# US 10,441,628 B2 · High activity tumour inhibitor and preparation method and use thereof

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- Number: US 10,441,628 B2
- Document ID: US10441628B2
- Status: Granted
- Kind: B2
- Application number: 15/519,753
- Filed: 2015-10-15
- Published: 2017-11-09
- Granted: 2019-10-15
- Earliest claimed: 2014-10-17
- Assignees: Bao Kang Biomedical Healthcare Inc
- Applicants: Bao Kang Biomedical Healthcare Inc
- Inventors: Kangshan Li
- Web page: https://patentgrep.com/patent/US10441628B2

## CPC

- A61K 38/16: Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof {(enzyme inhibitors A61K38/005)}
- A61K 38/10: Peptides having 12 to 20 amino acids {(A61K38/043 - A61K38/046 take precedence)}
- A61P 35/00: Antineoplastic agents
- C07K 7/08: having 12 to 20 amino acids (gastrins C07K14/595; somatostatins C07K14/655; melanotropins C07K14/68)
- C07K 14/00: Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
- 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 in the present invention are a YAP protein inhibiting polypeptide and application thereof. In particular, the present invention obtains a key binding site of YAP protein and TEAD, screens a polypeptide with best YAP inhibitory activity and modifies the polypeptide, such as adding a disulfide linkage, replacing an amino acid, removing and/or adding (for example, adding a cell-penetrating element), and finally screens and verifies the obtaining of a series of polypeptides with YAP protein activity inhibiting effect and good stability. Experiments show that the polypeptide of the present invention can effectively inhibit the binding activity between YAP protein and TEAD, thus providing good therapeutic effect on digestive tract tumors (especially liver cancer).

## Claims

### Claim 1

An isolated polypeptide having the sequence as shown in SEQ ID NO: 37.

### Claim 2

A modified polypeptide which is formed by acylation of a polypeptide having the sequence of SEQ ID NO: 37.

### Claim 3 (depends on 2)

The modified polypeptide of claim 2, which has a structure as shown in formula B:
P0-XG formula B
wherein XG represents C10-C24 acyl, and P0 represents the sequence of SEQ ID NO: 37.

### Claim 4

A pharmaceutical composition comprising a polypeptide having the sequence of SEQ ID NO: 37 or an acylated polypeptide of a polypeptide having the sequence of SEQ ID NO: 37 or a pharmaceutically acceptable salt of the polypeptide or the acylated polypeptide as an active ingredient.