OF NUCLEAR OR X-RADIATION (radiation analysis of materials, mass spectrometry G01N23/00; tubes for determining the presence, intensity, density or energy of radiation or particles H01J47/00)

## Abstract

The present invention provides for peptides that bind to Receptor for Hyaluronic Acid Mediated Motility (RHAMM) molecules. More specifically, provided are peptides capable of specifically binding RHAMM molecules and capable of binding RHAMM with substantially high affinity. These novel RHAMM-binding peptides provide the basis for new imaging probes that can be used to identify cells expressing RHAMM, and for methods of imaging, prognosis, diagnosis and treatment of conditions associated with RHAMM expression.

## Claims

### Claim 1

A RHAMM-binding peptide characterized in that said RHAMM-binding peptide comprises a sequence having a formula EEXEEZ (SEQ ID NO: 18), wherein X is selected from alanine or glycine, and Z is selected from tyrosine or glutamic acid, or a functional analog thereof.

### Claim 2

A RHAMM-binding peptide characterized in that said RHAMM-binding peptide comprises at least one of the amino acid sequences selected from the group consisting of SEQ ID NO: 1 to SEQ ID NO: 17, or a functional analog thereof.

### Claim 3 (depends on 2)

The RHAMM-binding peptide of claim 2, characterized in that said RHAMM-binding peptide is selected from SEQ ID NO: 1, SEQ ID NO: 3, SEQ ID NO: 9, SEQ ID NO: 10, SEQ ID NO: 11, SEQ ID NO: 12 and SEQ ID NO: 14, or a functional analog thereof.

### Claim 4 (depends on 1)

The RHAMM-binding peptide of claim 1, characterized in that said RHAMM-binding peptide is selected from SEQ ID NO:1, SEQ ID NO:3, SEQ ID NO: 9, and SEQ ID NO:11, or a functional analog thereof.

### Claim 5 (depends on 1)

The RHAMM-binding peptide of claim 1, wherein said RHAMM-binding peptide is a tubulin-derived peptide.

### Claim 6

(canceled)

### Claim 7

(canceled)

### Claim 8

(canceled)

### Claim 9

(canceled)

### Claim 10 (depends on 1)

The RHAMM-binding peptide of claim 1 characterized in that said RHAMM-binding peptide is conjugated with a detectable label.

### Claim 11 (depends on 10)

The RHAMM-binding peptide of claim 10 characterized in that the detectable label is selected from biotin-based labels, magnetic labels, radioactive labels, fluorescent labels, electrodense reagents, enzymes, digoxigenin or haptens.

### Claim 12 (depends on 1)

The RHAMM-binding peptide of claim 1 characterized in that said RHAMM-binding peptide is conjugated to a cytotoxic molecule or radioactive molecule.

### Claim 13

(canceled)

### Claim 14

(canceled)

### Claim 15

(canceled)

### Claim 16

A probe comprising a tubulin-derived, RHAMM-binding peptide and a detectable label capable of being detected by a detection technique.

### Claim 17 (depends on 16)

The probe of claim 16 characterized in that the detectable label is selected from biotin-based labels, magnetic labels, radioactive labels, fluorescent labels, electrodense reagents, enzymes, digoxigenin or haptens.

### Claim 18 (depends on 16)

The probe of claim 16 characterized in that said tubulin-derived, RHAMM-binding peptide is conjugated to the detectable label.

### Claim 19 (depends on 16)

The probe of claim 16 characterized in that said tubulin-derived, RHAMM-binding peptide comprises a sequence having a formula EEXEEZ (SEQ ID NO: 18), wherein X is selected from alanine or glycine, and Z is selected from tyrosine or glutamic acid.

### Claim 20 (depends on 16)

The probe of claim 16 characterized in that the tubulin-derived, RHAMM-binding peptide comprises at least one of the amino acid sequences selected from the group consisting of SEQ ID NO: 1 to SEQ ID NO: 17.

### Claim 21 (depends on 16)

The probe of claim 16, characterized in that the probe is used to study cells expressing RHAMM.

### Claim 22 (depends on 16)

The probe of claim 16, characterized in that said probe is selected from SEQ ID NOs: 25, 27, 29, 31, 33 and 35.

### Claim 23 (depends on 16)

The probe of claim 16 characterized in that the tubulin-derived, RHAMM-binding peptide is conjugated to a Ga-DOTA label or to a Re(CO)3+ label.

### Claim at position 24

24-55. (canceled)

### Claim 56

An isolated peptide comprising a sequence selected from the group consisting of SEQ ID NO: 1 to SEQ ID NO: 17.

### Claim 57

(canceled)

### Claim 58 (depends on 56)

The isolated peptide of claim 56, wherein said isolated peptide is selected from the group consisting of SEQ ID NO:1 SEQ ID NO:3, SEQ ID NO:9, and SEQ ID NO: 11.

### Claim 59 (depends on 19)

The probe of claim 19, characterized in that said RHAMM-binding peptide is selected from SEQ ID NO: 1, SEQ ID NO:3, SEQ ID NO:9, and SEQ ID NO: 11.

### Claim 60 (depends on 16)

The probe of claim 16, characterized in that said probe is selected from SEQ ID NOs: 25, 27, 29, and 31.

### Claim 61 (depends on 2)

The RHAMM-binding peptide of claim 2, wherein said RHAMM-binding peptide is a tubulin-derived peptide.

### Claim 62 (depends on 2)

The RHAMM-binding peptide of claim 2 characterized in that said RHAMM-binding peptide is conjugated with a detectable label.

### Claim 63 (depends on 2)

The RHAMM-binding peptide of claim 2 characterized in that said RHAMM-binding peptide is conjugated to a cytotoxic molecule or radioactive molecule.
