Title : ICA-105574 interacts with a common binding site to elicit opposite effects on inactivation gating of EAG and ERG potassium channels.

Pub. Date : 2013 Apr

PMID : 23319419






6 Functional Relationships(s)
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1 Although ICA greatly attenuates ERG inactivation by shifting its voltage dependence to more positive potentials, it enhances the rate and extent of EAG inactivation without altering its voltage dependence. isocyanic acid ETS transcription factor ERG Homo sapiens
2 Here, we investigate whether the inverse functional response to ICA in EAG and ERG channels is related to differences in ICA binding site or to intrinsic mechanisms of inactivation. isocyanic acid ETS transcription factor ERG Homo sapiens
3 ICA is a mixed agonist of mutant EAG and EAG/ERG chimera channels that inactivate by a combination of slow and fast mechanisms. isocyanic acid ETS transcription factor ERG Homo sapiens
4 With the exception of three residues, the specific amino acids that form the putative binding pocket for ICA in ERG are conserved in EAG. isocyanic acid ETS transcription factor ERG Homo sapiens
5 Mutations introduced into EAG to replicate the ICA binding site in ERG did not alter the functional response to ICA. isocyanic acid ETS transcription factor ERG Homo sapiens
6 Together these findings suggest that ICA binds to the same site in EAG and ERG channels to elicit opposite functional effects. isocyanic acid ETS transcription factor ERG Homo sapiens