Towards a Structural View of Drug Binding to hERG K + Channels
نویسندگان
چکیده
منابع مشابه
Drug trapping in hERG K+ channels: (not) a matter of drug size?
Inhibition of hERG K+ channels by structurally diverse drugs prolongs the ventricular action potential and increases the risk of torsade de pointes arrhythmias and sudden cardiac death. The capture of drugs behind closed channel gates, so-called drug trapping, is suggested to harbor an increased pro-arrhythmic risk. In this study, the trapping mechanisms of a trapped hERG blocker propafenone an...
متن کاملIntracellular K+ is required for the inactivation-induced high-affinity binding of cisapride to HERG channels.
Many commonly used medications can cause long QT syndrome and thus increase the risk of life-threatening arrhythmias. High-affinity human Ether-à-go-go-related gene (HERG) potassium channel blockade by structurally diverse compounds is almost exclusively responsible for this side effect. Understanding drug-HERG channel interactions is an important step in avoiding drug-induced long QT syndromes...
متن کاملHERG-like K+ Channels in Microglia
A voltage-gated K+ conductance resembling that of the human ether-à-go-go-related gene product (HERG) was studied using whole-cell voltage-clamp recording, and found to be the predominant conductance at hyperpolarized potentials in a cell line (MLS-9) derived from primary cultures of rat microglia. Its behavior differed markedly from the classical inward rectifier K+ currents described previous...
متن کاملSaxitoxin Is a Gating Modifier of hERG K+ Channels
Potassium (K+) channels mediate numerous electrical events in excitable cells, including cellular membrane potential repolarization. The hERG K+ channel plays an important role in myocardial repolarization, and inhibition of these K+ channels is associated with long QT syndromes that can cause fatal cardiac arrhythmias. In this study, we identify saxitoxin (STX) as a hERG channel modifier and i...
متن کاملAntiarrhythmic drug carvedilol inhibits HERG potassium channels.
OBJECTIVE The aryloxypropanolamine carvedilol is a multiple action cardiovascular drug with blocking effects on alpha-receptors, beta-receptors, Ca(2+)-channels, Na(+)-channels and various native cardiac K(+) channels, thereby prolonging the cardiac action potential. In a number of clinical trials with patients suffering from congestive heart failure, carvedilol appeared to be superior to other...
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ژورنال
عنوان ژورنال: Trends in Pharmacological Sciences
سال: 2017
ISSN: 0165-6147
DOI: 10.1016/j.tips.2017.06.004