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Class of long-acting glucagon-like peptide-1 (GLP-1) analog and application thereof

A technology of glucagon and analogs, which is applied in the field of long-acting glucagon-like peptide-1 analogs, can solve problems such as prolonging the half-life of GLP-1, and achieve the effect of stable chemical properties and avoiding local itching

Active Publication Date: 2017-08-18
CHINA PHARM UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, since GLP-1 is rapidly filtered and eliminated by the kidneys, resistance to degradation by DPP-IV enzymes can only prolong the half-life of GLP-1 to a certain extent

Method used

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  • Class of long-acting glucagon-like peptide-1 (GLP-1) analog and application thereof
  • Class of long-acting glucagon-like peptide-1 (GLP-1) analog and application thereof
  • Class of long-acting glucagon-like peptide-1 (GLP-1) analog and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0066]

[0067] solid-phase synthesis.

[0068] 1. Synthesis of cysteine-modified polypeptide chain

[0069] 1.1. Resin swelling

[0070] Weigh 50 mg of Fmoc-Rink amide-MBHA Resin (degree of substitution 0.4 mmol / g), swell with 7 mL of DCM for 30 min, filter to remove DCM, then swell with 10 mL of NMP for 30 min, and finally rinse with NMP, DCM, and 7 mL of NMP.

[0071] 1.2. Removal of Fmoc protecting group

[0072] Put the swollen resin into the reactor, add 7 mL of 25% piperidine / NMP (V / V) solution containing 0.1M HOBt, react for 1 min, and filter off the solution after completion; then add 25% piperidine containing 0.1M HOBt Pyridine / NMP (V / V) solution 7mL, reacted for 4min, filtered off the solution after completion, washed with NMP. A resin free of the initially attached Fmoc protecting group is obtained.

[0073] 1.3. Synthesis of Fmoc-Arg(pbf)-Rink amide-MBHA Resin

[0074] Fmoc-Arg(pbf)-OH (32.0 mg, 0.04 mmol), HBTU (15.1 mg, 0.04 mmol), HOBt (5.4 mg, 0.04 mmo...

Embodiment 2

[0091]

[0092] The synthesis method is the same as in Example 1, and the theoretical relative molecular mass is 4020.1. ESI-MS m / z: Calcd.[M+3H] 3+ 1341.0, [M+4H] 4+ 1006.0; Found[M+3H] 3+ 1341.2, [M+4H] 4+ 1006.9.

Embodiment 3

[0094]

[0095] The synthesis method is the same as in Example 1, and the theoretical relative molecular mass is 3979.0. ESI-MS m / z: Calcd.[M+3H] 3+ 1327.3, [M+4H] 4+ 995.8; Found[M+3H] 3+ 1327.2, [M+4H] 4+ 995.3.

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Abstract

The invention relates to a class of long-acting glucagon-like peptide-1 (GLP-1) analog and a synthesis method thereof. The GLP-1 analogue with longer pharmacological action time is obtained by modifying GLP-1. The synthesis of target polypeptide is quickly achieved by a orthogonal protection strategy solid phase synthesis method. The crude product is purified and lyophilized to obtain the GLP-1 analog.

Description

technical field [0001] The invention relates to a class of long-acting glucagon-like peptide-1 (GLP-1) analogs and applications thereof. Background technique [0002] Diabetes is the third chronic non-communicable disease that seriously threatens human health after tumors and cardiovascular diseases. Currently, there are about 300 million diabetics in the world, which is expected to increase to 500 million by 2025. Clinically, intensive insulin therapy is used to delay the progression of diabetes, but insulin injections have the risk of hypoglycemia. The therapeutic effect is affected by factors such as dose, injection site, and injection route, and there are large individual differences. If insulin is used carelessly, severe hypoglycemic side effects will occur. [0003] Glucagon-like peptide-1 (GLP-1) is a glucose-dependent incretin hormone. GLP-1 stimulates insulin secretion without hypoglycemia. This glucose-dependent insulin-stimulating property avoids The risk of hy...

Claims

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Application Information

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IPC IPC(8): C07K14/605A61K38/26A61P3/10
CPCA61K38/00C07K14/605
Inventor 黄文龙钱海蔡星光孙李丹戴雨轩韩京
Owner CHINA PHARM UNIV
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