Application and research method of atopaxar hydrobromide as novel JAK-STAT3 signal path inhibitor

A JAK-STAT3, signaling pathway technology, applied in the field of medical applications, can solve problems such as interference with platelet signaling

Active Publication Date: 2019-11-01
QINGDAO MARINE BIOPHARMACEUTICAL RES INST +1
View PDF3 Cites 2 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

E5555 is a reversible protease activated receptor (PAR)-1 thrombin receptor antagonist, which can interf

Method used

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
View more

Image

Smart Image Click on the blue labels to locate them in the text.
Viewing Examples
Smart Image
  • Application and research method of atopaxar hydrobromide as novel JAK-STAT3 signal path inhibitor
  • Application and research method of atopaxar hydrobromide as novel JAK-STAT3 signal path inhibitor
  • Application and research method of atopaxar hydrobromide as novel JAK-STAT3 signal path inhibitor

Examples

Experimental program
Comparison scheme
Effect test

Embodiment Construction

[0061] For ease of understanding, the technical solutions of the present invention are further specifically described below in conjunction with the accompanying drawings and through embodiments:

[0062] A research method for atopaxa bromide as a novel JAK-STAT3 signaling pathway inhibitor, specifically comprising the following steps:

[0063] S1: Cell culture: cells such as hTERT-BJ, HELA, HepG2, A549, and SKA (the stable transfected strains of the high-throughput screening platform for anti-tumor drugs based on STAT3, which have been successfully constructed in our laboratory) were cultured in DMEM high-glucose culture Base, DU145 and MDA-MB-231 cells were cultured in RPMI-1640 medium at 37°C, 5% CO 2 cultivated under conditions. DMEM high-glucose medium and RPMI-1640 medium contain double anti-penicillin streptomycin and 10% fetal bovine serum FBS.

[0064] S2: Protein extraction: Culture the cells to 80% confluence in a 100mm cell culture dish, wash with 4°C pre-cooled P...

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to view more

PUM

No PUM Login to view more

Abstract

The invention relates to an application of atopaxar hydrobromide as a novel JAK-STAT3 signal channel inhibitor. The atopaxar hydrobromide can be used for inhibiting STAT3 activity and STAT3 downstreamgene expression to control cell proliferation; the atopaxar hydrobromide has an inhibition effect on STAT3 activation induced by cytokines and JAKs self-phosphorylation; in computer molecular simulation, the atopaxar hydrobromide can be combined with an SH2 structural domain of STAT3 and has very high affinity with a JAK kinase JH1 structural domain; and the atopaxar hydrobromide can horizontallyinhibit the tumor cell growth. A research method of the atopaxar hydrobromide as a novel JAK-STAT3 signal pathway inhibitor comprises the following steps: cell culturing; protein extraction; western-Blot; RNA extraction; RT-PCR (Reverse Transcription-Polymerase Chain Reaction) and fluorescent quantitative PCR; luciferase activity analysis; cell viability analysis; cell cycle detection by flow cytometry; cell apoptosis detection by flow cytometry; nude mouse transplantation tumor experiments; computer molecular dynamics simulation docking analysis; and data calculation and processing. The invention lays a foundation for further cell cycle detection and subsequent research and development of novel small molecule drugs.

Description

technical field [0001] The invention belongs to the field of medical application, and relates to a new medical application and research method of atropaxabromic acid, specifically, its application and research method as a JAK-STAT3 signaling pathway inhibitor. Background technique [0002] The JAK-STAT signaling pathway is an important intracellular signal transduction pathway in the process of cell growth, activation, differentiation, apoptosis and its function. Abnormal activation of STAT3 signaling can lead to tumorigenesis, such as breast cancer, lung cancer. Due to their important functions in tumorigenesis, JAKs (Janus kinases) and STATs (signal transducers and activators of transcription) have become popular targets for drug design. Although inhibitors against JAKs and STATs have been approved by FDA, EMA or clinical trials, certain drawbacks such as drug resistance and side effects have also been observed. In addition, as kinase inhibitors, these drugs can bind to ...

Claims

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to view more

Application Information

Patent Timeline
no application Login to view more
IPC IPC(8): A61K31/5377A61P35/00C12Q1/66C12Q1/6851G01N15/14G01N21/31G01N33/50
CPCA61K31/5377A61P35/00C12Q1/6851C12Q1/66G01N33/5011G01N21/31G01N15/14C12Q2531/113C12Q2563/107
Inventor 杨金波赵晨阳张心心
Owner QINGDAO MARINE BIOPHARMACEUTICAL RES INST
Who we serve
  • R&D Engineer
  • R&D Manager
  • IP Professional
Why Eureka
  • Industry Leading Data Capabilities
  • Powerful AI technology
  • Patent DNA Extraction
Social media
Try Eureka
PatSnap group products

Browse by: Latest US Patents, China's latest patents, Technical Efficacy Thesaurus, Application Domain, Technology Topic.

© 2024 PatSnap. All rights reserved.Legal|Privacy policy|Modern Slavery Act Transparency Statement|Sitemap