# US 8,541,378 B2 · Recombinant albumins fused with poly-cysteine peptide and the methods for preparing the same

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

- Number: US 8,541,378 B2
- Document ID: US8541378B2
- Status: Granted
- Kind: B2
- Application number: 12/792,186
- Filed: 2010-06-02
- Published: 2010-12-09
- Granted: 2013-09-24
- Earliest claimed: 2009-06-05
- Assignees: Korea Institute of Science and Technology
- Applicants: Hyung Jun Ahn; Ick Chan Kwon; Kuiwon Choi; Kwangmyeng Kim; Inchan Youn; Sehoon Kim
- Inventors: Hyung Jun Ahn; Ick Chan Kwon; Kuiwon Choi; Kwangmyeng Kim; Inchan Youn; Sehoon Kim
- Web page: https://patentgrep.com/patent/US8541378B2

## CPC

- C07K 14/76: Albumins
- A61K 47/643: {Albumins, e.g. HSA, BSA, ovalbumin or a Keyhole Limpet Hemocyanin [KHL]}
- C07K 14/765: Serum albumin, e.g. HSA
- C07K 2319/20: containing a tag with affinity for a non-protein ligand
- 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)

## Abstract

The present invention relates to recombinant albumins fused with poly-cysteine peptide and methods for preparing the same, more precisely recombinant albumins in which cysteines that can be used for drug binding are amplified at N-terminal and C-terminal of the albumin and methods for preparing the same. The recombinant albumin of the present invention demonstrates improved albumin-drug conjugation efficiency when it is used for drug delivery system, indicating that it can effectively deliver a large amount of drug to a target tissue. At the same time, the recombinant albumin of the present invention can be used as an excellent drug deliverer with reduced side effects, compared with the conventional albumin carriers, by regulating the amount of drug conjugated to each unit of albumin by regulating the number of cysteine fused thereto. In addition, the recombinant albumin of the present invention can be used for the screening of a novel drug and for the non-invasive real-time diagnosis and treatment of disease by combining with a fluorescent material or a contrast agent for molecular imaging.

## Claims

### Claim 1

A recombinant albumin fused with a poly-cysteine peptide, wherein the poly-cysteine peptide has the sequence represented by SEQ. ID. NO. 1 or NO. 2.

### Claim 2 (depends on 1)

The recombinant albumin according to claim 1, wherein the albumin is human albumin represented by SEQ. ID. NO. 5.

### Claim 3 (depends on 1)

The recombinant albumin according to claim 1, wherein the poly-cysteine peptide is fused with the N-terminus of the albumin.

### Claim 4 (depends on 1)

The recombinant albumin according to claim 1, wherein a linker peptide is additionally included between albumin and the poly-cysteine peptide.

### Claim 5 (depends on 4)

The recombinant albumin according to claim 4, wherein the linker peptide has the sequence represented by SEQ. ID. NO. 3.

### Claim 6 (depends on 3)

The recombinant albumin according to claim 3, wherein a target tissue recognition ligand is covalently conjugated to the N-terminus of the poly-cysteine peptide.

### Claim 7 (depends on 6)

The recombinant albumin-drug conjugates prepared by combining a drug with the recombinant albumin of claim 6.

### Claim 8 (depends on 7)

The recombinant albumin-drug conjugate according to claim 7, wherein the drug is an anticancer agent, siRNA or a therapeutic agent.

### Claim 9 (depends on 7)

A pharmaceutical composition comprising the recombinant albumin-drug conjugate of claim 7.

### Claim 10 (depends on 6)

The polypeptide of claim 6 further comprising a covalently conjugated fluorophore.

### Claim 11

A recombinant albumin fused with a poly-cysteine peptide, wherein the resulting polypeptide has the sequence represented by SEQ. ID. NO. 4.

### Claim 12 (depends on 7)

A method for in vivo delivery of the conjugates containing the step of administering the recombinant albumin-drug conjugates of claim 7 into a subject.