870 results match your criteria Channels[Journal]


Sphingosine Kinase 2 Inhibitor ABC294640 Suppresses Neuronal Excitability and Inhibits Multiple Endogenously and Exogenously Expressed Voltage-Gated Ion Channels in Cultured Cells.

Channels (Austin) 2020 Jul 2. Epub 2020 Jul 2.

Division of Molecular Medicine, Hefei National Laboratory for Physical Sciences at Microscale, CAS Key Laboratory of Innate Immunity and Chronic Disease, Neurodegenerative Disorder Research Center, School of Life Sciences, University of Science and Technology of China , Hefei, Anhui 230027, China.

Sphingolipidsregulatemultiplecellularprocesses, including proliferation,autophagy, andapoptosis.Sphingosinekinases,thekeyenzymesinthemetabolismofsphingolipids,areoverexpressedinmanycancers,makingthemimportanttargetsforthedevelopmentof antitumordrugs.ABC294640isaselectivesphingosinekinase2(SK2)inhibitorthatshowsgoodantitumoractivityinvitro. Read More

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http://dx.doi.org/10.1080/19336950.2020.1788364DOI Listing

The Slo3/Lrrc52 complex is sensitive to phosphoinositides.

Channels (Austin) 2020 Dec;14(1):1-3

Graduate School of Medicine, Osaka University , Suita, Japan.

The voltage-sensing phosphatase (VSP) is a unique protein that shows voltage-dependent phosphatase activity toward phosphoinositides. Recently, we reported that VSP is activated and generates polarized PtdIns(4,5)P distribution in sperm flagellum. Interestingly, such specialized PtdIns(4,5)P distribution appears to contribute to the activity of Slo3, a sperm-specific K channels. Read More

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http://dx.doi.org/10.1080/19336950.2020.1778393DOI Listing
December 2020

The effect of MD1 on potassium and L-type calcium current of cardiomyocytes from high-fat diet mice.

Channels (Austin) 2020 Jan;14(1):181-189

Department of Cardiology, Renmin Hospital of Wuhan University , Wuhan, Hubei, China.

Myeloid differentiation protein 1 (MD1) is exerted an anti-arrhythmic effect in obese mice. Therefore, we sought to clarify whether MD1 can alter the electrophysiological remodeling of cardiac myocytes from obese mice by regulating voltage-gated potassium current and calcium current. MD1 knock-out (KO) and wild type (WT) mice were given a high-fat diet (HFD) for 20 weeks, starting at the age of 6 weeks. Read More

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http://dx.doi.org/10.1080/19336950.2020.1772628DOI Listing
January 2020

A de novo CACNA1D missense mutation in a patient with congenital hyperinsulinism, primary hyperaldosteronism and hypotonia.

Channels (Austin) 2020 Dec;14(1):175-180

Pediatric Endocrinology Unit, Hospital Universitario la Fe, Valencia, Spain.

Congenital hyperinsulinemic hypoglycemia is the most frequent cause of persistent and recurrent hypoglycemia in the first years of life and in many patients rare genetic variants can be identified. Recently a case of congenital hyperinsulinemic hypoglycemia and a severe neurodevelopmental syndrome due to a mutation in the voltage-gated Cav1.3 Ca channel gene has been reported which required long-term treatment with diazoxide. Read More

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http://dx.doi.org/10.1080/19336950.2020.1761171DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC7219433PMC
December 2020

The CaMKII phosphorylation site Thr1604 in the Ca1.2 channel is involved in pathological myocardial hypertrophy in rats.

Channels (Austin) 2020 Dec;14(1):151-162

Department of Pharmaceutical Toxicology, School of Pharmacy, China Medical University, Shenyang, China.

Residue Thr1604 in the Ca1.2 channel is a Ca/calmodulin dependent protein kinase II (CaMKII) phosphorylation site, and its phosphorylation status maintains the basic activity of the channel. However, the role of Ca1. Read More

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http://dx.doi.org/10.1080/19336950.2020.1750189DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC7188351PMC
December 2020

The role of TRPV1 channels in atherosclerosis.

Channels (Austin) 2020 Dec;14(1):141-150

Zhejiang Provincial People's Hospital, Qingdao University, Hangzhou, China.

