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钾离子通道是分布最为广泛、种类繁多的一类离子通道,因其生理功能的多样性,已成为许多疾病的药物作用靶点。近年来,许多化学结构不同的药物均因钾离子通道阻滞引起的严重心肌毒性而被撤出市场,使得小分子药物的钾通道抑制活性筛选面临重大挑战。介绍检测钾离子通道的小分子荧光探针的研究进展,并总结小分子荧光探针的作用机制,为今后小分子荧光探针的设计提供思路,使得小分子荧光探针可以广泛应用于候选药物的高通量筛选、钾离子通道的活体成像与检测。
Potassium channels are the most widely distributed and diverse class of ion channels. Due to their diverse physiological functions, potassium channels have become the target of many diseases. In recent years, many drugs with different chemical structures have been withdrawn from the market due to severe myocardial toxicity caused by potassium channel blockade, which makes the screening of potassium channel inhibitory activity of small molecule drugs face major challenges. This paper introduces the research progress of small molecule fluorescent probes for detecting K + channels and summarizes the mechanism of small molecule fluorescent probes so as to provide ideas for the design of small molecule fluorescent probes in future so that small molecule fluorescent probes can be widely used in drug candidates High throughput screening, in vivo imaging and detection of potassium channels.