Modeling HERG Isoforms
نویسندگان
چکیده
منابع مشابه
hERG Gating Microdomains Defined by S6 Mutagenesis and Molecular Modeling
Human ether-à-go-go-related gene (hERG) channels mediate cardiac repolarization and bind drugs that can cause acquired long QT syndrome and life-threatening arrhythmias. Drugs bind in the vestibule formed by the S6 transmembrane domain, which also contains the activation gate that traps drugs in the vestibule and contributes to their efficacy of block. Although drug-binding residues have been i...
متن کاملPredictive in silico modeling for hERG channel blockers.
hERG-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. Several in silico approaches have attempted to predict hERG channel blockade. Some of th...
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Protein kinases C (PKC) modulate the activity of the Kv11.1 ion channel current (hERG). However, the differential effects of specific PKC subtypes on the biophysics of the channel are unknown. The pharmaceutical tools to selectively modulate PKC subtypes are not membrane permeable and must be added directly to the intracellular solution in electrophysiology studies. Here, the PatchXpress electr...
متن کاملModels of HERG gating.
HERG (Kv11.1, KCNH2) is a voltage-gated potassium channel with unique gating characteristics. HERG has fast voltage-dependent inactivation, relatively slow deactivation, and fast recovery from inactivation. This combination of gating kinetics makes study of HERG difficult without using mathematical models. Several HERG models have been developed, with fundamentally different organization. HERG ...
متن کاملCardiaC toxiCity herg
One of the major reasons of drug withdrawal or drug label revision is the drug induced sudden cardiac death associated with a prolongation of the QT interval in the electrocardiogram (ECG). When the QT interval is prolonged, there is an increased risk of ventricular tachyarrhythmia, including the life threatening form torsade de pointes. The QT interval of the ECG is a measure of the duration o...
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ژورنال
عنوان ژورنال: Biophysical Journal
سال: 2013
ISSN: 0006-3495
DOI: 10.1016/j.bpj.2012.11.1485