Transient receptor potential vanilloid subfamily member 1 (TRPV1) is a nonselective cation channel, that is mainly distributed in sensory nerve endings and can release a variety of neurotransmitters after activation. Early studies showed that it mainly conducts pain sensation, but research has demonstrated that it also plays an important role in cardiovascular diseases. Notably, in atherosclerosis, the activation of TRPV1 can regulate lipid metabolism, reduce foam cell formation, protect endothelial cells, inhibit smooth muscle cell proliferation and inhibit inflammation and oxidation. Read More

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http://dx.doi.org/10.1080/19336950.2020.1747803DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC7153790PMC
December 2020
2.410 Impact Factor

The mutation L69P in the PAS domain of the hERG potassium channel results in LQTS by trafficking deficiency.

Channels (Austin) 2020 Dec;14(1):163-174

Institute of Legal Medicine, University of Frankfurt, Frankfurt Am Main, Germany.

The congenital long QT syndrome (LQTS) is a cardiac disorder characterized by a prolonged QT interval on the electrocardiogram and an increased susceptibility to ventricular arrhythmias and sudden cardiac death. A frequent cause for LQTS is mutations in the gene (also known as the or ), which reduce or modulate the potassium current I and hence alter cardiac repolarization. In a patient with a clinically diagnosed LQTS, we identified the mutation L69P in the N-terminal PAS (Per-Arnt-Sim) domain of hERG. Read More

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http://dx.doi.org/10.1080/19336950.2020.1751522DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC7188350PMC
December 2020

Transcriptomic analysis of glycan-processing genes in the dorsal root ganglia of diabetic mice and functional characterization on Ca3.2 channels.

Channels (Austin) 2020 Dec;14(1):132-140

Institute of Organic Chemistry and Biochemistry, Czech Academy of Sciences, Prague, Czech Republic.

Ca3.2 T-type calcium channels play an essential role in the transmission of peripheral nociception in the dorsal root ganglia (DRG) and alteration of Ca3.2 expression is associated with the development of peripheral painful diabetic neuropathy (PDN). Read More

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http://dx.doi.org/10.1080/19336950.2020.1745406DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC7153791PMC
December 2020

The quest to identify the mechanism underlying adrenergic regulation of cardiac Ca channels.

Channels (Austin) 2020 Dec;14(1):123-131

Division of Cardiology, Department of Medicine, Columbia University, Vagelos College of Physicians and Surgeons, New York, USA.

Activation of protein kinase A by cyclic AMP results in a multi-fold upregulation of Ca1.2 currents in the heart, as originally reported in the 1970's and 1980's. Despite considerable interest and much investment, the molecular mechanisms responsible for this signature modulation remained stubbornly elusive for over 40 years. Read More

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http://dx.doi.org/10.1080/19336950.2020.1740502DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC7153787PMC
December 2020

The structure and function of TRIP8b, an auxiliary subunit of hyperpolarization-activated cyclic-nucleotide gated channels.

Channels (Austin) 2020 Dec;14(1):110-122

Department of Neurology, Vanderbilt University Medical Center, Nashville, TN, USA.

Hyperpolarization-activated cyclic nucleotide-gated (HCN) channels are expressed throughout the mammalian central nervous system (CNS). These channels have been implicated in a wide range of diseases, including Major Depressive Disorder and multiple subtypes of epilepsy. The diversity of functions that HCN channels perform is in part attributable to differences in their subcellular localization. Read More

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http://dx.doi.org/10.1080/19336950.2020.1740501DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC7153792PMC
December 2020

Mutations in calmodulin-binding domains of TRPV4/6 channels confer invasive properties to colon adenocarcinoma cells.

Channels (Austin) 2020 Dec;14(1):101-109

Laboratoire Physico Chimie Curie, Institut Curie, CNRS UMR168, PSL Research University, Paris, France.

Transient receptor potential (TRP) channels form a family of polymodal cation channels gated by thermal, mechanical, or chemical stimuli, with many of them involved in the control of proliferation, apoptosis, or cell cycle. From an evolutionary point of view, TRP family is characterized by high conservation of duplicated genes originating from whole-genome duplication at the onset of vertebrates. The conservation of such "ohnolog" genes is theoretically linked to an increased probability of generating phenotypes deleterious for the organism upon gene mutation. Read More

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http://dx.doi.org/10.1080/19336950.2020.1740506DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC7153789PMC
December 2020

T-type channels in neuropathic pain - Villain or victim?

