Environment-Sensitive Fluorescent Probe for the Human Ether-a-go-go-Related Gene Potassium Channel
Author(s) -
Zhenzhen Liu,
Tianyu Jiang,
Beilei Wang,
Bowen Ke,
Yubin Zhou,
Lüpei Du,
Minyong Li
Publication year - 2016
Publication title -
analytical chemistry
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 2.117
H-Index - 332
eISSN - 1520-6882
pISSN - 0003-2700
DOI - 10.1021/acs.analchem.5b04220
Subject(s) - herg , chemistry , potassium channel , fluorescence , channel (broadcasting) , potassium channel blocker , biophysics , potassium , nanotechnology , organic chemistry , physics , materials science , engineering , quantum mechanics , electrical engineering , biology
A novel environment-sensitive probe S2 with turn-on switch for Human Ether-a-go-go-Related Gene (hERG) potassium channel was developed herein. After careful evaluation, this fluorescent probe showed high binding affinity with hERG potassium channel with an IC50 value of 41.65 nM and can be well applied to hERG channel imaging or cellular distribution study for hERG channel blockers. Compared with other imaging techniques, such as immunofluorescence and fluorescent protein-based approaches, this method is convenient and affordable, especially since a washing procedure is not needed. Meanwhile, this environment-sensitive turn-on design strategy may provide a good example for the probe development for these targets that have no reactive or catalytic activity.
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