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Modifications of exenatide and their applications

A technology of exenatide and modifiers, which is applied in the field of exenatide modifiers, can solve the problems of heavy burden and unsatisfactory effect, and achieve the effects of long half-life, high affinity and activating ability, and long-lasting effect

Active Publication Date: 2021-12-03
CHANGCHUN BCHT BIOTECH +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] Compared with exenatide, the above exenatide analogs prolong the hypoglycemic time and reduce the frequency of administration to a certain extent, but the effect is still not ideal. For patients suffering from diabetes for a long time, it is recommended to give The frequency of medication is still high, and the physical, psychological and economic burdens on patients are still heavy

Method used

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  • Modifications of exenatide and their applications
  • Modifications of exenatide and their applications
  • Modifications of exenatide and their applications

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0038] Example 1: Modifications of Exenatide of the present invention

[0039] The modification of Exenatide provided in this example has the chemical formula:

[0040] (Palmitic Acid) His-Gly-Glu-Gly-Thr-Phe-Thr-Ser-Asp-Leu-Ser-Lys-Gln-Met-Glu-Glu-Glu-Ala-Val-Arg-Leu-Phe-Ile- Glu-Trp-Leu-Lys-Asn-Gly-Gly-Pro-Ser-Ser-Gly-Ala-Pro-Pro-Pro-Pro-Ser-NH 2

[0041] Preparation:

[0042] Table 1 The protected amino acids and their abbreviations and English abbreviations required for solid-phase synthesis of exenatide by Fmoc method

[0043]

[0044]

[0045] Exenatide was synthesized by Fmoc solid-phase synthesis, using Fmoc-Rink MBHA Amide resin, using 20% ​​piperidine / N,N-dimethylformamide (DMF) to remove Fmoc, and the coupling reagent was hydroxybenzene Oxytriazole (HOBT) / N,N-diisopropylcarbodiimide (DIC), DMF is the reaction solvent, and the reaction monitoring adopts the ninhydrin detection method. The following protected amino acids are connected to the Rink MBHA Amide ...

Embodiment 2

[0047] Example 2: Modifications of Exenatide of the present invention

[0048] The modification of Exenatide provided in this example has the chemical formula:

[0049] (lauric acid) His-Gly-Glu-Gly-Thr-Phe-Thr-Ser-Asp-Leu-Ser-Lys-Gln-Met-Glu-Glu-Glu-Ala-Val-Arg-Leu-Phe-Ile- Glu-Trp-Leu-Lys-Asn-Gly-Gly-Pro-Ser-Ser-Gly-Ala-Pro-Pro-Pro-Pro-Ser-NH 2

Embodiment 3

[0050] Example 3: Modifications of Exenatide of the present invention

[0051] (Palmitic Acid) His-Gly-Glu-Gly-Thr-Phe-Thr-Ser-Asp-Leu-Ser-Lys-Gln-Met-Glu-Trp-Glu-Ala-Val-Arg-Leu-Phe-Ile- Glu-Trp-Leu-Lys-Asn-Phe-Gly-Pro-Ser-Ser-Gly-Ala-Pro-Pro-Pro-Pro-Ser-NH 2

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Abstract

The invention relates to the field of biotechnology, in particular to a modified exenatide and its application. In the present invention, modified exenatide is obtained by modifying the N-terminal amino acid amino group of exenatide and its functional equivalents with fatty acid. It has been verified by experiments that compared with exenatide, this modification not only retains the agonistic ability with the GLP-1 receptor, but also can tolerate the degradation of the peptide chain by various enzymes, the half-life is significantly prolonged, and its critical micelle concentration Significantly lower than exenatide polypeptide and other modified products, it has a longer-lasting hypoglycemic effect.

Description

technical field [0001] The invention relates to the field of biotechnology, in particular to a modification of exenatide and an application thereof. Background technique [0002] Exenatide (also known as Exenatide or Exenatide, Exenatide, or Exendin-4), a polypeptide composed of 39 amino acids, its amino acid sequence is: His-Gly-Glu-Gly-Thr-Phe- Thr-Ser-Asp-Leu-Ser-Lys-Gln-Met-Glu-Glu-Glu-Ala-Val-Arg-Leu-Phe-Ile-Glu-Trp-Leu-Lys-Asn-Gly-Gly-Pro- Ser-Ser-Gly-Ala-Pro-Pro-Pro-Ser-NH 2 . Exenatide, as an effective human glucagon-like peptide-1 (GLP-1) receptor agonist, can be used to treat various diseases related to GLP-1 receptor, such as exenatide can simulate GLP The glucose regulating effect of -1 is used in the treatment of type II diabetes. Unlike other hypoglycemic drugs, exenatide increases insulin synthesis and secretion only in the presence of glucose, greatly reducing the risk of hypoglycemia. Therefore, exenatide is favored as an effective hypoglycemic drug. H...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07K14/575A61K38/22A61P3/10A61P3/04A61P9/12A61P3/06A61P9/00A61P25/28A61P25/16
CPCA61K38/00A61P3/04A61P3/06A61P3/10A61P9/00A61P9/12A61P25/16A61P25/28C07K14/57563C07K19/00
Inventor 张勇孔维陈妍
Owner CHANGCHUN BCHT BIOTECH
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