Authors:
Norbert Weiss

Channels (Austin) 2020 Dec;14(1):98-100

Institute of Organic Chemistry and Biochemistry, Czech Academy of Sciences, Prague, Czech Republic.

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http://dx.doi.org/10.1080/19336950.2020.1740487DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC7153802PMC
December 2020

Obtaining transition rates from single-channel data without initial parameter seeding.

Channels (Austin) 2020 Dec;14(1):87-97

Aarhus Institute of Advanced Studies, Aarhus University, Aarhus, Denmark.

Ion-channels are membrane proteins that can adopt several distinct structural conformations. Some of the conformations are open and allow the passage of ions through the membrane; others are closed and hinder ion flow. Patch-clamp recordings of single ion-channels show if a channel is open or closed, but does not immediately reveal the underlying mechanism, which typically includes several open and closed conformations. Read More

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http://dx.doi.org/10.1080/19336950.2020.1732004DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC7153788PMC
December 2020

Regulation of the cold-sensing TRPM8 channels by phosphoinositides and G-coupled receptors.

Channels (Austin) 2020 Dec;14(1):79-86

Department of Pharmacology, Physiology and Neuroscience, Rutgers New Jersey Medical School, Newark, NJ, USA.

The Transient Receptor Potential Melastatin 8 (TRPM8) ion channel is an important sensor of environmental cold temperatures. Cold- and menthol-induced activation of this channel requires the presence of the membrane phospholipid phosphatidylinositol 4,5-bisphosphate [PI(4,5)P]. This review discusses recent findings on the role of PI(4,5)P and G-proteins in the modulation of TRPM8 upon receptor activation. Read More

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http://dx.doi.org/10.1080/19336950.2020.1734266DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC7153793PMC
December 2020

PAC proton-activated chloride channel contributes to acid-induced cell death in primary rat cortical neurons.

Channels (Austin) 2020 Dec;14(1):53-58

Department of Physiology, Johns Hopkins University School of Medicine, Baltimore, MD, USA.

Severe local acidosis causes tissue damage and pain, and is associated with many diseases, including cerebral and cardiac ischemia, cancer, infection, and inflammation. However, the molecular mechanisms of the cellular response to extracellular acidic environment are not fully understood. We recently identified a novel and evolutionarily conserved membrane protein, PAC (also known as PACC1 or TMEM206), encoding the proton-activated chloride (Cl) channel, whose activity is widely observed in human cell lines. Read More

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http://dx.doi.org/10.1080/19336950.2020.1730019DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC7153786PMC
December 2020

Activating Sirt1 by resveratrol suppresses Nav1.7 expression in DRG through miR-182 and alleviates neuropathic pain in rats.

Channels (Austin) 2020 Dec;14(1):69-78

Department of Anesthesiology, First Hospital of Qinhuangdao, Qinhuangdao, Hebei, China.

Neuropathic pain is clinically unsatisfactorily treated because of unclear mechanisms. The present study aims to explore the concrete mechanisms underlying the alleviation of resveratrol-activated silent information regulator 1 (Sirt1) to chronic constriction injury (CCI)-induced neuropathic pain. CCI surgery was conducted to the unilateral sciatic nerve of male Sprague-Dawley rats to induce neuropathic pain experimentally. Read More

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http://dx.doi.org/10.1080/19336950.2020.1732003DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC7039643PMC
December 2020

TRPV1 inhibits smooth muscle cell phenotype switching in a mouse model of abdominal aortic aneurysm.

Channels (Austin) 2020 Dec;14(1):59-68

Department of Cardiology, Shengjing Hospital of China Medical University, Shenyang, China.

The natural outcome of abdominal aortic aneurysm (AAA) is that of slow progression and ultimate rupture, then a life-threatening hemorrhage consequently. Ruptured AAA is a dramatic catastrophe and constitutes one of the leading causes of acute death in elderly men. However, the mechanism of AAA is still unclear. Read More

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http://dx.doi.org/10.1080/19336950.2020.1730020DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC7039625PMC
December 2020

Flow fluorometry quantification of anion channel VRAC subunit LRRC8A at the membrane of living U937 cells.

Channels (Austin) 2020 Dec;14(1):45-52

Institute of Cytology, Russian Academy of Sciences, St-Petersburg, Russia.

