Use of rip3 inhibitor in the preparation of anti-platelet thrombus medicine

An anti-platelet, 1.RIP3 technology, used in drug combinations, blood diseases, pharmaceutical formulations, etc., can solve problems such as unknown status

Active Publication Date: 2020-07-14
SUZHOU UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Most existing studies focus on the regulation of RIP3 on apoptosis and programmed necrosis, but its role in hemostasis and thrombosis is still unknown

Method used

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  • Use of rip3 inhibitor in the preparation of anti-platelet thrombus medicine
  • Use of rip3 inhibitor in the preparation of anti-platelet thrombus medicine
  • Use of rip3 inhibitor in the preparation of anti-platelet thrombus medicine

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0036] Example 1: Anti-thrombosis experiment of GSK'872.

[0037] 1. Reagents and materials:

[0038] Aspirin, A3P5P, bovine serum albumin (BSA), sodium pentobarbital, RGDS (Arg-Gly-Asp-Ser), and SB216763 were purchased from Sigma-Aldrich; Calcein-AM was purchased from Tongren Institute of Chemistry; U46619 was purchased from Calbiochem; thrombin, collagen, ADP and Chrono-Lume were purchased from Chronolog; FITC-labeled mouse P-selectin (Wug.E9), PE-labeled mouse integrin αIIbβ3 (JON / A), anti-mouse GPIb antibody Purchased from Emfret Analytics; PE-labeled anti-mouse CD41 was purchased from BioLegend; FITC-labeled mouse fibrinogen was purchased from Abcam; TXB2 enzyme-linked immunoassay kit was purchased from ENZO Life Sciences; anti-mouse RIP3 antibody was purchased from ProSci; anti-phospho-Akt (Thr308), anti-phospho-Akt (Ser473), anti-total Akt, anti-phospho-ERK1 / 2 (Thr202 / Tyr204), anti-phospho-Gsk3β (Ser9), anti-human RIP3, and anti-β- Actin (β-actin) antibody was purchas...

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Abstract

The invention discloses the application of RIP3 inhibitor in the preparation of anti-platelet thrombus medicine. Specifically, the present invention explores the role of RIP3 in the process of hemostasis and thrombus formation through experiments for the first time, and finds that RIP3 not only participates in the regulation of platelet function in vitro experiments, but also plays an important role in the process of hemostasis and thrombus formation in vivo. It can be used as a new target for antithrombotic therapy. By regulating the release of platelet dense body granules, RIP3 selectively affects thromboxane A2 (TXA2) and thrombin-mediated platelet activation, suggesting that RIP3 inhibitors (especially GSK'872) can participate in the process of platelet thrombus formation, thereby inhibiting Thrombosis can be developed into a new type of anti-platelet thrombus drug, which is of great scientific and economic value.

Description

technical field [0001] The invention belongs to the field of antithrombotic drugs and relates to the use of RIP3 inhibitors in the preparation of antithrombotic drugs. Background technique [0002] It is well known that platelets play an important role in the process of hemostasis and thrombus formation. Once the blood vessel is damaged, platelets can adhere to the protein components under the endothelium and be activated at the same time, thereby triggering the release of dense granules in the platelets and the synthesis of thromboxane A2 (TXA2). Released soluble platelet agonists (such as adenosine diphosphate (ADP), thrombin, and TXA2) further recruit circulating platelets and bind to G protein-coupled receptors (GPCRs) on the surface of platelets. ) to make the aggregation reaction more stable, thereby forming an irreversible platelet thrombus to achieve the effect of coagulation and hemostasis. [0003] As an important component of dense granules, ADP plays a major me...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K45/00A61K38/55A61P7/02
CPCA61K38/55A61K45/00
Inventor 戴克胜
Owner SUZHOU UNIV
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