IndraLab

Statements

Fluconazole inhibits KCNH2. 7 / 7
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"Whether fluconazole also inhibits hERG is currently unknown."
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"HERG currents were blocked by fluconazole in a concentration-dependent manner."
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"In the present study, it was found that fluconazole directly inhibits the cellular hERG current expressed in HEK293 cells with an IC 50 of 48.2 μM. Recently, Katchman et al. (2006) classified drugs fo[MISSING/INVALID CREDENTIALS: limited to 200 char for Elsevier]"
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"By studying the effect of fluconazole on the human ether-a-go-go-related gene (hERG) K channels (wild type, F656C, and Y652A) expressed in human embryonic kidney (HEK293) cells, Han et al. found that the mechanism by which fluconazole causes acquired long QT syndrome (LQTS) may be through direct inhibition of hERG currents and disruption of hERG protein transport; the obligatory determinants of hERG current inhibition by fluconazole are the Y652 and F656 molecular mutations."
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"The precise mechanism by which fluconazole reduces the cell surface expression of the hERG channel protein remains to be determined."
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"We have also demonstrated that Y652 and F656 are critical molecular determinants for the block of the hERG channels by fluconazole."
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"Whether fluconazole also inhibits hERG is currently unknown."
19570657