A Thallium-Based Screening Procedure to Identify Molecules That Modulate the Activity of Ca2+-Activated Monovalent Cation-Selective Channels
January 2018
TLDR The conclusion is that a new test was created to find substances that affect specific ion channels, and it works well for drug discovery.
The document from April 1, 2018, details a study that developed and optimized a thallium-based fluorescent screening assay to identify modulators of TRPM5 and TRPM4 ion channels, which are important in various diseases. The assay was shown to be effective in detecting thallium flux indicative of channel activity, and it was used to screen a library of 75 compounds. TPPO was identified as the most potent TRPM5 inhibitor, and SID 2848719 as the top potentiator. Ketoconazole was characterized as a TRPM5 inhibitor with an IC50 of 3.23 µM. The assay demonstrated good reproducibility, a high signal-to-noise ratio, and was confirmed to be a suitable tool for high-content screening with limited variability, as indicated by the Z' factor. The study suggests that this assay could aid in drug development and understanding the physiological roles of TRPM4 and TRPM5 channels. The authors reported no conflicts of interest and acknowledged financial support from research grants.
