Xenopus laevis GLP-1 analogue and uses thereof

A technology of Xenopus laevis and analogues, which is applied in the direction of drug combination, animal/human protein, medical preparations containing active ingredients, etc., can solve the problem of short half-life and achieve high in vitro stability

Inactive Publication Date: 2018-08-03
XUZHOU NORMAL UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, natural GLP-1 has limitations, that is, its half-life is extremely short, and it will be degraded by dipeptidyl peptidase (DPP-IV) after 2 to 3 minutes of secretion, even if GLP-1 is given exogenously, it is also very fast Will be degraded by DPP-IV

Method used

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  • Xenopus laevis GLP-1 analogue and uses thereof
  • Xenopus laevis GLP-1 analogue and uses thereof
  • Xenopus laevis GLP-1 analogue and uses thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0046]

[0047] (1) Swelling of the resin

[0048] 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.

[0049] (2) Removal of resin Fmoc protecting group

[0050] Transfer the swollen resin to a peptide synthesizer, add 7mL 20% piperidine / DMF to react at room temperature for 5min, filter off the deprotection solution, wash the resin once with 7mL DMF, then add 7mL 20%piperidine / DMF to deprotect and wash the resin for 15min, Finally, the resin was washed 4 times with 7 mL of DMF, 1.5 min each time, to obtain the Rink resin from which the Fmoc protecting group was removed.

[0051] (3) Synthesis of Fmoc-Lys-Rink amide-MBHA Resin

[0052] Weigh Fmoc-Lys(Boc)-OH (0.4mmol), dissolve it with 3mL 10% D...

Embodiment 2～19

[0062] According to the method described in Example 1, the Xenopus laevis glucagon-like peptide-1 (XenGLP-1) analogues of Examples 2 to 30 were synthesized according to the corresponding sequences and side chains, and the respective peptides were confirmed by ESI-MS. molecular weight.

Embodiment 2

[0064]

[0065] The theoretical relative molecular mass is 3838.3. ESI-MS m / z:calu[M+3H] 3+ 1290.4,[M+4H] 4+ 968.1;found[M+3H] 3+ 1290.6,[M+4H] 4+ 968.5.

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Abstract

The invention relates to an Xenopus laevis GLP-1 analogue, a synthesis method and applications thereof. According to the present invention, the side chain and the C terminal of Xenopus laevis GLP-1 are subjected to structure modification to obtain the Xenopus laevis GLP-1 analogue with advantages of high blood glucose lowering activity and long pharmacological action time; and the Xenopus laevis GLP-1 analogue has significantly improved biological activity, and further has effects of strong long-acting blood glucose lowering and strong weight reducing.

Description

technical field [0001] The invention relates to a Xenopus laevis glucagon-like peptide-1 analogue and its application Background technique [0002] Diabetes mellitus (DM) is a group of metabolic diseases characterized by chronic hyperglycemia caused by genetic and environmental factors. A series of metabolic disorders such as sugar, protein, fat, water and electrolytes are caused by relative or absolute deficiency of insulin secretion; or defects in insulin action. Persistent hyperglycemia is the basic feature. Prolonged illness can cause damage to multiple systems, leading to chronic complications in the eyes, kidneys, nerves, cardiovascular and cerebrovascular organs, and lower limbs. On March 6, 2016, the World Health Organization released the global diabetes report for the first time, showing that the number of adults with diabetes in the world has tripled in the past 40 years, and most of them live in developing countries. The report shows that the prevalence of diab...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07K14/605A61K38/26A61P3/04A61P3/10A61P9/12A61P3/06A61P3/00A61P25/00A61P9/10A61P9/00A61P1/00A61P1/14
CPCA61K38/00A61P1/00A61P1/14A61P3/00A61P3/04A61P3/06A61P3/10A61P9/00A61P9/10A61P9/12A61P25/00C07K14/605
Inventor 韩京费颖颖周凤张莹
Owner XUZHOU NORMAL UNIVERSITY
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