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Discovery of a novel Nav1.5 inhibitor reducing cardiac conduction via structure-based virtual screening and assays

   
@article{APS11498,
	author = {Ying-ying Wang and Gao-ang Wang and Qing You and Yi-fei Liu and Wang-lin Qu and Yi-hong Chen and Chen-zhang Mu and Xi Zhou and Min Liu and Wei Yang and Ting-jun Hou},
	title = {Discovery of a novel Nav1.5 inhibitor reducing cardiac conduction via structure-based virtual screening and assays},
	journal = {Acta Pharmacologica Sinica},
	volume = {47},
	number = {4},
	year = {2026},
	keywords = {},
	abstract = {Nav1.5 is the main sodium channel subtype in the heart, playing a crucial role in maintaining regular cardiac electrical activity. It is a well-established therapeutic target for class I antiarrhythmic drugs used to treat both inherited and acquired arrhythmias. In this study, we report a highly effective (IC50 = 1.38 ± 0.28 μM) and novel Nav1.5 inhibitor, KH2, identified through an integrated drug discovery approach. Molecular dynamics (MD) simulations and experimental findings reveal that, unlike traditional class I antiarrhythmic drugs, KH2 shows a completely novel binding mechanism. Moreover, using electrophysiological mapping systems on rat isolated hearts, we found that KH2 significantly reduced cardiac conduction, highlighting its potential as a therapeutic agent for arrhythmias. Our finding of KH2 provided a valuable reference for designing drugs targeting Nav1.5 to treat arrhythmias.},
	issn = {1745-7254},	url = {http://www.chinaphar.com/article/view/11498}
}