IndraLab

Statements

Pentamidine inhibits KCNH2. 13 / 13
3 | 10
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"For example, the antiarrhythmic agents ketoconazole and fluoxetine have been shown to reduce hERG density by at least 50% following 48 hours of treatment, XREF_BIBR - XREF_BIBR whereas pentamidine and probucol reduce cell-surface hERG without affecting ion conduction."
20156596
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"Molecular determinants of pentamidine induced hERG trafficking inhibition."
22046004
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"The drug pentamidine, at near therapeutic concentrations that do not cause direct KCNH2 channel block, disrupts normal KCNH2 channel protein processing and maturation to reduce its surface membrane expression."
15711590
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"As expected, pentamidine (10muM), a reference compound known to inhibit hERG trafficking, significantly inhibited the hERG tail current amplitude by 57%, a value in good agreement with the literature (Kuryshev et al., 2005)."
28941245
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"XREF_BIBR Pentamidine impedes hERG trafficking from endoplasmic reticulum (ER) to cell membrane."
26543354
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"Pentamidine and desipramine were reported to suppress hERG forward trafficking to the cell surface, and the aromatic amino F656 mediated the effects of pentamidine [XREF_BIBR, XREF_BIBR]."
27690007
ctd
No evidence text available
21158687
ctd
No evidence text available
15711590
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"Subsequently, the antimicrobial agent pentamidine was also found to impair hERG function by acting as a trafficking inhibitor (Kuryshev et al., 2005; Cordes et al., 2005)."
18616963
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"In contrast, pentamidine had no direct effect on the hERG channel current but reduced trafficking of hERG channels."
25366487
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"Pentamidine and desipramine were reported to suppress hERG forward trafficking from the endoplasmic reticulum, and the aromatic amino F656 in S6 domain mediated the effects of pentamidine [XREF_BIBR, XREF_BIBR]."
27690007
ctd
No evidence text available
19652455
reach
"XREF_BIBR Invitro experiments showed that despite being a poor direct blocker of I Kr at therapeutic concentrations, XREF_BIBR pentamidine inhibits hERG trafficking (XREF_FIG), causing action potential prolongation in both animal and human cells."
33763655