# US 11,299,524 B2 · KIF13B-derived peptide and method of inhibiting angiogenesis

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- Number: US 11,299,524 B2
- Document ID: US11299524B2
- Status: Granted
- Kind: B2
- Application number: 16/325,006
- Filed: 2017-08-31
- Published: 2019-06-06
- Granted: 2022-04-12
- Earliest claimed: 2016-09-02
- Assignees: The Board of Trustees of the University of Illinois
- Applicants: The Board of Trustees of the University of Illinois
- Inventors: Kaori Yamada; Asrar Malik
- Web page: https://patentgrep.com/patent/US11299524B2

## CPC

- C07K 14/435: from animals; from humans
- 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 38/17: from animals; from humans {(enzyme inhibitors A61K38/005)}
- A61K 47/543: {Lipids, e.g. triglycerides; Polyamines, e.g. spermine or spermidine}
- A61K 47/549: {Sugars, nucleosides, nucleotides or nucleic acids}
- A61P 9/00: Drugs for disorders of the cardiovascular system
- C07H 23/00: Compounds containing boron, silicon or a metal, e.g. chelates or vitamin B12 (esters with inorganic acids C07H11/00)
- C12N 9/14: Hydrolases (3)
- C07K 2319/10: containing a tag for extracellular membrane crossing, e.g. TAT or VP22
- 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
- C07H: SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS (derivatives of aldonic or saccharic acids C07C, C07D; aldonic acids, saccharic acids C07C59/105, C07C59/285; cyanohydrins C07C255/16; glycals C07D; compounds of unknown constitution C07G; polysaccharides, derivatives thereof C08B; DNA or RNA concerning genetic engineering, vectors, e.g. plasmids, or their isolation, preparation or purification C12N15/00; sugar industry C13)
- C12N: MICROORGANISMS OR ENZYMES; COMPOSITIONS THEREOF; PROPAGATING, PRESERVING, OR MAINTAINING MICROORGANISMS; MUTATION OR GENETIC ENGINEERING; CULTURE MEDIA (microbiological testing media C12Q1/00)

## Abstract

A construct composed of a Kinesin-derived Angiogenesis Inhibitor peptide and one or more carrier moieties and/or stabilizing moieties is provided as are methods for inhibiting angiogenesis and treating a disease or condition characterized by excessive vascularity.

## Claims

### Claim 1

A construct of no more than 65 amino acids comprising the amino acid sequence Thr-Pro-Xaa1-Asp-Glu-Arg-Xaa2-Xaa3-Leu-Ile-Xaa4-Arg-Val-Xaa5-Val-Xaa6 (SEQ ID NO:2) operably linked to
(a) one or more carrier moieties,
(b) one or more stabilizing moieties, or
(c) a combination of (a) and (b),
wherein Xaa1 is Val, Ala or Ser; Xaa2 is Leu or Val; Xaa3 is Phe or Tyr; Xaa4 is Leu or Val; Xaa5 is Thr or Ala; and Xaa6 is Gln or Arg.

### Claim 2 (depends on 1)

The construct of claim 1, wherein the one or more carrier moieties comprise a cell penetrating peptide, a lipid, Vitamin12, or a combination thereof.

### Claim 3 (depends on 2)

The construct of claim 2, wherein the cell penetrating peptide comprises a peptide of SEQ ID NO:4-60.

### Claim 4 (depends on 1)

The construct of claim 1, wherein the one or more stabilizing moieties comprise a peptide, post-translational modification, non-natural amino acid residue, a macromolecule or a combination thereof.

### Claim 5 (depends on 4)

The construct of claim 4, wherein the post-translational modification comprises N-terminal acetylation or C-terminal amidation.

### Claim 6 (depends on 4)

The construct of claim 4, wherein the non-natural amino acid residue comprises a D-amino acid residue.

### Claim 7 (depends on 4)

The construct of claim 4, wherein the macromolecule comprises polyethylene glycol, polysialic acid, hydroxyethyl starch, albumin or an immunoglobulin fragment.

### Claim 8 (depends on 1)

The construct of claim 1, wherein said construct comprises the amino acid sequence TPVDERLFLIVRVTVQ (SEQ ID NO:3).

### Claim 9 (depends on 8)

The construct of claim 8, wherein said construct is SRGTPVDERLFLIVRVTVQLSHP-NH2 (SEQ ID NO:113).

### Claim 10 (depends on 1)

A pharmaceutical composition comprising the construct of claim 1 and a pharmaceutically acceptable excipient.

### Claim 11 (depends on 1)

A method for inhibiting angiogenesis comprising contacting cells or tissue with an effective amount of a construct of claim 1 thereby inhibiting angiogenesis in the cells or tissue.

### Claim 12 (depends on 1)

A method of treating a disease or condition in a subject characterized by excessive vascularity comprising administering to the subject an effective amount of a construct of claim 1 thereby treating the disease or condition.

### Claim 13 (depends on 12)

The method of claim 12, wherein the disease or condition is an inflammatory disease, cancer, or retinal vasculopathy.
