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September 1, 1998The Journal of PhysiologyOpen Access

Modulation of human erg K+ channel gating by activation of a G protein‐coupled receptor and protein kinase C

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Population

Two-electrode voltage-clamped Xenopus oocytes co-expressing the human ether-à-go-go-related gene K+ channel…

Comparison

Addition of thyrotropin-releasing hormone or… vs Control conditions or presence of GF109203X

Design

Preclinical

Authors

FBFrancisco BarrosUniversidad de OviedoDGDavid Gómez‐VarelaUniversity of ViennaCVCristina G. ViloriaUniversidad de Oviedo

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Implication

Hypothesis-generating for PKC-HERG modulation; leaves open translation to human arrhythmia risk.

Structured PICO

P
Population
Two-electrode voltage-clamped Xenopus oocytes co-expressing the human ether-à-go-go-related gene (HERG) K+ channel protein and the thyrotropin-releasing hormone (TRH) receptor
I
Intervention
Addition of thyrotropin-releasing hormone (TRH) or direct pharmacological activation of protein kinase C (PKC) with beta-phorbol 12-myristate, 13-acetate (PMA)
C
Comparator
Control conditions or presence of GF109203X (a specific inhibitor of PKC)
O
Outcome
Modifications of HERG channel gating kinetics (deactivation, activation time course, and voltage dependence)surrogate

A PKC-dependent pathway links G protein-coupled receptors to the modulation of HERG channel gating, providing a mechanism for physiological regulation of cardiac function.

Cite This Study

Barros et al. (1998) studied this question.

synapsesocial.com/papers/6a7e1401fc4f0e65bd3bfa74https://doi.org/10.1111/j.1469-7793.1998.333bh.x
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Also Consider

Synapse has enriched 5 closely related papers on similar clinical questions. Consider them for comparative context:

  1. 1Fast inactivation causes rectification of the IKr channel.1996 · 397 citations
  2. 2A Novel Role for HERG K+ Channels: Spike‐Frequency Adaptation1997 · 180 citations
  3. 3Time, voltage and ionic concentration dependence of rectification of h‐<i>er</i>g expressed in <i>Xenopus</i> oocytes1996 · 77 citations
  4. 4Class III Antiarrhythmic Drugs Block HERG, a Human Cardiac Delayed Rectifier K<sup>+</sup>Channel1996 · 287 citations
  5. 5Blockade of HERG channels expressed in <i>Xenopus</i> oocytes by the histamine receptor antagonists terfenadine and astemizole1996 · 229 citations