Premium
Inhibition of hERG Channel Trafficking: An Under‐Explored Mechanism for Drug‐Induced QT Prolongation
Author(s) -
Yeung KapSun,
Meanwell Nicholas A.
Publication year - 2008
Publication title -
chemmedchem
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.817
H-Index - 100
eISSN - 1860-7187
pISSN - 1860-7179
DOI - 10.1002/cmdc.200800170
Subject(s) - herg , long qt syndrome , pharmacology , qt interval , ketoconazole , chemistry , potassium channel , astemizole , medicine , antifungal , dermatology
hERG channel trafficking inhibition leads to QT prolongation : Drugs that cause long QT syndrome usually do so by directly blocking the hERG channel through binding in the pore domain. However, an increasing number of drugs, including the widely prescribed antifungal ketoconazole and the antidepressant fluoxetine, can induce long QT syndrome by an indirect effect in which hERG channel expression at the cell surface is reduced.