Assessing the expression of channels on the cell membrane is a necessary step in studying the functioning of ion channels in living cells. We explore, first, if endogenous VRAC can be assayed using flow cytometry and a commercially available antibody against an extracellular loop of the LRRC8A, also known as SWELL1, subunit of the VRAC channel. The second goal is to determine if an increase in the number of VRAC channels at the cell membrane is responsible for an increase in chloride permeability of the membrane in two well-known cases: during staurosporine (STS)-induced apoptosis and after water balance disturbance caused by hypotonic medium. Read More

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http://dx.doi.org/10.1080/19336950.2020.1730535DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC7039630PMC
December 2020

TRAM1 protein may support ER protein import by modulating the phospholipid bilayer near the lateral gate of the Sec61-channel.

Channels (Austin) 2020 Dec;14(1):28-44

Medical Biochemistry and Molecular Biology, Saarland University, Homburg, Germany.

In mammalian cells, one-third of all polypeptides is transported into or through the ER-membrane via the Sec61-channel. While the Sec61-complex facilitates the transport of all polypeptides with amino-terminal signal peptides (SP) or SP-equivalent transmembrane helices (TMH), the translocating chain-associated membrane protein (now termed TRAM1) was proposed to support transport of a subset of precursors. To identify possible determinants of TRAM1 substrate specificity, we systematically identified TRAM1-dependent precursors by analyzing cellular protein abundance changes upon TRAM1 depletion in HeLa cells using quantitative label-free proteomics. Read More

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http://dx.doi.org/10.1080/19336950.2020.1724759DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC7039644PMC
December 2020

Bibliometric analysis of potassium channel research.

Channels (Austin) 2020 Dec;14(1):18-27

Guanganmen Hospital, China Academy of Chinese Medical Sciences, Beijing, China.

Objective: To explore the research status, hotspots, and trends in research on potassium channel.

Methods: The Web of Science core collection database was used as the data source and the visual analysis software Citespace5.4 R3 was used to visualize the studies of potassium channel in the past 10 years. Read More

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http://dx.doi.org/10.1080/19336950.2019.1705055DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC7039634PMC
December 2020

Trafficking mechanisms underlying Na channel subcellular localization in neurons.

Channels (Austin) 2020 Dec;14(1):1-17

Molecular, Cellular and Integrative Neurosciences Graduate Program, Colorado State University, Fort Collins, CO, USA.

Voltage gated sodium channels (Na) play a crucial role in action potential initiation and propagation. Although the discovery of Na channels dates back more than 65 years, and great advances in understanding their localization, biophysical properties, and links to disease have been made, there are still many questions to be answered regarding the cellular and molecular mechanisms involved in Na channel trafficking, localization and regulation. This review summarizes the different trafficking mechanisms underlying the polarized Na channel localization in neurons, with an emphasis on the axon initial segment (AIS), as well as discussing the latest advances regarding how neurons regulate their excitability by modifying AIS length and location. Read More

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http://dx.doi.org/10.1080/19336950.2019.1700082DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC7039628PMC
December 2020

Elementary calcium signaling in arterial smooth muscle.

Channels (Austin) 2019 12;13(1):505-519

Charité - Universitätsmedizin Berlin, Experimental and Clinical Research Center (ECRC), a joint cooperation between the Charité Medical Faculty and the Max Delbrück Center for Molecular Medicine (MDC), Berlin, Germany.

Vascular smooth muscle cells (VSMCs) of small peripheral arteries contribute to blood pressure control by adapting their contractile state. These adaptations depend on the VSMC cytosolic Ca concentration, regulated by complex local elementary Ca signaling pathways. Ca sparks represent local, transient, rapid calcium release events from a cluster of ryanodine receptors (RyRs) in the sarcoplasmic reticulum. Read More

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http://dx.doi.org/10.1080/19336950.2019.1688910DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6930021PMC
December 2019

PI3Kα in cardioprotection: Cytoskeleton, late Na current, and mechanism of arrhythmias.

Channels (Austin) 2019 12;13(1):520-532

Department of Medicine, University of Alberta, Edmonton, Canada.

