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Predictive in silico modeling for hERG channel blockers
Drug Discovery Today, 2005hERG-mediated sudden death as a side effect of non-antiarrhythmic drugs has been receiving increased regulatory attention. Perhaps owing to the unique shape of the ligand-binding site and its hydrophobic character, the hERG channel has been shown to interact with pharmaceuticals of widely varying structure.
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Ligand Structural Aspects of hERG Channel Blockade
Current Topics in Medicinal Chemistry, 2008Sudden death as a side effect of action of non-antiarrhythmic drugs is a major pharmacological safety concern facing the pharmaceutical industry and the health regulatory authorities. A number of drugs have been withdrawn from the market in recent years due to cardiovascular toxicity associated with undesirable blockade of hERG potassium channel ...
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Cryo-EM Structure of K+-Bound hERG Channel Complexed with the Blocker Astemizole
Structure, 2021Satoshi Ogasawara +2 more
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Insights into hERG channel activators
The human Ether-a-go-go-Related Gene (hERG) potassium channel plays a crucial role in cardiac repolarization. Dysfunction of this channel can lead to severe cardiac arrhythmias, particularly Long QT Syndrome (LQTS), which is associated with an increased risk of torsades de pointes and sudden cardiac death.openaire +1 more source
HERG channel and cancer: A mechanistic review of carcinogenic processes and therapeutic potential
Biochimica Et Biophysica Acta: Reviews on Cancer, 2020Amit R L Persad, Humphrey Fonge
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Cryo-EM Structure of the Open Human Ether-à-go-go-Related K+ Channel hERG
Cell, 2017Roderick MacKinnon, Weiwei Wang
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Mechanism of Block and Identification of the Verapamil Binding Domain to HERG Potassium Channels
Circulation Research, 1999Shetuan Zhang +2 more
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Facilitation of hERG Current Occurs in Various hERG Channel Blockers
Journal of Molecular and Cellular Cardiology, 2008Atsushi Inanobe +2 more
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