The novel fluorogenic probe A1 provides a promising new toolkit for imaging the hERG potassium channel in basic electrophysiology research without significantly altering its function.
May enable hERG imaging in preclinical models; leaves open clinical translation and human validation.
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.
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Liu et al. (2015) studied this question.
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