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Long-acting African clawed frog glucagon-like peptide-1 (GLP-1) analogue and application thereof

A technology of glucagon and Xenopus laevis, which is applied in the field of long-acting Xenopus glucagon-like peptide-1 analogs, can solve the problem of reducing the immunogenicity of heterologous proteins, increasing the molecular weight of protein drugs, and reducing the risk of kidney failure. Problems such as globular filtration rate, to achieve the effect of prolonging the time of hypoglycemic action in the body, reducing immunogenicity, and lowering blood sugar

Pending Publication Date: 2017-05-24
XUZHOU NORMAL UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

At present, the methods for prolonging the half-life of polypeptide and protein drugs are mainly based on three principles: 1, increase the molecular weight of protein drugs, reduce the glomerular filtration rate; Slowly release the free protein drug, so that the balance between the bound drug and the free drug moves toward the free drug; 3. Reduce the immunogenicity of the heterologous protein, thereby reducing its clearance rate in the body

Method used

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  • Long-acting African clawed frog glucagon-like peptide-1 (GLP-1) analogue and application thereof
  • Long-acting African clawed frog glucagon-like peptide-1 (GLP-1) analogue and application thereof
  • Long-acting African clawed frog glucagon-like peptide-1 (GLP-1) analogue and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0075] His-Gly-Glu-Gly-Thr-Tyr-Thr-Asn-Asp-Val-Cys(S-PEG anolog)-Glu-Tyr-Leu-Glu-Glu-Lys-Ala-Ala-Lys-Glu-Phe- Ile-Glu-Trp-Leu-Ile-Lys-Gly-Lys-NH 2 (SEQ. ID NO:2)

[0076] Solid-phase synthesis of (0.1mmol)

[0077] (1) Swelling of the resin

[0078] Weigh 0.262g of Fmoc-Rink amide-MBHA Resin (substitution amount 0.382mmol / g), swell with 7mL DCM for 2min, remove DCM by suction filtration, then swell with 10mL DCM for 30min, and finally rinse with DCM and DMF 7mL respectively.

[0079] (3) Removal of Fmoc protecting group

[0080] Put the swollen resin into the reactor, add 7mL of 20% piperidine / DMF (V / V) solution, shake back and forth at 180°C for 5min in the reactor, the reaction temperature is 25°C, filter the solution after the reaction; Add 7 mL of 20% piperidine / DMF (V / V) solution and shake back and forth at 180°C for 15 min in the reactor at a reaction temperature of 25°C. After the reaction, the solution was filtered off and washed with DMF. A resin free of the ini...

Embodiment 2～10

[0093] According to the method described in Example 1, the Xenopus laevis glucagon-like peptide-1 (GLP-1) analogues of Examples 2-10 were synthesized according to the corresponding sequences, and their respective molecular weights were confirmed by ESI-MS.

Embodiment 2

[0095] His-Gly-Glu-Gly-Thr-Tyr-Thr-Asn-Asp-Val-Thr-Cys(S-PEG anolog)-Tyr-Leu-Glu-Glu-Lys-Ala-Ala-Lys-Glu-Phe- Ile-Glu-Trp-Leu-Ile-Lys-Gly-Lys-NH 2 (SEQ. ID NO:3)

[0096] The average theoretical relative molecular mass is 5460.0. ESI-MS m / z:calu[M+4H] 4+ 1366.0, [M+5H] 5+ 1093.0;found[M+4H] 4+ 1365.7, [M+5H] 5+ 1092.6.

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Abstract

The invention relates to a long-acting African clawed frog glucagon-like peptide-1 (GLP-1) analogue as well as a synthesis method and application thereof. An African clawed frog glucagon-like peptide-1 is subjected to PEG (Polyethylene Glycol) modification to obtain the African clawed frog GLP-1 analogue which can keep blood glucose lowering activity and has longer pharmacological action time. The African clawed frog GLP-1 analogue provided by the invention is high in synthesis yield and low in cost; and the half-life period of the analogue is remarkably prolonged and the biological activity is remarkably improved.

Description

technical field [0001] The present invention relates to a long-acting Xenopus laevis glucagon-like peptide-1 (GLP-1) analog and its application. Background technique [0002] Diabetes Mellitus (Diabetes Mellitus) is a chronic systemic disease related to genetic factors and a variety of environmental factors. Insulin-dependent diabetes mellitus (type 1) and non-insulin-dependent diabetes mellitus (type 2), in which type 2 patients account for more than 80% of diabetes cases. Diabetes is a global high incidence. According to the World Health Organization, the number of diabetic patients worldwide will reach 300 million by 2025. A recent epidemiological survey report in China shows that the prevalence of diabetes in China is as high as 9.7%, which is much higher than the global average prevalence of 6.4%. According to this prevalence rate, the number of people with diabetes in my country has exceeded 90 million, and there are also There are approximately 150 million people at ...

Claims

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Application Information

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IPC IPC(8): C07K14/605C07K1/16A61K38/26A61K47/60A61P3/10A61P3/04
CPCA61K38/26C07K14/605
Inventor 韩京傅俊杰崔旭周凤费颖颖张莹司鹏斌
Owner XUZHOU NORMAL UNIVERSITY
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