# US 10,869,910 B2 · Molecular design of recombinant protein drug

> Agents: this data is available as JSON from the patentgrep API and MCP server — see https://patentgrep.com/llms.txt

- Number: US 10,869,910 B2
- Document ID: US10869910B2
- Status: Granted
- Kind: B2
- Application number: 15/550,751
- Filed: 2016-02-14
- Published: 2018-07-19
- Granted: 2020-12-22
- Earliest claimed: 2015-02-13
- Assignees: Tsinghua University; Beijing Protgen Ltd.
- Applicants: Tsinghua University; Beijing Protgen Ltd.
- Inventors: Yongzhang Luo; Peng Liu; Xinan Lu
- Web page: https://patentgrep.com/patent/US10869910B2

## CPC

- A61K 38/1891: {Angiogenesic factors; Angiogenin}
- A61K 38/17: from animals; from humans {(enzyme inhibitors A61K38/005)}
- A61K 47/10: Alcohols; Phenols; Salts thereof, e.g. glycerol; Polyethylene glycols [PEG]; Poloxamers; PEG/POE alkyl ethers
- A61K 47/50: the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
- A61P 5/50: for increasing or potentiating the activity of insulin
- A61P 35/00: Antineoplastic agents
- C07K 14/435: from animals; from humans
- C07K 14/78: Connective tissue peptides, e.g. collagen, elastin, laminin, fibronectin, vitronectin or cold insoluble globulin [CIG]
- 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

Provided is a mutant of an endostatin. The mutant has improved ATPase activity and improved activity of inhibiting angiogenesis and inhibiting tumors. Further provided is use of the mutant in treatment of angiogenesis related diseases such as tumors.

## Claims

### Claim 1

A method for increasing the anti-angiogenesis activity of an endostatin or variant thereof, comprising genetically engineering the A motif of the endostatin or variant thereof, to obtain an endostatin mutant with increased ATPase activity compared to the endostatin or variant thereof, wherein said endostatin mutant comprises the sequence set forth in SEQ ID NO: 3.

### Claim 2 (depends on 1)

The method of claim 1, further comprising covalently linking said mutant to a PEG molecule.

### Claim 3 (depends on 2)

The method of claim 2, wherein said PEG molecule has a molecular weight of 5-40 kD.

### Claim 4 (depends on 2)

The method of claim 2, wherein said PEG molecule is covalently linked to the α-amino group at the N-terminal of said mutant.

### Claim 5 (depends on 2)

The method of claim 2, wherein said PEG molecule is monomethoxypolyethylene glycol.

### Claim 6 (depends on 2)

The method of claim 2, wherein said PEG molecule is monomethoxypolyethylene glycol propionaldehyde (mPEG-ALD).

### Claim 7 (depends on 1)

The method of claim 1, further comprising administering said mutant to a subject in need thereof for inhibiting endothelial cell migration in the subject.