IndraLab

Statements

Pyraclofos activates KCNH2. 43 / 43
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"A key hERG mutation, E518C, caused the large positive shifts in the hERG activation voltage."
33413079
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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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"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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"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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"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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"Two voltage protocols were used to activate hERG channels (XREF_FIG)."
23934164
sparser
"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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"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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"Modulation of hERG K + Channel Deactivation by Voltage Sensor Relaxation."
32184724
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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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"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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"Atazanavir has been reported not to alter voltage dependent activation or inactivation of wild-type (WT) hERG current (IhERG), but protocols to interrogate a requirement for channel opening were not applied (39)."
34017865
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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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"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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"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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"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 (Perry et al., 2010)."
34785211
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"Voltage activation of Kv11.1 (hErg1) is highly pH sensitive in low external Ca 2+."
23712551
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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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"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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"Our objective was to evaluate two potential sources of variability : the temperature at which recordings are performed and the voltage pulse protocol used to activate hERG K (+) channels expressed in HEK293 cells."
15385083
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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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"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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"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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"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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"Similar to other Kv channels, hERG1 is activated by voltage."
20544339
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"The normalized I tail reflects a voltage dependent activation of the HERG channels."
19949665
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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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"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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"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]"
28122216
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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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"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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"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 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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"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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"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
sparser
"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
sparser
"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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"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 voltage protocol shown in XREF_FIG was used to activate hERG channels and trigger I kr current (XREF_FIG)."
25286396
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"The normalized I tail reflects the voltage dependent activation of the HERG channels."
18191158
sparser
"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
sparser
"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