While hERG channel is notoriously regarded as an off-target due to drug-induced cardiotoxicity, its therapeutic potential as a drug target remains largely unexplored. Methods: This study investigated ...
Many drugs from different chemical classes and therapeutic areas have been shown to inhibit currents mediated via the hERG-coded ion channel, which is strongly correlated to a risk of inducing TdP.
Jennifer Love Hewitt’s hindsight is 20/20. The “Ghost Whisperer” actress reflected on being sexualized as a teen and having “grown men” make jokes about her breasts during her appearance ...
Regulatory agencies require the evaluation of new drugs on human ERG channels. Methods: To assess hERG potassium channel inhibition, we utilized the FLIPR® Potassium Assay, a commercially available ...
In particular, 17p presented strong inhibitory activity against PI3Kδ; significant isoform selectivity against PI3Kβ, PI3Kγ, and mTOR; acceptable safety profiles in normal cells, as well as in the ...
Expert Rev Clin Pharmacol. 2010;3(3):321-329. Despite a propensity to block hERG channel function, as determined by electrophysiology, for a limited number of compounds no cardiac arrhythmias have ...