# US 2022/0033474 A1 · Structure-sensitive peptide antigen of von willebrand factor

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- Number: US 2022/0033474 A1
- Document ID: US20220033474A1
- Status: Published application
- Kind: A1
- Application number: 17/051,761
- Filed: 2019-10-11
- Published: 2022-02-03
- Earliest claimed: 2019-09-24
- Assignees: Soochow University
- Applicants: Soochow University
- Inventors: Wei DENG
- Web page: https://patentgrep.com/patent/US20220033474A1

## CPC

- C07K 14/755: Factors VIII {, e.g. factor VIII C (AHF), factor VIII Ag (VWF)}
- A61K 39/0005: {Vertebrate antigens (from snakes A61K39/38)}
- C07K 14/745: Blood coagulation or fibrinolysis factors
- C07K 16/36: against blood coagulation factors
- G01N 33/6893: {related to diseases not provided for elsewhere}
- G01N 33/86: involving blood coagulating time {or factors, or their receptors}
- C07K 2317/34: Identification of a linear epitope shorter than 20 amino acid residues or of a conformational epitope defined by amino acid residues
- G01N 2333/755: Factors VIII, e.g. factor VIII C [AHF], factor VIII Ag [VWF]
- G01N 2800/22: Haematology
- G01N 2800/224: Haemostasis or coagulation
- 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)
- 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 discloses a polypeptide antigen sequence, its spatially sensitive position in von Willebrand factor (VWF), and use thereof in the production of preparations for the diagnosis and/or treatment of VWF-related blood diseases. The polypeptide antigen comprises the amino acid sequence as shown in SEQ ID NO: 1, or a biologically active fragment or a variant thereof. The spatial position of the polypeptide transits from non-solvent exposure to solvent exposure when VWF is in activation process upon exposing to blood shear stress, so as to be recognized by an antibody. The antibody that recognizes the active state of VWF prepared by using the polypeptide antigen is useful in diagnosing and treating a variety of VWF-related diseases.

## Claims

### Claim 1

Use of a peptide antigen in the production of preparations for diagnosis and/or treatment of blood diseases associated with von Willebrand factor (VWF), wherein the peptide antigen comprises the amino acid sequence as shown in SEQ ID NO: 1, or a biologically active fragment or variant thereof, and the peptide antigen is derived from the A1 domain of human VWF.

### Claim 2 (depends on 1)

The use according to claim 1, wherein the peptide antigen is located in the loop region between the β3 fold and α2 helix in the A1 domain of VWF.

### Claim 3 (depends on 1)

The use according to claim 1, wherein when VWF is in an active state, the peptide antigen is recognized by a specific antibody thereof.

### Claim 4 (depends on 1)

The use according to claim 1, wherein the peptide antigen is derived from human.

### Claim 5 (depends on 1)

The use according to claim 1, wherein the preparation is a vaccine composition, an antibody drug or a diagnostic kit.

### Claim 6

An antibody, wherein the antibody specifically recognizes a peptide antigen comprising the amino acid sequence as shown in SEQ ID NO: 1, or a biologically active fragment or a variant thereof.

### Claim 7 (depends on 6)

The antibody according to claim 6, wherein the antibody recognizes VWF in an active state; and the peptide antigen is derived from the A1 domain of human VWF.

### Claim 8 (depends on 6)

A diagnostic preparation, for determining whether a peptide antigen having the amino acid sequence as shown in SEQ ID NO: 1 is present in a sample, comprising the antibody according to claim 6.

### Claim 9 (depends on 1)

A therapeutic preparation, for recognizing and inhibiting VWF in an active state, comprising the antibody according to claim 1.