A stable cell line inducibly expressing hERG1a/1b heteromeric channels.

ABSTRACT: Heterologously expressed hERG channels represent a mainstay of in vitro drug safety screens intended to mitigate risk of cardiac I_Kr block and sudden cardiac death. This is true even as more channel types are adopted as part of the Comprehensive in vitro Proarrhythmia Assay (CiPA) intended to elevate specificity and thus enhance throughput of promising lead drugs. Until now, hERG1a homomeric channels have been used as a proxy for I_Kr despite a wealth of evidence showing that hERG1a/1b heteromers better represent native channels in terms of protein abundance and channel biophysical and pharmacological properties. Past efforts to create a stable hERG1a/1b cell line were met with unpredictable silencing of hERG1b expression despite stable integration of the gene into the

SUBMITTER: Rios-Perez EB 

PROVIDER: S-EPMC8663138 | biostudies-literature | 2021 Jul-Aug

REPOSITORIES: biostudies-literature