IndraLab

Statements

Pentamidine inhibits KCNH2. 26 / 29
3 | 26
reach
"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
reach
"Further study of the functional effects and molecular mechanisms of 17-AAG is required, and analyses of the expression levels of each cardiac channel in human cardiomyocytes may also be warranted.In c[MISSING/INVALID CREDENTIALS: limited to 200 char for Elsevier]"
30391349
reach
"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
reach
"It was found that pentamidine does not block cardiac ion channels but rather disrupts hERG processing and maturation, reducing surface expression and hERG current density, at therapeutic concentration[MISSING/INVALID CREDENTIALS: limited to 200 char for Elsevier]"
16344000
reach
"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
reach
"Arsenic trioxide and pentamidine inhibit hERG protein trafficking rather than directly inhibiting the channel action ( Ficker et al., 2004; Cordes et al., 2005 )."
20951697
reach
"Pentamidine has been reported to block the transport of hERG channels to the cardiomyocyte plasma membrane ."
35931748
reach
"XREF_BIBR Pentamidine impedes hERG trafficking from endoplasmic reticulum (ER) to cell membrane."
26543354
reach
"However, it was especially valuable for detecting delayed arrhythmic activity caused by long-term exposure-induced hERG trafficking inhibition by pentamidine, and non-QT related arrhythmia by the Na +[MISSING/INVALID CREDENTIALS: limited to 200 char for Elsevier]"
27646297
reach
"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
reach
"Subsequent mechanistic studies determined that pentamidine inhibits the trafficking and maturation of hERG, with an IC close to therapeutic doses, upon 24 h incubation in hERG-expressing HEK293 cells (Kuryshev et al., 2005)."
37492082
reach
"Pentamidine) ( Kuryshev et al., 2005 ) inhibited hERG protein trafficking rather than directly inhibiting channel action."
27575519
reach
"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
reach
"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
reach
"Pentamidine was reported to reduce hERG current by interfering with its surface expression, rather than direct ion channel block ( Kuryshev et al., 2005 )."
19616638
reach
"In contrast, pentamidine had no direct effect on the hERG channel current but reduced trafficking of hERG channels."
25366487
reach
"As also observed in earlier studies, pentamidine treatment significantly decreased maturation (mature/immature ratio) of hERG."
35540224
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
reach
"Molecular determinants of pentamidine induced hERG trafficking inhibition."
22046004
reach
"The results showed that both pentamidine and 17-AAG inhibited hERG trafficking in hERG-CHOs, whearas in the MEA assay using hES-CMs, torsadogenic pentamidine, but not non-torsadogenic 17-AAG, prolonge[MISSING/INVALID CREDENTIALS: limited to 200 char for Elsevier]"
30391349
reach
"We have recently shown that another torsadogenic drug, pentamidine, also inhibits hERG trafficking ( Kuryshev et al., 2005 )."
15950494
reach
"Recent studies have also demonstrated that pentamidine-induced hERG trafficking inhibition could be rescued in the presence of the pharmacological chaperone astemizole [30] ."
23103450
reach
"Pentamidine inhibited forward hERG protein maturation ( Fig. 2 A, B)."
30391349
reach
"Our results indicated that chronic exposure of pentamidine inhibited hERG tail current in a concentration-dependent manner (IC 50 : 3–10 μM), and no effect was observed up to 30 μM acutely in hERG-CHO[MISSING/INVALID CREDENTIALS: limited to 200 char for Elsevier]"
30391349
reach
"Pharmacological chaperones such as astemizole and dofetilide are known to abolish the interference of trafficking caused by pentamidine, suggesting that pentamidine may inhibit hERG channel maturation[MISSING/INVALID CREDENTIALS: limited to 200 char for Elsevier]"
30391349
reach
"In accordance with these findings, we observed that the level of protein expression of fully glycosylated, mature hERG channels was reduced by chronic pentamidine exposure in hERG-CHOs ( Fig. 2 B)."
30391349