研究目的
To develop AIE light-up probes for imaging the hERG potassium channel, aiming to provide a simple and safe method for visualizing hERG channels in cells, with potential applications in cancer diagnosis and treatment.
研究成果
Four AIE light-up probes for hERG channels were successfully developed, exhibiting good fluorescent properties, low cytotoxicity, and high affinity, particularly probe L3 with IC50 of 0.32 nM. They enable effective imaging of hERG channels in cells at nanomolar levels, providing a foundation for advanced sensing and imaging applications, though improvements in emission wavelength are needed for in vivo use.
研究不足
The probes use blue-green emissive TPE fluorogens, which limit in vivo applications due to poor tissue penetration and high autofluorescence. Future work should focus on developing red or NIR emissive probes for broader applicability.
1：Experimental Design and Method Selection:
The study designed fluorescent probes based on the AIE effect, using TPE as the fluorophore and astemizole/E-4031 as pharmacophores, with a 'click' reaction for synthesis. The rationale was to create probes that light up upon binding to hERG channels due to restricted intramolecular rotation.
2：Sample Selection and Data Sources:
hERG transfected HEK293 cells were used for binding affinity, cytotoxicity, and imaging assays.
3：List of Experimental Equipment and Materials:
Probes L1-L4 were synthesized; equipment included a Zeiss Axio Observer A1 microscope for imaging, and materials for spectroscopic measurements (e.g., acetonitrile, PBS).
4：Experimental Procedures and Operational Workflow:
Probes were synthesized via 'click' chemistry; spectroscopic properties were measured in PBS; inhibitory activities were assessed using radio-ligand binding assays; cytotoxicity was evaluated with CCK-8 assays; fluorescent imaging was performed on cells incubated with probes, with and without astemizole inhibition.
5：Data Analysis Methods:
Data were analyzed using the Cheng-Prusoff equation for Ki values, and ImageJ software for adjusting background in imaging.
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