PI 3-kinase α (PI3Kα) is a lipid kinase that converts phosphatidylinositol-4,5-bisphosphate (PIP2) to phosphatidylinositol-3,4,5-triphosphate (PIP3). PI3Kα regulates a variety of cellular processes such as nutrient sensing, cell cycle, migration, and others. Heightened activity of PI3Kα in many types of cancer made it a prime oncology drug target, but also raises concerns of possible adverse effects on the heart. Read More

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http://dx.doi.org/10.1080/19336950.2019.1697127DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6930018PMC
December 2019
2.410 Impact Factor

Evaluation of edonerpic maleate as a CRMP2 inhibitor for pain relief.

Channels (Austin) 2019 12;13(1):498-504

Department of Pharmacology, College of Medicine, The University of Arizona Health Sciences, Tucson, AZ, USA.

We have previously reported that the microtubule-associated collapsin response mediator protein 2 (CRMP2) is necessary for the expression of chronic pain. CRMP2 achieves this control of nociceptive signaling by virtue of its ability to regulate voltage-gated calcium and sodium channels. To date, however, no drugs exist that target CRMP2. Read More

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http://dx.doi.org/10.1080/19336950.2019.1684608DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6833970PMC
December 2019
2.410 Impact Factor

A conserved arginine/lysine-based motif promotes ER export of KCNE1 and KCNE2 to regulate KCNQ1 channel activity.

Channels (Austin) 2019 12;13(1):483-497

Key Laboratory of Molecular Biophysics of the Ministry of Education, College of Life Science and Technology, Huazhong University of Science and Technology, Wuhan, Hubei, China.

KCNE β-subunits play critical roles in modulating cardiac voltage-gated potassium channels. Among them, KCNE1 associates with KCNQ1 channel to confer a slow-activated current, while KCNE2 functions as a dominant negative modulator to suppress the current amplitude of KCNQ1. Any anomaly in these channels will lead to serious myocardial diseases, such as the long QT syndrome (LQTS). Read More

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http://dx.doi.org/10.1080/19336950.2019.1685626DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6833972PMC
December 2019
2.410 Impact Factor

Ion channels as potential redox sensors in lysosomes.

Channels (Austin) 2019 12;13(1):477-482

Collaborative Innovation Center of Yangtze River Delta Region Green Pharmaceuticals, College of Pharmaceutical Sciences, Zhejiang University of Technology, Hangzhou, China.

Lysosomes are central organelles that recycle materials and energy to maintain intracellular homeostasis. Lysosomes are capable of sensing environmental cues such as nutrition to regulate their function accordingly. Whether lysosomes can sense redox signaling, however, was unclear. Read More

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http://dx.doi.org/10.1080/19336950.2019.1684428DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6833971PMC
December 2019

Voltage vs. Ligand I: Structural basis of the intrinsic flexibility of S3 segment and its significance in ion channel activation.

Channels (Austin) 2019 12;13(1):455-476

Facultad de Medicina, Departamento de Bioquímica, Universidad Nacional Autónoma de México, 04510 Mexico City, Mexico. Current address: Department of Biochemistry, University of Bayreuth , Bayreuth , Germany.

We systematically predict the internal flexibility of the S3 segment, one of the most mobile elements in the voltage-sensor domain. By analyzing the primary amino acid sequences of V-sensor containing proteins, including Hv1, TPC channels and the voltage-sensing phosphatases, we established correlations between the local flexibility and modes of activation for different members of the VGIC superfamily. Taking advantage of the structural information available, we also assessed structural aspects to understand the role played by the flexibility of S3 during the gating of the pore. Read More

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http://dx.doi.org/10.1080/19336950.2019.1674242DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6833973PMC
December 2019
2.410 Impact Factor

Anterograde trafficking signals in GABA subunits are required for functional expression.

Channels (Austin) 2019 12;13(1):440-454

Neuroscience & Experimental Therapeutics, Albany Medical College , Albany , NY , USA.

Pentameric GABA receptors are composed from 19 possible subunits. The GABA β subunit is unique because the β and β subunits can assemble and traffic to the cell surface as homomers, whereas most of the other subunits, including β, are heteromers. The intracellular domain (ICD) of the GABA subunits has been implicated in targeting and clustering GABA receptors at the plasma membrane. Read More

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http://dx.doi.org/10.1080/19336950.2019.1676368DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6802930PMC
December 2019

The influence of membrane bilayer thickness on KcsA channel activity.

Channels (Austin) 2019 12;13(1):424-439

From the Département de pharmacologie et physiologie, Faculté de médecine, Université de Montréal , Montréal , Canada.

