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Exenatide short peptide simulation peptide and application thereof in preparing medicament for curing diabetes

A technology of exenatide and therapeutic drugs, applied in the field of biopharmaceuticals, can solve problems such as insufficient control of blood sugar

Inactive Publication Date: 2008-07-09
JILIN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] At present, the artificially synthesized Exendin-4 has been jointly researched and developed by Amylin Company and Eli Lilly Company as a new type of hypoglycemic drug. Type 2 diabetics whose blood sugar is not adequately controlled

Method used

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  • Exenatide short peptide simulation peptide and application thereof in preparing medicament for curing diabetes
  • Exenatide short peptide simulation peptide and application thereof in preparing medicament for curing diabetes

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0054] Solid Phase Synthesis of Compound E1 (Gln-Pro-Ser-Val-Gly-Met-Lys-Pro-Ser-Pro-Arg-His)

[0055] Raw materials: Fmoc-Gln(Trt)-OH, Fmoc-Pro-OH, Fmoc-Ser(But)-OH, Fmoc-Val-OH, Fmoc-Gly-OH, Fmoc-Met-OH, Fmoc-Lys(Boc) -OH, Fmoc-Arg(pbf)-OH, Fmoc-His(Trt)-OH, coupling reaction condensing agent is benzotriazole-1-oxygen-tris(dimethylamino)phosphorus hexafluorophosphate (BOP) , 1-hydroxybenzotriazole (HOBT), N-methylmorpholine (NMM). The deprotecting agent is 20% piperidine / DMF solution. The cleavage reagent is trifluoroacetic acid.

[0056]Reaction: Weigh Rink Amide MBHA resin, swell the resin in DMF at room temperature for 30 minutes, and wash with DMF three times. Add 20% piperidine / DMF solution and react at room temperature for 1 hour to deprotect. Then wash with DMF three times, add Fmoc-His(Trt)-OH, react at room temperature for 3 hours, then wash with DMF three times, add 20% piperidine / DMF solution, react at room temperature for 1 hour to deprotect. Then wash with ...

Embodiment 2

[0060] Solid Phase Synthesis of Compound E2 (Ser-Val-Ser-Val-Gly-Met-Lys-Pro-Ser-Pro-Arg-Pro)

[0061] Raw materials: Fmoc-Ser(But)-OH, Fmoc-Pro-OH, Fmoc-Ser(But)-OH, Fmoc-Val-OH, Fmoc-Gly-OH, Fmoc-Met-OH, Fmoc-Lys(Boc) -OH, Fmoc-Arg(pbf)-OH, coupling reaction condensing agent is benzotriazole-1-oxo-tris(dimethylamino)phosphorus hexafluorophosphate (BOP), 1-hydroxybenzotriazole (HOBT), N-methylmorpholine (NMM). The deprotecting agent is 20% piperidine / DMF solution. The cleavage reagent is trifluoroacetic acid.

[0062] Reaction: Weigh Rink Amide MBHA resin, swell the resin in DMF at room temperature for 30 minutes, and wash with DMF three times. Add 20% piperidine / DMF solution and react at room temperature for 1 hour to deprotect. Then wash with DMF three times, add Fmoc-Pro-OH, react at room temperature for 3 hours, then wash with DMF three times, add 20% piperidine / DMF solution, react at room temperature for 1 hour to deprotect. Then wash with DMF three times, then add ...

Embodiment 3

[0066] Solid Phase Synthesis of Compound E3 (Ser-Val-Phe-Val-Gly-Met-Lys-Pro-Ser-Pro-Ser-Pro)

[0067] Raw materials: Fmoc-Ser(But)-OH, Fmoc-Pro-OH, Fmoc-Ser(But)-OH, Fmoc-Val-OH, Fmoc-Gly-OH, Fmoc-Met-OH, Fmoc-Lys(Boc) -OH, Fmoc-Phe-OH

[0068] , The coupling reaction condensing agent is benzotriazole-1-oxygen-tris(dimethylamino)phosphorus hexafluorophosphate (BOP), 1-hydroxybenzotriazole (HOBT), N-methylmorpholine ( NMM). The deprotecting agent is 20% piperidine / DMF solution. The cleavage reagent is trifluoroacetic acid.

[0069] Reaction: Weigh Rink Amide MBHA resin, swell the resin in DMF at room temperature for 30 minutes, and wash with DMF three times. Add 20% piperidine / DMF solution and react at room temperature for 1 hour to deprotect. Then wash with DMF three times, add Fmoc-Pro-OH, react at room temperature for 3 hours, then wash with DMF three times, add 20% piperidine / DMF solution, react at room temperature for 1 hour to deprotect. Then wash with DMF three ti...

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Abstract

The invention provides an exenatide short peptide and imitation peptide, which transforms the structure of exenatide, and is a novel compound. The invention further discloses a preparation process of exenatide short peptide and imitation peptide, which is suitable to be produced in industrialization. The invention further discloses an application on the preparation therapeutic medicaments of diabetes.

Description

technical field [0001] The invention discloses an exenatide short peptidomimetic peptide and a preparation method thereof, and also discloses its application in the preparation of medicines for treating diabetes, and belongs to the technical field of biopharmaceuticals. Background technique [0002] Exenatide (hereinafter referred to as: Exendin-4) involved in the present invention is a polypeptide secreted in the salivary glands of the Gila monster in the southwestern United States, containing 39 amino acids, and human glucagon-like peptide-1 (glucagon -likepeptidel, GLP-1) has 53% homology, has a high affinity with the GLP-1 receptor and has similar physiological functions. [0003] Exendin-4 has pharmacological effects such as promoting insulin secretion, inhibiting glucagon release, lowering triglyceride levels, and delaying gastric acid secretion activity. In addition, Exendin-4 can also promote pancreatic β-cell proliferation, stimulate β-cell regeneration and inhibit ...

Claims

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Application Information

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IPC IPC(8): C07K7/08C07K1/06A61K38/10A61P3/10
Inventor 李惟宋相伟王丽萍王丽凤
Owner JILIN UNIV
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