一种无标记筛选方法及其筛选的FPR1偏向性激动剂在急性肺损伤上的应用

Kinetin Riboside was screened using a label-free screening method. This compound, as an FPR1-biased agonist, can specifically activate the G protein signaling pathway, solving the problem of the lack of drugs for treating acute lung injury in the existing technology and realizing an effective treatment for acute lung injury.

CN121521807BActive Publication Date: 2026-07-17JINAN UNIVERSITY

Patent Information

Authority / Receiving Office
CN · China
Patent Type
Patents(China)
Current Assignee / Owner
JINAN UNIVERSITY
Filing Date
2025-11-19
Publication Date
2026-07-17

AI Technical Summary

Technical Problem

Currently, there is a lack of specific drugs for the effective treatment of acute lung injury. Existing treatments such as glucocorticoids can only relieve inflammation, but the hospital mortality rate is still as high as 40%. Therefore, there is a need to find more precise treatment drugs.

Method used

FPR1-biased agonists were screened using a label-free screening method. Cell signal changes were monitored using the Epic label-free screening instrument and calcium ion indicators. Combined with G protein dissociation and β-arrestin recruitment experiments, kinetin riboside (KR) was screened out. This compound can specifically activate the G protein signaling pathway and inhibit superoxide production and degranulation.

Benefits of technology

The study identified kinetin nucleosides with therapeutic effects on acute lung injury, which significantly inhibited superoxide production and degranulation, reduced neutrophil infiltration, alleviated lung tissue damage, and decreased mortality.

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Abstract

本发明公开了一种无标记筛选方法及其筛选的FPR1偏向性激动剂在急性肺损伤上的应用。本发明利用Epic无标记筛选结合钙流筛选,得到初筛的FPR1激动剂;通过G蛋白解离实验和β‑arrestin募集实验,得到FPR1偏向性激动剂;通过已知的FPR1激动剂筛选,得到FRP1拮抗剂。本发明首次获得了FPR1偏向性激动剂激动素核苷,通过检测偏向性激动剂KR抑制超氧、抑制脱落细胞和抑制MPO的功能,证实偏向性激动剂KR具有治疗急性肺损伤的功能。本发明首次发现了激动素核苷具有治疗急性肺损伤作用。
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