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Gerobriecin pancrease glucagon peptidel (SGLP-1), its preparation and use

A glucagon-reactive technology, applied in the field of glucagon-like peptide 1 analogues, can solve the problems of high cost, long half-life, failure, etc., and achieve improved hypoglycemic effect, prolonged half-life, and better stimulation of insulin secretion The effect of action

Active Publication Date: 2008-03-12
DALIAN D N BIO ENG
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] Exendin4 has a long half-life in the human body and has an obvious hypoglycemic effect. However, the chemically synthesized Exendin4 is a peptide composed of 39 amino acids, which is expensive. Moreover, as a heterologous polypeptide, long-term use may induce the body to produce corresponding antibodies and may fail

Method used

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  • Gerobriecin pancrease glucagon peptidel (SGLP-1), its preparation and use
  • Gerobriecin pancrease glucagon peptidel (SGLP-1), its preparation and use

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0024] Synthesize sGLP-1 according to the following method, and its sequence is as follows:

[0025] His-Gly-Glu-Gly-Thr-Phe-Thr-Ser-Asp-Val-Ser-Ser-Tyr-Leu-Glu-Gly-Gln-Ala-Ala-Lys-Glu-Phe-Ile-Ala-Trp- Leu

[0026] Step 1: Synthesis of sGLP-1 peptide resin:

[0027]Weigh 0.5 gram of Wang resin (or other polypeptide synthetic resins) and pour it into the synthesis reaction column, add dimethylformamide solvent to swell, and weigh 0.1 gram of FMOC (9 pyrene) successively according to the amino acid sequence of the hypoglycemic peptide of the present invention methoxycarbonyl amino acid N-terminal protection) in the container of the reactor, according to the solid-phase chemical synthesis method invented by Merrifield (the specific method is as follows) according to the amino acid sequence of sGLP-1 of the present invention, starting from the C-terminus, in order In the synthesis reaction column, add the 4ml N that dissolves with the dimethylformamide of 10ml, N diisopropylcarb...

Embodiment 2

[0033] Synthesize sGLP-1 according to the method described in Example 1, and its sequence is as follows:

[0034] His-Ser-Glu-Gly-Thr-Phe-Thr-Ser-Asp-Val-Ser-Ser-Tyr-Leu-Glu-Gly-Gln-Ala-Ala-Lys-Glu-Phe-Ile-Ala-Trp- Leu.

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Abstract

SGLP-1, its production and use are disclosed. The sGLP-1 contains 26 amino acids. Its sequence is as following: His-X1-Glu-Gly-Thr-Phe-Thr-Ser-Asp-Val-Ser-ser-Tyr-Leu-Glu-Gly-Gln-Ala-Ala-Lys-Glu-Phe-Ile-Ala-Trp-Leu. It is cheap, has better binding ability with insulin receptor, stronger drug effect and to resist dipeptide peptase degradation.

Description

Technical field: [0001] The present invention relates to an analogue of glucagon-like peptide-1 (GLP-1) that stimulates insulin secretion, and also relates to its preparation method and application. Background technique: [0002] In recent years, the research on insulin secretory peptide GLP-1 and Exendin4 has progressed rapidly. The two have high homology, and they have achieved good results in the treatment of type II diabetes. GLP-1 is a polypeptide isolated and purified from the human intestine, and Exendin4 is a short peptide isolated from the venom of the Mexican monitor lizard. The two can promote the synthesis and secretion of insulin by the pancreas at very low concentrations, thus helping diabetics to control blood sugar. [0003] GLP-1 is an intestinal hormone secreted by the human body, which is produced by proglucagon molecules through the action of intestinal proteolytic enzymes, so it is called glucagon peptides. When the blood sugar concentration is higher ...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07K14/605C07K1/00A61K38/26A61K9/08A61K9/20A61K9/48A61P3/10
CPCA61K38/00C07K14/61C07K14/605A61P3/10
Inventor 李元黄庆生李别虎张虎明张明杰薛小平王延竹韩文君张卫华张胜军
Owner DALIAN D N BIO ENG
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