Suppr超能文献

磁离子通道激活(MICA)介导的筛选分析:一种用于远程激活机械敏感离子通道的动态平台。

Magnetic Ion Channel Activation (MICA)-Enabled Screening Assay: A Dynamic Platform for Remote Activation of Mechanosensitive Ion Channels.

机构信息

Healthcare Technology Institute, Institute of Translational Medicine, University of Birmingham, Birmingham B15 2TH, UK.

Centre for Pharmaceutical Engineering Science, School of Pharmacy and Medical Sciences, Faculty of Lifesciences, University of Bradford, Bradford BD7 1DP, UK.

出版信息

Int J Mol Sci. 2023 Feb 8;24(4):3364. doi: 10.3390/ijms24043364.

Abstract

This study reports results of a mechanical platform-based screening assay (MICA) to evaluate the remote activation of mechanosensitive ion channels. Here, we studied ERK pathway activation and the elevation in intracellular Ca levels in response to the MICA application using the Luciferase assay and Fluo-8AM assay, respectively. Functionalised magnetic nanoparticles (MNPs) targeting membrane-bound integrins and mechanosensitive TREK1 ion channels were studied with HEK293 cell lines under MICA application. The study demonstrated that active targeting of mechanosensitive integrins via RGD (Arginylglycylaspartic acid) motifs or TREK1 (KCNK2, potassium channel subfamily K member 2) ion channels can stimulate the ERK pathway and intracellular calcium levels compared to non-MICA controls. This screening assay offers a powerful tool, which aligns with existing high-throughput drug screening platforms for use in the assessment of drugs that interact with ion channels and influence ion channel-modulated diseases.

摘要

本研究报告了一种基于机械平台的筛选测定法(MICA)的研究结果,用于评估机械敏感离子通道的远程激活。在这里,我们分别使用荧光素酶测定法和 Fluo-8AM 测定法研究了 MICA 应用后 ERK 通路的激活和细胞内 Ca2+水平的升高。用针对膜结合整联蛋白和机械敏感 TREK1 离子通道的功能化磁性纳米颗粒(MNPs)在 MICA 应用下研究了 HEK293 细胞系。该研究表明,通过 RGD(精氨酸-甘氨酸-天冬氨酸)基序或 TREK1(KCNK2,钾通道亚家族 K 成员 2)离子通道对机械敏感整联蛋白的主动靶向,与非 MICA 对照相比,可以刺激 ERK 通路和细胞内钙水平。该筛选测定法提供了一种强大的工具,与现有的高通量药物筛选平台相匹配,可用于评估与离子通道相互作用并影响离子通道调节疾病的药物。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/9312/9962865/a6f559670118/ijms-24-03364-g001.jpg

文献检索

告别复杂PubMed语法,用中文像聊天一样搜索,搜遍4000万医学文献。AI智能推荐,让科研检索更轻松。

立即免费搜索

文件翻译

保留排版,准确专业,支持PDF/Word/PPT等文件格式,支持 12+语言互译。

免费翻译文档

深度研究

AI帮你快速写综述,25分钟生成高质量综述,智能提取关键信息,辅助科研写作。

立即免费体验