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Dual-target polypeptide compounds and use of dual-target polypeptide compound in preparation of drug for treating diabetes and diseases characterized by the same

A peptide compound, dual-target technology, applied in the application field of dual-target peptide compounds and drugs, to prevent weight gain, low cost, and easy to scale up production.

Active Publication Date: 2019-10-08
SUN YAT SEN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

There is an urgent need for effective diabetes treatment drugs in the market

Method used

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  • Dual-target polypeptide compounds and use of dual-target polypeptide compound in preparation of drug for treating diabetes and diseases characterized by the same
  • Dual-target polypeptide compounds and use of dual-target polypeptide compound in preparation of drug for treating diabetes and diseases characterized by the same
  • Dual-target polypeptide compounds and use of dual-target polypeptide compound in preparation of drug for treating diabetes and diseases characterized by the same

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0035] Embodiment 1 polypeptide compound

[0036] Table 1. Structures of polypeptide compounds provided in the examples of the present invention

[0037]

Embodiment 2

[0038] Example 2. GCGR and GLP-1R in vitro activity assay

[0039] Utilize cAMP Assay Kit (CISBIO company) to detect the agonistic effect of the polypeptide compound PEPT#1-4 described in the present invention on glucagon-like peptide 1 receptor (GLP-1R) and glucagon receptor (GCGR), construct The dose-response curve quantitatively evaluates the agonistic activity of the polypeptide compound PEPT#1-4 on GLP-1R and GCGR. In the experiment, Exenatide, Glucagon and Oxyntomodulin were used as reference substances.

[0040] The experimental method is as follows:

[0041] (1) First construct HEK-293 cells stably expressing human GCGR or GLP-1R for the CRE-luciferase system. According to 98.0L DMEM / 10% FBS medium per well, 5000 cells were inoculated into a 384-well plate and cultured overnight.

[0042] (2) On the second day after the cells were plated, the polypeptide compounds PEPT#1-4 to be tested were prepared into serial dilutions from 0.005nM to 100.0nM; the reference substa...

Embodiment 3

[0048] Example 3. Evaluation of the Hypoglycemic Activity of Compound PEPT#1-4 and Exenatide Based on the Oral Glucose Tolerance Test (OGTT)

[0049] experimental method:

[0050] (1) Male C57Bl / 6J mice aged 12-16 weeks were randomly divided into 6 groups (8 mice in each group, and the difference in blood glucose between groups was not more than 1.1mmol / L), which were normal group and exenatide positive control group respectively. 1. The drug group of the test polypeptide compound series.

[0051] (2) The test mice were administered by subcutaneous injection, the administration dose was 3ug / mouse, and the administration volume was 0.1ml / mouse. The normal group was given an equal volume of vehicle PBS solution.

[0052] (3) After 4 hours of administration, an initial blood sample (fasting blood glucose level) was obtained.

[0053] (4) Subsequently, each mouse was given intragastric administration of glucose (100 mg / ml glucose solution×20 ml), and the animals were returned t...

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PUM

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Abstract

The invention relates to dual-target polypeptide compounds and use of the dual-target polypeptide compound in preparation of a drug for treating diabetes and diseases characterized by the same. The invention belongs to the field of biomedical chemistry, and relates to the dual target polypeptide compounds glucagon-like peptide-1 receptor(GLP-1R) and a glucagon receptor (GCGR) having the agonisticeffect at the same time. The dual-target agonist-polypeptide compound provided by the invention can simultaneously agonize both GLP-1R and GCGR membrane receptors, has the ability to effectively regulate collective glucose homeostasis and energy metabolism, and can significantly lower blood glucose concentration. The polypeptide compound provided by the invention has high biological activity and low side effects; exhibits remarkable stability in pharmacological experiments of drugs; is subjected to amplification production , has low cost, and has potential for preparing the drug for treating diabetes.

Description

technical field [0001] The invention belongs to the field of biomedical chemistry and relates to a class of receptors for glucagon-like peptide-1 receptor (GLP-1R) and glucagon receptor (Glucagon receptor, GCGR). A dual-target polypeptide compound with an agonistic effect. The invention also relates to the application of the compound in the preparation of medicines for treating diabetes, obesity and other diabetes-related complications. Background technique [0002] Diabetes mellitus (DM) is a metabolic disorder caused by a variety of etiologies, characterized by chronic hyperglycemia, accompanied by insulin secretion defects or insulin action disorders, leading to carbohydrate, fat, and protein metabolic disorders, resulting in chronic disease in various organs. Injury, dysfunction and failure. In recent years, diabetes has become another chronic disease that seriously endangers human health worldwide after cardiovascular and cerebrovascular diseases and malignant tumors....

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07K14/605C07K14/575A61K38/22A61K38/26A61P3/10
CPCA61K38/00A61P3/10C07K14/57563C07K14/605
Inventor 周晖皓蒋先兴
Owner SUN YAT SEN UNIV
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