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Statements

Pyraclofos activates KCNH2. 74 / 74
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"We further evaluated the effect of HW-0168 on voltage dependent activation and inactivation of hERG current."
31481348
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"The normalized I tail reflects a voltage-dependent activation of the HERG channels."
16860311
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"To examine the effect of Celastrol on voltage dependent activation of hERG channels, we normalized I–V relationships for peak tail currents."
31667381
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"However, when using the perforated patch-clamp in HEK-293 cells, trazodone did not modify the voltage-dependent activation of I hERG ( Fig. 6 C) and the blocking effect of trazodone was not voltage-de[MISSING/INVALID CREDENTIALS: limited to 200 char for Elsevier]"
24412489
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"Depolarizing voltage pulses were applied for 2.2 s to voltages between −80 and +100 mV in 10 mV increments (0.1 Hz) to activate hERG channels, and tail currents were recorded during a constant repolar[MISSING/INVALID CREDENTIALS: limited to 200 char for Elsevier]"
22314138
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"The half-maximal hERG activation voltage ( V 1/2 ) was not significantly affected by the R744P mutation (hERG WT, V 1/2 = −6.6 ± 1.7 mV; hERG R744P, V 1/2 = 8.7 ± 0.5 mV; hERG WT + hERG R744P, V 1/2 =[MISSING/INVALID CREDENTIALS: limited to 200 char for Elsevier]"
22314138
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"The hERG current was fully activated and inactivated by a voltage depolarized to +60 mV followed by –100 mV for 10 ms, and then to test steps of different voltages to observe inactivation time course [MISSING/INVALID CREDENTIALS: limited to 200 char for Elsevier]"
26689773
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"The normalized I tail reflects the voltage dependent activation of the HERG channels."
18191158
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"This rightward shift in voltage‐dependent activation of hERG was associated with a slower rise‐time of currents during the activating command at some voltages."
33091232
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"This indicates that maintenance of the consensus site for PKA phosphorylation in the amino-terminus is not necessary for the TRH induced modifications of HERG activation voltage dependence.The shifts [MISSING/INVALID CREDENTIALS: limited to 200 char for Elsevier]"
12560090
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"Fig. 2 A (control) shows the HERG currents elicited by voltage steps ranging from -120 to +40 mV applied in 10 mV increments from the holding potential of -80 mV."
10422790
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"The present results are consistent with, and extend, the 2008 study showing that Src inhibition did not change the voltage dependent activation of hERG XREF_BIBR."
24587194
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"APETx1 is a gating-modifier toxin that binds to the VSD and inhibits the voltage-dependent activation of hERG, thus stabilizing the resting-state, S4-down conformation of the VSD [ xref , xref ]."
33413079
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"In order to characterise the block of HERG by erythromycin [10–12] in our mammalian cell system, HERG current tails elicited by the voltage protocol in Fig. 1 A (lower panel) were compared before and [MISSING/INVALID CREDENTIALS: limited to 200 char for Elsevier]"
16446155
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"The ether-a-go-go related gene encodes the conducting α-subunit of the human voltage-activated K + channel hERG [1] ."
23277102
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"Before and after perfusion of 1μM Celastrol, the V was -15.7 ± 1.07mV (n = 5) and -15.2 ± 0.46 mV (n = 5), and the slope was 8.66 ± 0.55 and 8.67 ± 0.22 respectively.To examine the effect of Celastrol on voltage dependent activation of hERG channels, we normalized I–V relationships for peak tail currents."
31667381
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"Atazanavir has been reported not to alter voltage dependent activation or inactivation of wild-type (WT) hERG current (I hERG ), but protocols to interrogate a requirement for channel opening were not applied ( xref )."
34017865
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"In addition, we studied the voltage dependence of hERG block and also provided evidence for drug-induced hyperpolarizing shifts in voltage-dependent activation of hERG channels, as well as smaller hyperpolarizing shifts of voltage-dependent inactivation of hNav1.5 channels."
34785211
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"This unusual gating property enables tests of the mechanism by which voltage induces facilitation of hERG by blockers."
36041862
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"Significance Statement Nifekalant is a clinically important antiarrhythmic agent and a hERG blocker which can also facilitate voltage-dependent activation of hERG channels after a preconditioning pulse."
36041862
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"In addition, we studied the voltage dependence of hERG block and also provided evidence for drug-induced hyperpolarizing shifts in voltage-dependent activation of hERG channels, as well as smaller hyperpolarizing shifts of voltage-dependent inactivation of hNav1.5 channels."
34785211
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"The results of the present study demonstrated that the level and duration of voltage steps that activate HERG channels influenced potency estimation for some, but not all, compounds."
