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Article
Open AccessCloxyquin activates hTRESK by allosteric modulation of the selectivity filter
The TWIK-related spinal cord K+ channel (TRESK, K2P18.1) is a K2P channel contributing to the maintenance of membrane potentials in various cells. Recently, physiological TRESK function was identified as a key pl...
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Article
Open AccessEnhanced firing of locus coeruleus neurons and SK channel dysfunction are conserved in distinct models of prodromal Parkinson’s disease
Parkinson’s disease (PD) is clinically defined by the presence of the cardinal motor symptoms, which are associated with a loss of dopaminergic nigrostriatal neurons in the substantia nigra pars compacta (SNpc...
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Article
A lower X-gate in TASK channels traps inhibitors within the vestibule
TWIK-related acid-sensitive potassium (TASK) channels—members of the two pore domain potassium (K2P) channel family—are found in neurons1, cardiomyocytes2–4 and vascular smooth muscle cells5, where they are invol...
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Article
Open AccessFunctional mutagenesis screens reveal the ‘cap structure’ formation in disulfide-bridge free TASK channels
Two-pore-domain potassium (K2P) channels have a large extracellular cap structure formed by two M1-P1 linkers, containing a cysteine for dimerization. However, this cysteine is not present in the TASK-1/3/5 subfa...
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Article
The role of acid-sensitive two-pore domain potassium channels in cardiac electrophysiology: focus on arrhythmias
The current kinetics of two-pore domain potassium (K2P) channels resemble those of the steady-state K+ currents being active during the plateau phase of cardiac action potentials. Recent studies support that K2P ...
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Article
Kv1.5 blockers preferentially inhibit TASK-1 channels: TASK-1 as a target against atrial fibrillation and obstructive sleep apnea?
Atrial fibrillation and obstructive sleep apnea are responsible for significant morbidity and mortality in the industrialized world. There is a high medical need for novel drugs against both diseases, and here...
