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Application of indacaterol maleate as cGAS-STING pathway targeted agonist

An agonist, acid indene technology, applied in the field of medicine, can solve the problems such as no article, no patent application, etc., and achieve the effects of high safety, low cost and good development prospects

Pending Publication Date: 2022-01-04
JINAN UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] At present, there is no article showing the relationship between indacaterol maleate and cGAS-STING pathway, and no patent application yet

Method used

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  • Application of indacaterol maleate as cGAS-STING pathway targeted agonist
  • Application of indacaterol maleate as cGAS-STING pathway targeted agonist
  • Application of indacaterol maleate as cGAS-STING pathway targeted agonist

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Embodiment 1

[0019] In order to achieve the above object, the present invention adopts the following technical solutions:

[0020] 1. Identification of indacaterol maleate targeting cGAS-STING pathway by biotin photoaffinity labeling combined with proteomics. The specific steps are:

[0021] (1) Combining indacaterol maleate with a photocrosslinking probe. Dissolve 50 mg of indacaterol maleate (purchased from Shanghai Taosu Biochemical Technology Co., Ltd.) in 5 mL of dimethylformamide (N,N-Dimethylformamide, DMF), and add 25.8 mg of probe diacridine (3 -(but-3-yn-1-yl)-3-(2-iodoethyl)-3H-diazirine) (purchased from Shanghai Bi De Pharmaceutical Technology Co., Ltd.) and 26 mg potassium carbonate, mix the solution and stir at 60 ° C 12 hours. After the reaction, 10 mL of ultrapure water was added to cool down, and extracted with ethyl acetate (twice, 10 mL each), combined with 10 mL of brine, washed the organic layer twice, and dried over anhydrous sodium sulfate. The residue remaining ...

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Abstract

The invention discloses application of indacaterol maleate as a cGAS-STING pathway targeted agonist. In-vitro level verification, biotin photoaffinity labeling, conjugated protein omics, bioinformatics and molecular biology results show that the indacaterol maleate can activate a cGAS-STING pathway in a targeted manner and inhibit cancer cell proliferation and has a good treatment prospect in adjuvant therapy of colorectal cancer related diseases.

Description

technical field [0001] The invention belongs to the technical field of medicine, and in particular relates to the application of indacaterol maleate as a cGAS-STING pathway targeting agonist. Background technique [0002] The structural formula of indacaterol maleate is as follows: [0003] [0004] Chronic obstructive pulmonary disease (COPD) is a disease of persistent and progressive airflow limitation [1]. Due to factors such as impaired peripheral muscle function, obstructed ventilation, and impaired cardiopulmonary function, patients with COPD often experience symptoms such as dyspnea and muscle weakness, which further lead to impaired activity tolerance and reduced quality of life [2]. As a bronchodilator, indacaterol maleate is a long-acting β2-receptor agonist that can continuously relax bronchial smooth muscle and relieve lung hyperinflation, thereby improving airflow limitation and reducing symptoms in patients with COPD[3] . [0005] The cyclic GMP-AMP synth...

Claims

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Application Information

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IPC IPC(8): A61K31/4704A61P35/00
CPCA61K31/4704A61P35/00
Inventor 何庆瑜李杨葭
Owner JINAN UNIVERSITY
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