15936218
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"Since hiPSC-CMs likely contain other voltage activated ionic currents, we investigated the hERG component of the voltage activated currents, by isolating hERG current as an E-4031-sensitive current."
25923442
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"A key hERG mutation, E518C, caused the large positive shifts in the hERG activation voltage."
33413079
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"The enhancement on voltage dependent activation of hERG current resemble the effects reported for majority of hERG openers."
31481348
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"Manual hERG Test Voltage Protocol: the hERG current was elicited from a holding potential of −80 mV by a voltage step to +60 mV for 2000 ms, followed by repolarization to −40 mV."
37759755
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"For the automated patch clamp procedure, once a stable whole-cell configuration was achieved, cells were held at a resting voltage of ∼80 mV and then stimulated by a voltage pattern to activate hERG c[MISSING/INVALID CREDENTIALS: limited to 200 char for Elsevier]"
18448342
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"Voltage dependent activation of HERG currents became faster at negative test voltages but there were no changes at positive voltages after cibenzoline."
15168062
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"Our objective was to test two potential sources of variability within the same test system: the temperature at which the recordings are performed ( Crumb, 2000 ) and the voltage pulse protocol used to[MISSING/INVALID CREDENTIALS: limited to 200 char for Elsevier]"
15385083
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"The enhancement on voltage dependent activation of hERG current resemble the effects reported for majority of hERG openers."
31481348
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"Like other K v channels, hERG is activated by membrane voltage; however, distinct from other K v channels, hERG channels have unusually slow kinetics of closing (deactivation)."
22522181
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"If this approach could be combined with voltage clamp stimuli that allow very fast determination of all relevant hERG kinetics in a few seconds, cell-specific models can be made that can capture the h[MISSING/INVALID CREDENTIALS: limited to 200 char for Elsevier]"
30826123
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"The normalized I tail reflects a voltage dependent activation of the HERG channels."
19949665
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"Wild-type HERG channels treated with TMRM showed no voltage dependent changes in fluorescence (unpublished results); therefore, it is unlikely that the observed fluorescence changes are from TMRM labeling of native cysteines in other regions of the channel."
11865022
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"However, PI(4)P5-K itself had little, if any, effect on the amplitude or voltage-dependent activation of I HERG ( Fig. 3 and Table 1 )."
25704028
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"The HERG current was elicited by 0.4-s voltage steps from -80 to +20 mV, followed by a 0.4-s step to -60 mV to record outward tail currents at intervals of 2, 6 and 15 s."
12460639
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"Two voltage protocols were used to activate hERG channels (XREF_FIG)."
23934164
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"APETx1 is a gating-modifier toxin that binds to the VSD and inhibits the voltage dependent activation of hERG, thus stabilizing the resting-state, S4-down conformation of the VSD [XREF_BIBR, XREF_BIBR]."
33413079
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"The normalized I tail reflects a voltage-dependent activation of the HERG channels."
16860311
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"These observations invoke the need to understand the underlying deactivation regulatory mechanisms.Recent studies suggest that voltage sensor relaxation contributes to slow deactivation in hERG channels (Tan et al., 2012; Goodchild and Fedida, 2014; Thouta et al., 2017)."
30530765
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"Although in situ Fuc editing had no apparent impact on the voltage dependent activation of hERG channel, it was detected to have a major influence on the hERG maximum current by whole-cell voltage-clamp experiments."
29292859
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"The insets to XREF_FIG A and B show the voltage protocol used to elicit I hERG, which was similar to that applied in prior hERG channel studies from our laboratory."
31049424
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"The hERG current ( I hERG ) was induced by single 2 s voltage pulse to +20 mV from the holding potential of −80 mV and a repolarization to −40 mV."
17010640
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"The voltage protocol shown in XREF_FIG was used to activate hERG channels and trigger I kr current (XREF_FIG)."
25286396
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"Similar to other Kv channels, hERG1 is activated by voltage."
20544339
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"The mutation A536W, which switches the voltage dependent activation of hERG K + channels to a much more negative potential 30, was expected to alter cell excitability and consequently induce behavioral defects in worms."
30258187
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"The voltage-dependent activation, inactivation and deactivation of hERG1 channels are depicted in Fig. 3 ."
19351523
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"HERG K + currents were elicited by 1-s depolarizing voltage steps to +20 mV from a holding potential of -80 mV followed by a 1-s repolarization back to -40 mV."
11040340
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"Deletion of the N terminal hERG‐specific domain between residues 138–373 has previously been reported to produce a negative shift in voltage‐dependent activation of I hERG , (Viloria, Barros, Giraldez, Gomez‐Varela, & de la Pena,  xref ), implicating this region in modulation of activation kinetics."
