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Micro-wave promoted solid-phase synthesis of glucagons-like peptide-1(GLP-1) analogue and uses thereof

A glucagon and GLP-1 technology, which is applied in the field of glucagon-like peptide-1 analogs and their microwave-promoted solid-phase synthesis, can solve the problem of inability to synthesize target polypeptides, loss of synthetic significance, and long synthesis cycle. problems, to achieve the effect of convenient purification work, shortened synthesis cycle, and short synthesis cycle

Inactive Publication Date: 2008-09-03
CHINA PHARM UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Using the traditional solid-phase method to synthesize long peptides, the yield is often very low and the impurities are more difficult to purify, thus losing the meaning of synthesis from a practical point of view
Secondly, the synthesis cycle is long. In the case of no difficult peptide sequence in the middle, it usually takes nearly a week to complete the synthesis cycle of 30 peptides. If there is a difficult peptide sequence, it is often impossible to synthesize the target peptide.

Method used

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  • Micro-wave promoted solid-phase synthesis of glucagons-like peptide-1(GLP-1) analogue and uses thereof
  • Micro-wave promoted solid-phase synthesis of glucagons-like peptide-1(GLP-1) analogue and uses thereof
  • Micro-wave promoted solid-phase synthesis of glucagons-like peptide-1(GLP-1) analogue and uses thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0046] His- D-Gly -Glu-Gly-Thr-Phe-Thr-Ser-Asp-Val-Ser-Ser-Tyr-Leu-Glu-Gly-Gln-Ala-Ala-Lys-Glu-Phe-Ile-Ala-Trp-Leu-Val -Lys-Gly-Arg-NH 2 (SEQ.ID NO: 2) Microwave to promote solid phase synthesis

[0047] (1) Swelling of resin

[0048] Weigh 50mg of Fmoc-rink amide-MBHA Resin (substitution amount 0.4mmol / g), swell with 7mL DCM for 30min, suction filter to remove DCM, then swell with 10mL NMP for 30min, and finally rinse with NMP, DCM, NMP 7mL respectively.

[0049] (2) Microwave promotes the removal of Fmoc protecting group

[0050] Put the swollen resin into the reactor, add 7 mL of 25% piperidine / NMP(V / V) solution containing 0.1M HOBT, and react in the microwave reactor for 1 min, the microwave power is 15W, and the reaction temperature is controlled at 50℃ Use an air compressor to compress the air to cool, filter out the solution after the reaction; add 7mL of 25% piperidine / NMP(V / V) solution containing 0.1M HOBT and react for another 4min in the microwave reactor with a microw...

Embodiment 2～28

[0064] According to the method described in Example 1, the polypeptides of Examples 2-28 were synthesized according to the corresponding sequences, and their molecular weights were confirmed by electrospray mass spectrometry (ESI-MS).

Embodiment 2

[0066] His- Asn -Glu-Gly-Thr-Phe-Thr-Ser-Asp-Val-Ser-Ser-Tyr-Leu-Glu-Gly-Gln-Ala-Ala-Lys-Glu-Phe-Ile-Ala-Trp-Leu-Val -Lys-Gly-Arg-NH 2 (SEQ. ID NO: 3); The theoretical relative molecular mass is 3340.7. ESI-MS m / z: found[M+3H] 3+ 1114.5, [M+4H] 4+ 836.1, [M+5H] 5+ 669.1; calu[M+3H] 3+ 1114.6, [M+4H] 4+ 836.3, [M+5H] 5+ 669.1.

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Abstract

The invention relates to new type GLP-1 analogues and a microwave promotive solid phase synthesis process of the same. GLP-1 analogues with longer pharmacological action time can be obtained by modifying 8, 9, 16, 22, 27 or 37 sites of natural GLP-1, the chemical synthesis is highly effectively and rapidly realized by microwave promotive solid phase synthesis process, the crude product is purified by highly effective liquid phase, and GLP-1 analogues is obtained after lyophilized.

Description

Technical field [0001] The present invention relates to glucagon-like peptide-1 (GLP-1) analogs and a microwave-assisted solid-phase synthesis method thereof. Background technique [0002] Diabetes is the third chronic non-communicable disease that seriously threatens human health after tumors and cardiovascular diseases. At present, there are about 200 million people with diabetes in the world, and it is expected to increase to 300 million by 2025. In 2007, there were 30 million diabetic patients in China. It is estimated that by 2030, the number of diabetic patients in my country will exceed 50 million. China has become the second largest country with diabetes after India, and type 2 diabetes accounts for about 90% of the total number of diabetic patients. . The most effective way to treat type 2 diabetes is insulin injections. Intensive insulin therapy is used clinically to delay the progress of diabetes. Insulin therapy can reverse the damage of pancreatic β-cell function whi...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07K14/605C07K1/04C07K1/08A61K38/26A61P3/10
CPCY02P20/55
Inventor 黄文龙张惠斌迟玉石周金培周映红倪帅键钱海
Owner CHINA PHARM UNIV
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