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Cholic acid-XenGLP-1 (xenopus glucagon-like peptide-1) conjugated peptide and application thereof

A technology of glucagon and Xenopus laevis, applied in the direction of glucagon, hormone peptide, specific peptide, etc., can solve the problem of restricting new GLP-1 receptor agonists, etc., and achieve the effect of hypoglycemic effect time and weight loss Excellent and high in vitro stability effect

Inactive Publication Date: 2018-02-16
XUZHOU NORMAL UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

At present, most of the research on GLP-1 receptor agonists is based on the structural modification and chemical modification of the GLP-1 peptide sequence to prolong its half-life, which greatly limits the ability of novel GLP-1 receptors to be affected. Development of body agonists

Method used

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  • Cholic acid-XenGLP-1 (xenopus glucagon-like peptide-1) conjugated peptide and application thereof
  • Cholic acid-XenGLP-1 (xenopus glucagon-like peptide-1) conjugated peptide and application thereof
  • Cholic acid-XenGLP-1 (xenopus glucagon-like peptide-1) conjugated peptide and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0038]

[0039] (1) Swelling of the resin

[0040] Weigh 0.262g (0.1mmol) of Rink Amide MBHA resin with a loading capacity of 0.382mmol / g, put it into a 25mL reactor, wash the resin once with 7mL of DCM and methanol alternately, and wash the resin twice with 7mL of DCM, The resin was then swollen with 7 mL of DCM for 1 h, and finally the resin was washed 3 times with 7 mL of DMF.

[0041] (2) Removal of resin Fmoc protecting group

[0042] Transfer the swollen resin to a peptide synthesizer, add 7 mL of 20% piperidine / DMF to react at room temperature for 5 min, filter off the deprotection solution, wash the resin once with 7 mL of DMF, add 7 mL of 20% piperidine / DMF to deprotect and wash the resin for 15 min, and finally Wash the resin 4 times with 7 mL DMF, 1.5 min each time, to obtain the Rink resin from which the Fmoc protecting group has been removed.

[0043] (3) Synthesis of Fmoc-Lys-Rink amide-MBHAResin

[0044] Weigh Fmoc-Lys(Boc)-OH (0.4mmol), dissolve it with 3mL...

Embodiment 2～6

[0054] According to the method described in Example 1, the XenGLP-1 analogs of Examples 2-6 were synthesized according to the corresponding sequences and side chains, and their respective molecular weights were confirmed by ESI-MS.

Embodiment 2

[0056]

[0057] The theoretical relative molecular mass is 4185.3. ESI-MS m / z:calu[M+3H] 3+ 1396.1,[M+4H] 4+ 1047.3;found[M+3H] 3+ 1396.8,[M+4H] 4+ 1047.8.

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Abstract

The invention relates to a cholic acid-XenGLP-1 (xenopus glucagon-like peptide-1) conjugated peptide and an application thereof. Side chains of XenGLP-1 are subjected to structural modification, a cholic acid micromolecular derivative with a high serum protein binding ratio is introduced, and the XenGLP-1 conjugated peptide with higher hypoglycemic activity and longer pharmacological action time is obtained. The XenGLP-1 conjugated peptide has significantly improved bioactivity and high long-term hypoglycemic and weight losing functions.

Description

technical field [0001] The invention relates to a class of Xenopus glucagon-like peptide-1 (XenGLP-1) analogs and applications thereof Background technique [0002] Diabetes mellitus (DM) is a global endocrine and metabolic disease, manifested in metabolic disorders of sugar, fat, and protein and acid-base imbalance in the body caused by insufficient insulin secretion, and is characterized by elevated blood sugar levels. According to the lack and damage of insulin in the body, diabetes is divided into: type 1 diabetes, type 2 diabetes, gestational diabetes and other types of diabetes. Among them, type 2 diabetes accounted for 90%. According to the statistics of the International Diabetes Federation (IDF), there were about 415 million people with diabetes worldwide in 2015, and 1 in every 11 people had diabetes. It is predicted that by 2040, there will be 642 million people with diabetes worldwide, and 151 million people with diabetes in China. At present, the clinical tre...

Claims

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Application Information

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IPC IPC(8): C07K14/605A61K38/26A61P3/04A61P3/10A61P9/12A61P3/06A61P3/00A61P25/00A61P9/10A61P9/00A61P1/00A61P1/14
CPCA61K38/00C07K14/605
Inventor 周凤韩京傅俊杰费颖颖张莹
Owner XUZHOU NORMAL UNIVERSITY
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