Atomic resolution structures have provided significant insight into the gating and permeation mechanisms of various ion channels, including potassium channels. However, ion channels may also be regulated by numerous factors, including the physiochemical properties of the membrane in which they are embedded. For example, the matching of the bilayer's hydrophobic region to the hydrophobic external surface of the ion channel is thought to minimize the energetic penalty needed to solvate hydrophobic residues or exposed lipid tails. Read More

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http://dx.doi.org/10.1080/19336950.2019.1676367DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6802934PMC
December 2019

Heteromeric TRPV4/TRPC1 channels mediate calcium-sensing receptor-induced relaxations and nitric oxide production in mesenteric arteries: comparative study using wild-type and TRPC1 mice.

Channels (Austin) 2019 12 11;13(1):410-423. Epub 2019 Oct 11.

Vascular Biology Research Centre, Molecular & Clinical Sciences Research Institute, St. George's, University of London, London, UK.

We have previously provided pharmacological evidence that stimulation of calcium-sensing receptors (CaSR) induces endothelium-dependent relaxations of rabbit mesenteric arteries through activation of heteromeric TRPV4/TRPC1 channels and nitric oxide (NO) production. The present study further investigates the role of heteromeric TRPV4/TRPC1 channels in these CaSR-induced vascular responses by comparing responses in mesenteric arteries from wild-type (WT) and TRPC1 mice. In WT mice, stimulation of CaSR induced endothelium-dependent relaxations of pre-contracted tone and NO generation in endothelial cells (ECs), which were inhibited by the TRPV4 channel blocker RN1734 and the TRPC1 blocking antibody T1E3. Read More

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http://dx.doi.org/10.1080/19336950.2019.1673131DOI Listing
December 2019

Voltage vs. Ligand II: Structural insights of the intrinsic flexibility in cyclic nucleotide-gated channels.

Channels (Austin) 2019 12;13(1):382-399

Departamento de Química ICET, Universidad Autónoma de Guadalajara , Zapopan , Jalisco , Mexico.

In the preceding article, we present a flexibility analysis of the voltage-gated ion channel (VGIC) superfamily. In this study, we describe in detail the flexibility profile of the voltage-sensor domain (VSD) and the pore domain (PD) concerning the evolution of 6TM ion channels. In particular, we highlight the role of flexibility in the emergence of CNG channels and describe a significant level of sequence similarity between the archetypical VSD and the TolQ proteins. Read More

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http://dx.doi.org/10.1080/19336950.2019.1666456DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6768053PMC
December 2019
2.410 Impact Factor

Acid-sensing ion channels mediate the degeneration of intervertebral disc via various pathways-A systematic review.

Channels (Austin) 2019 12;13(1):367-373

Department of Orthopedic Surgery, West China Hospital, Sichuan University , Chengdu , Sichuan Province , China.

To elucidate the pathological significance of acid-sensing ion channels (ASICs) in intervertebral disc degeneration (IVDD), the database of Medline, Web of Science, and EmBase were carefully screened. Search terms used in each database varied slightly to optimize results. Data relating to the correlation between ASICs and IVDD was systematically collected and integrated into the review. Read More

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http://dx.doi.org/10.1080/19336950.2019.1664038DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6768050PMC
December 2019
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TRPML1 and RAS-driven cancers - exploring a link with great therapeutic potential.

Channels (Austin) 2019 12;13(1):374-381

Department of Integrative Biology and Pharmacology, McGovern Medical School at the University of Texas Health Sciences Center (UTHealth) , Houston , TX , USA.

Activating mutations in the family of proto-oncogenes represent some of the leading causes of cancer. Unmitigated proliferation of cells harboring oncogenic mutations is accompanied by a massive increase in cellular bioenergetic demands, which offers unique opportunities for therapeutic intervention. To withstand the steep requirements for metabolic intermediates, RAS-driven cancer cells enhance endolysosome and autophagosome biogenesis. Read More

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http://dx.doi.org/10.1080/19336950.2019.1666457DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6768051PMC
December 2019

Voltage gated sodium channels in cancer and their potential mechanisms of action.

Channels (Austin) 2019 12;13(1):400-409

Department of Biomedical Physiology and Kinesiology, Simon Fraser University , Burnaby , BC , Canada.

