Fluorogenic Probe for the Human Ether-a-Go-Go-Related Gene Potassium Channel Imaging
نویسندگان
چکیده
The first small-molecule fluorogenic probe A1 for imaging the human Ether-a-go-go-Related Gene (hERG) potassium channel based on the photoinduced electron transfer (PET) off-on mechanism was described herein. After careful biological evaluation, this probe had the potential of detecting and imaging the hERG channel at the molecular and cellular level. Moreover, the competitive binding mechanism of this probe would presumably minimize the effects on the electrophysiological properties of the hERG channel. Therefore, this probe may serve as a powerful toolkit to the hERG-associated study.
منابع مشابه
Environment-Sensitive Fluorescent Probe for the Human Ether-a-go-go-Related Gene Potassium Channel
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 wi...
متن کاملHuman Ether-à-go-go–related Gene K+ Channel Gating Probed with Extracellular Ca2+
Human ether-à-go-go-related gene (HERG) encoded K+ channels were expressed in Chinese hamster ovary (CHO-K1) cells and studied by whole-cell voltage clamp in the presence of varied extracellular Ca2+ concentrations and physiological external K+. Elevation of external Ca2+ from 1.8 to 10 mM resulted in a reduction of whole-cell K+ current amplitude, slowed activation kinetics, and an increased r...
متن کاملAPETx1, a new toxin from the sea anemone Anthopleura elegantissima, blocks voltage-gated human ether-a-go-go-related gene potassium channels.
A new peptide, APETx1, which specifically inhibits human ether-a-go-go-related gene (HERG) channels, was purified from venom of the sea anemone Anthopleura elegantissima. APETx1 is a 42-amino acid peptide cross-linked by three disulfide bridges and shares 54% homology with BDS-I, another sea anemone K+ channel inhibitor. Although they differ in their specific targets, circular dichroism spectra...
متن کاملInhibitory effect of rhynchophylline on human ether-a-go-go related gene channel.
We studied the effects of Chinese traditional medicine rhynchophylline (Rhy) on human ether-a-go-go related gene (HERG) channel and characterized the electrophysiological properties of Rhy's pharmacological effect on HERG channel using Xenopus oocytes. Xenopus oocytes were injected with either 23 nl (5.75 ng) HERG cRNA or 23 nl distilled water. Xenopus oocytes were randomly assigned to receive ...
متن کاملMolecular determinants of cocaine block of human ether-á-go-go-related gene potassium channels.
The use of cocaine causes cardiac arrhythmias and sudden death. Blockade of the cardiac potassium channel human ether-á-go-go-related gene (hERG) has been implicated as a mechanism for the proarrhythmic action of cocaine. hERG encodes the pore-forming subunits of the rapidly activating delayed rectifier K(+) channel (I(Kr)), which is important for cardiac repolarization. Blockade of I(Kr)/hERG ...
متن کامل