# US 11,999,770 B2 · Peptides and nanoparticle formulations thereof

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- Number: US 11,999,770 B2
- Document ID: US11999770B2
- Status: Granted
- Kind: B2
- Application number: 17/134,977
- Filed: 2020-12-28
- Published: 2021-06-24
- Granted: 2024-06-04
- Earliest claimed: 2016-04-29
- Assignees: University of Bradford
- Applicants: University of Bradford
- Inventors: Mohamed El-Tanani; Paul McCarron; Ahmed Faheem
- Web page: https://patentgrep.com/patent/US11999770B2

## CPC

- C07K 14/4703: {Inhibitors; Suppressors}
- A61K 9/51: Nanocapsules; {Nanoparticles; (nanotubes A61K9/0092; polymeric micelles A61K9/1075; polymersomes A61K9/1273; pure drug nanoparticles A61K9/14; drug nanoparticles with adsorbed surface modifiers A61K9/141; conjugates, e.g. between drug and non-active nanoparticles, A61K47/50; preparations for in vivo diagnosis A61K49/00; with radioactive substances A61K51/00)}
- A61K 9/5153: {Polyesters, e.g. poly(lactide-co-glycolide)}
- A61P 35/00: Antineoplastic agents
- 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 14/4722: {G-proteins}
- A61K 9/5146: {obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyethylene glycol, polyamines, polyanhydrides}
- 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 2500/02: Screening involving studying the effect of compounds C on the interaction between interacting molecules A and B (e.g. A = enzyme and B = substrate for A, or A = receptor and B = ligand for the receptor)
- 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)

## Abstract

The present invention relates to peptides, methods for production of the same, nanoparticle formulations of the same and the use of these new peptides and nanoparticle formulations as inhibitors of protein-protein interactions, in particular for application in the treatment of diseases associated with overexpression of the RAN gene.

## Claims

### Claim 1

A method for inhibiting the binding of regulator chromosome condensation 1 (RCC1) to GDP bound Ras-related nuclear proteins (RanGDP) in a subject in need thereof, wherein one or more cells of the subject overexpress Ras-related nuclear protein (RAN), comprising administering to the subject a therapeutically effective amount of a peptide comprising the amino acid sequence of SEQ ID NO:5 to inhibit the binding of RCC1 to RanGDP in the one or more cells overexpressing RAN.

### Claim 2 (depends on 1)

The method of claim 1, wherein the therapeutically effective amount is administered by direct administration as a medicine.

### Claim 3 (depends on 1)

The method of claim 1 wherein the peptide comprising the amino acid sequence of SEQ ID NO:5 is further transformed into an alternative pharmaceutically acceptable form.

### Claim 4 (depends on 3)

The method of claim 3 wherein the alternative pharmaceutically acceptable form is a nanoparticle.

### Claim 5 (depends on 3)

The method of claim 3 wherein the alternative pharmaceutically acceptable form is an antibody.

### Claim 6 (depends on 3)

The method of claim 3 wherein the alternative pharmaceutically acceptable form is an antibody-drug conjugate.

### Claim 7 (depends on 1)

The method of claim 1 wherein an administered dose is from 1 mg/day to 5000 mg/day.

### Claim 8 (depends on 1)

The method of claim 1 wherein a dose range is 1 to 100 mg/kg body weight.

### Claim 9 (depends on 1)

The method of claim 1 wherein the composition is administered from 1 to 6 times per day.

### Claim 10 (depends on 1)

The method of claim 1 wherein the composition is administered directly to a tumour site.

### Claim 11 (depends on 1)

The method of claim 1, wherein the peptide comprising the amino acid sequence of SEQ ID NO:5 is in a nanoparticle formulation.

### Claim 12 (depends on 11)

The method of claim 11, wherein the nanoparticle comprises poly(lactic-co-glycolic acid) (PLGA).

### Claim 13 (depends on 12)

The method of claim 12, wherein the nanoparticle further comprises a poly(lactic-co-glycolic acid)/polyethylene glycol (PEG) block copolymer, optionally wherein the content of PEG relative to PLGA is from 1% to 15%.

### Claim 14 (depends on 11)

The method of claim 11, wherein the nanoparticle has a mean diameter of from 100 nm to 400 nm.

### Claim 15

A method for treating triple-negative breast cancer in a subject in need thereof, comprising administering to the subject a therapeutically effective amount of a peptide comprising the amino acid sequence of SEQ ID NO: 5.

### Claim 16

A method for treating non-small cell lung cancer in a subject in need thereof, comprising administering to the subject a therapeutically effective amount of a peptide comprising the amino acid sequence of SEQ ID NO: 5.
