<i>KCNQ2</i> Variants in Neonatal Epilepsy: Clinical Characteristics and Neurodevelopmental Outcomes in 30 Patients. [PDF]
Li Y, Li J, Li L, Zhang H, Sun X.
europepmc +1 more source
Voltage-gated potassium channels as important modulators of glucose-stimulated insulin secretion in pancreatic β-cells: insights from rodent and human studies. [PDF]
Xing JJ, Chen C.
europepmc +1 more source
SphereChip attaches spheroids and organoids to planar multielectrode arrays with microfluidics.
Hoebart C +4 more
europepmc +1 more source
Pharmacological Targeting of Neuronal Kv7.2/3 Channels: A Focus on Chemotypes and Receptor Sites
Background: The Kv7 (KCNQ) subfamily of voltage-gated potassium channels consists of 5 members (Kv7.1-5) each showing characteristic tissue distribution and physiological roles. Given their functional heterogeneity, Kv7 channels represent important pharmacological targets for the development of new drugs for neuronal, cardiovascular and metabolic ...
Francesco Miceli +2 more
exaly +6 more sources
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Cooperativity between calmodulin-binding sites in Kv7.2 channels
Journal of Cell Science, 2013Summary Among the multiple roles assigned to calmodulin (CaM), controlling the surface expression of Kv7.2 channels by binding to two discontinuous sites is a unique property of this Ca2+ binding protein. Mutations that interfere with CaM binding or the sequestering of CaM prevent this M-channel component from exiting the endoplasmic ...
Alaimo A. +6 more
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To identify pore domain ligands on Kv7.2 potassium ion channels, we compared wild-type (WT) and W236L mutant Kv7.2 channels in a series of assays with previously validated and novel agonist chemotypes. Positive controls were retigabine, flupirtine, and RL-81; i.e.
Ciria C, Hernandez +10 more
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Amitriptyline Is a Potent Blocker of Human Kv1.1 and Kv7.2/7.3 Channels
Anesthesia & Analgesia, 2007Kv1.1 and Kv7.2/7.3 channels control excitability of neuronal cells. As hyperexcitability is a sign of neuropathic pain, epilepsy, and anxiety disorders, these channels may be important molecular targets of amitriptyline that cause pharmacological as well as toxicological effects by altering neuronal excitability.
Mark A, Punke, Patrick, Friederich
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Homomeric Kv7.2 current suppression is a common feature in
SummaryObjectiveTo gain insight into the mechanisms underlying KCNQ2 encephalopathy by examining the electrophysiologic properties of mutant Kv7.2 channels in different multimeric configurations.MethodsWe analyzed the genotype‐phenotype relationship in 4 patients with KCNQ2 encephalopathy and performed electrophysiologic analysis of M‐currents mediated
Carolina Gomis‐Pérez +8 more
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Discovery of a novel KV7.2/7.3 channels agonist for the treatment of neuropathic pain
European Journal of Medicinal ChemistryHere, we designed, synthesized and evaluated a series of compounds as KV7.2/7.3 channels (or KCNQ2/3) agonists. The new compounds were assayed in vitro for KCNQ2/3 and other receptors binding affinity. The desired compound 16 showed high activity for KCNQ2/3 (EC50 = 1.03 ± 0.07 μM) without acute liver injury compared to flupirtine.
Kun Qian +10 more
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Genetic features and pharmacological rescue of novel Kv7.2 variants in patients with epilepsy
Journal of Medical GeneticsBackground Increasing evidence indicates a robust correlation between epilepsy and variants of the Kv7.2 ( KCNQ2 ) channel, which is critically involved in directing M-currents and regulating neuronal excitability within the nervous system.
Yue Song +16 more
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