MOL # 75135 1 Molecular determinants of pentamidine - induced hERG trafficking inhibition
نویسندگان
چکیده
The abbreviations used are: acLQTS, acquired long QT syndrome; astemizole,
منابع مشابه
Molecular determinants of pentamidine-induced hERG trafficking inhibition.
Pentamidine is an antiprotozoal compound that clinically causes acquired long QT syndrome (acLQTS), which is associated with prolonged QT intervals, tachycardias, and sudden cardiac arrest. Pentamidine delays terminal repolarization in human heart by acutely blocking cardiac inward rectifier currents. At the same time, pentamidine reduces surface expression of the cardiac potassium channel I(Kr...
متن کاملPentamidine-induced long QT syndrome and block of hERG trafficking.
The diamidine pentamidine is used to treat leishmaniasis, trypanosomiasis, and Pneumocystis carinii pneumonia. Treatment may be accompanied by prolongation of the QT interval of the electrocardiogram and torsades de pointes tachycardias. Up to now, it has been thought that therapeutic compounds causing QT prolongation are associated with direct block of the cardiac potassium channel human ether...
متن کاملhERG channel trafficking: novel targets in drug-induced long QT syndrome.
The cardiac potassium channel hERG (human ether-a-go-go-related gene) encodes the alpha-subunit of the rapid delayed rectifier current I(Kr) in the heart, which contributes to terminal repolarization in human cardiomyocytes. Direct block of hERG/I(Kr) channels by a large number of therapeutic compounds produces acLQTS [acquired LQTS (long QT syndrome)] characterized by drug-induced QT prolongat...
متن کاملIntracellular potassium stabilizes human ether-à-go-go-related gene channels for export from endoplasmic reticulum.
Several therapeutic compounds have been identified that prolong the QT interval on the electrocardiogram and cause torsade de pointes arrhythmias not by direct block of the cardiac potassium channel human ether-à-go-go-related gene (hERG) but via disruption of hERG trafficking to the cell surface membrane. One example of a clinically important compound class that potently inhibits hERG traffick...
متن کاملStereoselective Blockage of Quinidine and Quinine in the hERG Channel and the Effect of Their Rescue Potency on Drug-Induced hERG Trafficking Defect
Diastereoisomers of quinidine and quinine are used to treat arrhythmia and malaria, respectively. It has been reported that both drugs block the hERG (human ether-a-go-go-related gene) potassium channel which is essential for myocardium repolarization. Abnormality of repolarization increases risk of arrhythmia. The aim of our research is to study and compare the impacts of quinidine and quinine...
متن کاملذخیره در منابع من
با ذخیره ی این منبع در منابع من، دسترسی به آن را برای استفاده های بعدی آسان تر کنید
عنوان ژورنال:
دوره شماره
صفحات -
تاریخ انتشار 2011