# US 10,501,498 B2 · Conotoxin peptide κ-CPTx-BTL01, preparation method therefor, and uses thereof

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- Number: US 10,501,498 B2
- Document ID: US10501498B2
- Status: Granted
- Kind: B2
- Application number: 15/539,709
- Filed: 2014-12-26
- Published: 2018-07-05
- Granted: 2019-12-10
- Earliest claimed: 2014-12-26
- Assignees: Bgi Shenzhen
- Applicants: Bgi Shenzhen
- Inventors: Jie Liu; Zhilong Lin; Bo Wen; Ting Tong; Fen Mo; Chao Peng; Qiong Shi
- Web page: https://patentgrep.com/patent/US10501498B2

## CPC

- C07K 14/003: {Peptide-nucleic acids (PNAs)}
- A61K 38/02: Peptides of undefined number of amino acids; Derivatives thereof
- A61K 38/10: Peptides having 12 to 20 amino acids {(A61K38/043 - A61K38/046 take precedence)}
- A61P 9/00: Drugs for disorders of the cardiovascular system
- C07K 1/00: General methods for the preparation of peptides {, i.e. processes for the organic chemical preparation of peptides or proteins of any length}
- C07K 7/08: having 12 to 20 amino acids (gastrins C07K14/595; somatostatins C07K14/655; melanotropins C07K14/68)
- C12N 5/10: Cells modified by introduction of foreign genetic material
- C12N 15/63: Introduction of foreign genetic material using vectors; Vectors; Use of hosts therefor; Regulation of expression
- C07K 17/00: Carrier-bound or immobilised peptides (carrier-bound or immobilised enzymes C12N11/00); Preparation thereof
- 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
- C12N: MICROORGANISMS OR ENZYMES; COMPOSITIONS THEREOF; PROPAGATING, PRESERVING, OR MAINTAINING MICROORGANISMS; MUTATION OR GENETIC ENGINEERING; CULTURE MEDIA (microbiological testing media C12Q1/00)

## Abstract

Provided is a new conotoxin peptide κ-CPTx-bt101. The conotoxin peptide κ-CPTx-bt101 has derivative polypeptide that has an amino acid sequence indicated by SEQ ID NO:1, or has derivative polypeptide that has an amino acid sequence indicated by SEQ ID NO:1 and that is formed after substitution, addition or deletion of one or more amino acids are performed and has original functions. Also provided is polynucleotide for coding the peptide, comprising a constructed body of the polynucleotide, an expression carrier and transformed cells. A peptide preparation method and uses in the treatment of diseases related to a calcium ion channel.

## Claims

### Claim 1

A conotoxin peptide κ-CPTx-bt101, which is:
a polypeptide derived from polypeptide (a), which consists of the amino acid sequence as set forth in SEQ ID NO:1, by substitution of one or more amino acids therein and having the function of polypeptide (a), wherein the substitution of the one or more amino acids is selected from the group consisting of:
(i) substitution of the lysine at position 1 with arginine;
(ii) substitution of the threonine at position 4 with serine;
(iii) substitution of the valine at position 7 with leucine or isoleucine;
(iv) substitution of the glutamine at position 9 with asparagine;
(v) substitution of the valine at position 13 with leucine or isoleucine; and
(vi) substitution of the threonine at position 15 with serine.

### Claim 2 (depends on 1)

A method to inhibiting a high-voltage activated calcium ion channel comprising administration, to a subject, an effective amount of the conotoxin peptide κ-CPTx-bt101 according to claim 1.

### Claim 3 (depends on 1)

A method for producing the conotoxin peptide κ-CPTx-bt101 according to claim 1, which comprises:
(1) synthesizing the linear peptide of the conotoxin peptide κ-CPTx-bt101 according to its amino acid sequence by solid-phase chemical synthesis; and
(2) performing oxidative refolding of the linear peptide obtained in step (1) with glutathione method.

### Claim 4 (depends on 3)

The method according to claim 3, wherein the solid-phase chemical synthesis is fluorenylmethoxycarbonyl solid-phase chemical synthesis.