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PD-118057 contacts the pore helix of hERG1 channels to attenuate inactivation and enhance K(+) conductance

Human ether-a-go-go-related gene 1 (hERG1) K(+) channels mediate repolarization of cardiac action potentials. Unintended block of hERG1 channels by some drugs can prolong the QT interval and induce arrhythmia. Recently, hERG1 channel agonists were discovered and, based on their mechanisms of action...

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Autori principali: Perry, Matthew, Sachse, Frank B., Abbruzzese, Jennifer, Sanguinetti, Michael C.
Natura: Artigo
Lingua:Inglês
Pubblicazione: National Academy of Sciences 2009
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Accesso online:https://ncbi.nlm.nih.gov/pmc/articles/PMC2785294/
https://ncbi.nlm.nih.gov/pubmed/19892732
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1073/pnas.0906597106
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