33091232
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"Through application of a protocol in which the command voltage of the 2s pulse was varied between −40 and + 60 mV [ xref , xref ], tail current analysis was performed to characterise voltage-dependent activation of T618I I hERG ( xref B)."
35114584
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"The normalized I tail reflects the voltage-dependent activation of the hERG channels."
19497368
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"The fourth transmembrane segment (S4) contributes to form the voltage sensor domain (VSD), which sharply contributes to hERG1 biophysical properties [XREF_BIBR]."
26339650
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"The 4 s–4 s protocol accelerated the voltage-dependent activation of hERG current."
15936217
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"The internal solution contained (in mM): 92 CsF, 55 CsCl, 2 MgCl 2 , 5 EGTA, 5 HEPES, 1 MgATP, pH 7.2, 300 mOsM.The hERG current was elicited from a holding potential of −80 mV by a voltage step to +4[MISSING/INVALID CREDENTIALS: limited to 200 char for Elsevier]"
36084863
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"In recent years, it has been recognized that less proarrhythmic hERG blockers with clinical potential or Class III antiarrhythmic agents exhibit, in addition to their hERG-blocking activity, a second action that facilitates the voltage-dependent activation of the hERG channel."
38003453
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"The normalized I tail reflects the voltage-dependent activation of the hERG channels."
19497368
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"The voltage required to half-maximally activate HERG was shifted slightly from − 16.2 ± 2.4 mV in control to − 18.1 ± 1.8 mV with exposure to prucalopride (P < 0.05, n = 7; Fig. 1 B)."
17109852
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"Voltage activation of Kv11.1 (hErg1) is highly pH sensitive in low external Ca 2+."
23712551
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"In the present study, PCB 126 increased the amplitude of I hERG at the end of the step pulse concentration-dependently and showed the voltage-dependent augmentation of the I hERG ."
22676973
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"Co-expressing WT and hERG-T634S suppressed I hERG tails by ∼57% compared to WT alone, without significant alteration of voltage dependent activation of I hERG ."
32321643
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"Collectively, the data in xref B–D shows that T634S led a marked loss of hERG channel function over a wide range of experimental voltages, without a significant shift in voltage-dependent activation of I hERG ."
32321643
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"The I-V curve of I tail shows a voltage dependent activation of hERG channels that reached a steady-state at +30 mV."
19543501
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"First, voltage dependent block of the channel might decrease HERG current at potentials less than +50 mV, producing an apparent shift in the voltage dependent activation of the channels."
10102937
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"This general property of drugs to exert hyperpolarizing shifts in voltage-dependent hERG activation in addition to block was named facilitation by Perry, Sanguinetti and Mitcheson ( xref )."
34785211
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"In our experiments, suppression of WT I hERG was marked at positive but not negative voltages, and was accompanied by a ~−8 mV leftward shift in the voltage-dependent activation of WT I hERG ."
21989164
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"Like other K v channels, hERG is activated by membrane voltage; however, distinct from other K v channels, hERG channels have unusually slow kinetics of closing (deactivation)."
22522181
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"SCN5A encodes an alpha subunit of voltage-gated Na + channel while KCNH2 transcripts encode a voltage-activated potassium channel (hERG)."
28622605
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"Modulation of hERG K + Channel Deactivation by Voltage Sensor Relaxation."
32184724
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"Difference in the expression of K-calcium-activated channel KCNN4 and over-expression of the voltage-activated potassium channel KCNH2 are associated with poorer prognosis of patients diagnosed with pancreatic cancer ( xref )."
38694937
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"Additionally, the time- and voltage-dependent kinetics were restored to near hERG levels (Figures 6D–6G), consistent with the notion that the functional channels consist of mostly hERG subunits in the form of homotetramers instead of heterotetramers as in Figures 1E–1H."
34634443
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"Without nifekalant, this voltage protocol induced little, if any, increase in hERG current (Fig. 1 D)."
30674563
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"Significance Statement Nifekalant is a clinically important antiarrhythmic agent and a hERG blocker which can also facilitate voltage-dependent activation of hERG channels after a preconditioning pulse."
36041862
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"HERG currents were elicited by 1-s voltage pulses to + 30 mV (0.25 Hz), from a holding potential of − 80 mV followed by a repolarizing ramp (0.5 mV/ms) back to − 80 mV."
19442753
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"Using several mutations as tools, we define key steps in the deactivation pathway that limit voltage sensor return to produce the physiologically relevant resurgent hERG current in cardiomyocytes.Wild[MISSING/INVALID CREDENTIALS: limited to 200 char for Elsevier]"
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