Astemizole Derivatives as Fluorescent Probes for hERG Potassium Channel Imaging

Beilei Wang; Zhenzhen Liu; Zhao Ma; Minyong Li; Lupei Du

doi:10.1021/acsmedchemlett.5b00360

Astemizole Derivatives as Fluorescent Probes for hERG Potassium Channel Imaging

ACS Med Chem Lett. 2016 Jan 20;7(3):245-9. doi: 10.1021/acsmedchemlett.5b00360. eCollection 2016 Mar 10.

Authors

Beilei Wang¹, Zhenzhen Liu¹, Zhao Ma¹, Minyong Li¹, Lupei Du¹

Affiliation

¹ Department of Medicinal Chemistry, Key Laboratory of Chemical Biology (MOE), School of Pharmacy, Shandong University , Jinan, Shandong 250012, China.

Abstract

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.

Keywords: astemizole; cell imaging; fluorescent probes; hERG potassium channel.