Article
Inhibition of the HERG K+ channel by the antifungal drug ketoconazole depends on channel gating and involves the S6 residue F656.
FEBS letters - 3 Apr 2006
Ridley John M, Milnes James T, Duncan Rona S, McPate Mark J, James Andrew F, Witchel Harry J, Hancox Jules C
Abstract excerpt
The mechanism of human ether-à-go-go-related gene (HERG) K+ channel blockade by the antifungal agent ketoconazole was investigated using patch-clamp recording from mammalian cell lines. Ketoconazole inhibited whole-cell HERG current (IHERG) with a clinically relevant half-maximal inhibitory drug concentration (IC50) value of 1.7 microM. The voltage- and time-dependent characteristics of IHERG blockade by...
Read the complete abstract on PubMedTopics
Share this publication in a Topic to start or enrich a Post.
