Medicine fusion specifically bound with GLP-2 receptor

A technology of GLP-2 and GLP-2R, which is applied in the direction of drug combination, antipyretics, and pharmaceutical formulations, and can solve the problems of immunogenicity, reduced therapeutic effect, poor patient compliance, and large molecular size

Inactive Publication Date: 2013-03-06
HAISCO PHARMA GRP INC
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004]However, the above-mentioned conventional solutions have the following potential problems: (1) PEG-modified long-acting preparations, whose polymers are directly modified in GLP-2 or tail of its analog
Compared with GLP-2 or its analogs, the polymer has a larger molecular volume, and the steric hindrance effect will affect the effective binding of GLP-2 to its receptor (GLP-2R), resulting in a significant decrease in biological activity in vivo ; (2) The extension of the half-life of the Fc fusion polypeptide was not as significant as expected (US Pat. No. 6,756,480, incorporated herein by reference); (3) Other forms such as human albumin fusion or microspheres embedded in Risk of inducing immunogenicity in patients reducing therapeutic efficacy
[0005]Although teduglutide has been registered in the United States, the patient needs to take the drug once a day, and the patient's compliance is not good
There is currently no long-acting, highly active GLP-2 receptor agonist

Method used

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  • Medicine fusion specifically bound with GLP-2 receptor
  • Medicine fusion specifically bound with GLP-2 receptor
  • Medicine fusion specifically bound with GLP-2 receptor

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0085] This example describes the preparation of the X fragment sequence as: HGDGSFSDEMNTILDNLAARDFINWLIQTKITD (SEQ ID NO: 1),

[0086] The sequence of X' fragments is:

[0087] DTIKTQILWNIFDRAALNDLITNMEDSFSGDGH (SEQ ID NO: 5)

[0088] Y is GGGCGGG (SEQ ID NO: 3)

[0089] Z is a monomethoxypolyethylene glycol with a molecular weight of 20,000 Daltons and activated by maleic imide at the end

[0090] a and b do not exist, that is, the number of amino acid residues is 0

[0091] n=1

[0092] The preparation method of the drug fusion body, the fusion body is named HSK-B-04 in the present invention.

[0093] HSK-B-04 plasmid clone

[0094] Cloning of plasmids expressing the following protein sequences:

[0095] HGDGSFSDEMNTILDNLAARDFINWLIQTKITDGGGCGGGDTIKTQILWNIFDRAALNDLITNMEDSFSGDGH (SEQ ID NO: 6)

[0096] Primer 5' CATGCCATGGCC CAT ATG AAA TAC-3' (SEQ ID NO: 7)

[0097] 5' CCGAATTCTCATTAGTGACCGTC-3' (SEQ ID NO: 8)

[0098] The DNA sequence encoding the above...

Embodiment 2

[0108] This example describes the preparation of the X fragment sequence as:

[0109] HGDGSFSDEMNTILDNLAARDFINWLIQTKITDKKKKKK (SEQ ID NO:2),

[0110] The sequence of X' fragments is:

[0111] KKKKKKGRGKVLWAIFEKAAQGELYSSVDSTFTGEGH (SEQ ID NO: 10)

[0112] Y is GGGSGGGCGGGSGGG (SEQ ID NO: 4)

[0113] Z is a monomethoxypolyethylene glycol with a molecular weight of 30,000 Daltons and activated by maleic imide at the end

[0114] a and b do not exist, that is, the number of amino acid residues is 0

[0115] n=1

[0116] The preparation method of the drug fusion body, the fusion body is named HSK-B-05 in the present invention.

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Abstract

The invention discloses a medicine fusion bound with GLP-2R oligopeptide, and also discloses a preparation method of the medicine fusion and a method for treating inflammatory bowel diseases, Crohn diseases and short bowel syndrome by using the medicine fusion.

Description

technical field [0001] The invention belongs to the field of genetic engineering, and relates to a specific drug fusion body combined with GLP-2 receptors and its application. It mainly involves the introduction of active polypeptide fragments (X) that can effectively bind to GLP-2 receptors by means of genetic engineering n By connecting the chain with the (X) n Polypeptide fragment (X') composed of mirror image amino acid sequence n Linked together, with any modification of polymer, fatty acid and sugar modification at the linking chain. The formed drug fusion contains 2 segments of inverted repeat polypeptide fragment sequences (X) n with (X') n . The present invention also covers the application of the polypeptide and its modified product in treating inflammatory bowel disease, Crohn's disease and short bowel syndrome. Background technique [0002] The gastrointestinal tract is the main place for digestion and absorption of nutrients. When the body's gastrointestin...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K47/48A61K38/16A61K38/26C12N15/62C12N1/15C12N1/19C12N1/21C12N5/10A61P1/00A61P29/00
Inventor 于鹏展
Owner HAISCO PHARMA GRP INC
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