Astemizole Derivatives as Fluorescent Probes for hERG Potassium Channel Imaging

作者:Wang, Beilei; Liu, Zhenzhen; Ma, Zhao; Li, Minyong; Du, Lupei*
来源:ACS Medicinal Chemistry Letters, 2016, 7(3): 245-249.
DOI:10.1021/acsmedchemlett.5b00360

摘要

The detection and imaging of hERG potassium channels in living cells can provide useful information for hERG-correlation studies. Herein, three small-molecule fluorescent probes, based on the potent hERG channel inhibitor astemizole, for the imaging of hERG channels in hERG-transfected HEK293 cells (hERG-HEK293) and human colorectal cancer cells (HT-29), are described. These probes are expected to be applied in the physiological and pathological studies of hERG channels.