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 Ca2+ 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.
Original language | English |
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Article number | 3364 |
Number of pages | 9 |
Journal | International Journal of Molecular Sciences |
Volume | 24 |
Issue number | 4 |
DOIs | |
Publication status | Published - 8 Feb 2023 |
Keywords
- magnetic nanoparticles
- mechanosensitive ion channels
- mechano-transduction
- calcium assay
- drug screening
- nanomedicine
- Communication