Neuronal and Cardiovascular Potassium Channels as Therapeutic Drug Targets: Promise and Pitfalls

Potassium (K+) channels, with their diversity, often tissue-defined distribution, and critical role in controlling cellular excitability, have long held promise of being important drug targets for the treatment of dysrhythmias in the heart and abnormal neuronal activity within the brain. With the ex...

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Veröffentlicht in:Journal of Biomolecular Screening 2015-10, Vol.20 (9), p.1055-1073
Hauptverfasser: Humphries, Edward S. A., Dart, Caroline
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creator Humphries, Edward S. A.
Dart, Caroline
description Potassium (K+) channels, with their diversity, often tissue-defined distribution, and critical role in controlling cellular excitability, have long held promise of being important drug targets for the treatment of dysrhythmias in the heart and abnormal neuronal activity within the brain. With the exception of drugs that target one particular class, ATP-sensitive K+ (KATP) channels, very few selective K+ channel activators or inhibitors are currently licensed for clinical use in cardiovascular and neurological disease. Here we review what a range of human genetic disorders have told us about the role of specific K+ channel subunits, explore the potential of activators and inhibitors of specific channel populations as a therapeutic strategy, and discuss possible reasons for the difficulty in designing clinically relevant K+ channel modulators.
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subjects Animals
Cardiovascular Agents - pharmacology
Cardiovascular Agents - therapeutic use
Cardiovascular Diseases - drug therapy
Cardiovascular Diseases - metabolism
Humans
Myocardium - metabolism
Nervous System Diseases - drug therapy
Nervous System Diseases - metabolism
Neurons - metabolism
Potassium Channel Blockers - pharmacology
Potassium Channel Blockers - therapeutic use
Potassium Channels - physiology
Review
title Neuronal and Cardiovascular Potassium Channels as Therapeutic Drug Targets: Promise and Pitfalls
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