Voltage gated sodium channels (VGSC) are implicated in cancer cell invasion and metastasis. However, the mechanism by which VGSC increase cell invasiveness and probability of metastasis is still unknown. In this review we outline lesser known functions of VGSC outside of action potential propagation, and the current understanding of the effects of VGSC in cancer. Read More

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http://dx.doi.org/10.1080/19336950.2019.1666455DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6768049PMC
December 2019

Myrcene and terpene regulation of TRPV1.

Channels (Austin) 2019 12;13(1):344-366

Laboratory of Immunology and Signal Transduction, Chaminade University , Honolulu , HI , USA.

Nociceptive Transient Receptor Potential channels such as TRPV1 are targets for treating pain. Both antagonism and agonism of TRP channels can promote analgesia, through inactivation and chronic desensitization. Since plant-derived mixtures of cannabinoids and the component myrcene have been suggested as pain therapeutics, we screened terpenes found in for activity at TRPV1. Read More

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http://dx.doi.org/10.1080/19336950.2019.1654347DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6768052PMC
December 2019

Role of the voltage sensor module in Na domain IV on fast inactivation in sodium channelopathies: The implication of closed-state inactivation.

Channels (Austin) 2019 12;13(1):331-343

a Department of Cardiovascular Medicine, Gunma University Graduate School of Medicine , Maebashi , Gunma , Japan.

The segment 4 (S4) voltage sensor in voltage-gated sodium channels (Nas) have domain-specific functions, and the S4 segment in domain DIV (DIVS4) plays a key role in the activation and fast inactivation processes through the coupling of arginine residues in DIVS4 with residues of putative gating charge transfer center (pGCTC) in DIVS1-3. In addition, the first four arginine residues (R1-R4) in Na DIVS4 have position-specific functions in the fast inactivation process, and mutations in these residues are associated with diverse phenotypes of Na-related diseases (sodium channelopathies). R1 and R2 mutations commonly display a delayed fast inactivation, causing a gain-of-function, whereas R3 and R4 mutations commonly display a delayed recovery from inactivation and profound use-dependent current attenuation, causing a severe loss-of-function. Read More

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http://dx.doi.org/10.1080/19336950.2019.1649521DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6713248PMC
December 2019

Silencing of KCNA1 suppresses the cervical cancer development via mitochondria damage.

Channels (Austin) 2019 12;13(1):321-330

a Department of Obstetrics and Gynecology, Shandong Provincial Hospital Affiliated to Shandong University , Jinan , Shandong , China.

Voltage-gated potassium channel subfamily A member 1 (KCNA1/Kv1.1) is an important component of type A potassium channels, which has been found to be involved in various tumors. This study aimed to identify the role of KCNA1 in cervical cancer and explore the related mechanism. Read More

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http://dx.doi.org/10.1080/19336950.2019.1648627DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6682364PMC
December 2019

No transcriptional evidence for active Na channels in two classes of cancer cell.

Channels (Austin) 2019 12;13(1):311-320

a Wolfson Centre for Age-Related Diseases, King's College London , London , UK.

Voltage-gated sodium channel (Na) expression in non-excitable cells has raised questions regarding their non-canonical roles. Interestingly, a growing body of evidence also points towards the prevalence of aberrant Na expression in malignant tumors, potentially opening a new therapeutic window. In this study, the transcriptional consequences of channel inhibition were investigated in non-small cell lung carcinoma H460 and neuroblastoma SH-SYSY cell lines, that both express Na1. Read More

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https://www.tandfonline.com/doi/full/10.1080/19336950.2019.1
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http://dx.doi.org/10.1080/19336950.2019.1644858DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6682260PMC
December 2019
2 Reads

pHluorin-tagged TRPV1 shines light on capsaicin tachyphylaxis.

Channels (Austin) 2019 12;13(1):308-310

a Department of Physiology and Pharmacology , Inflammation Research Network-Snyder Institute for Chronic Diseases and Alberta Children's Hospital Research Institute, Cumming School of Medicine, University of Calgary , Calgary , Alberta , Canada.

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http://dx.doi.org/10.1080/19336950.2019.1638695DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6629181PMC
December 2019
3 Reads

mutation G615E results in Na1.5 voltage-gated sodium channels with normal voltage-dependent function yet loss of mechanosensitivity.

Channels (Austin) 2019 12;13(1):287-298

a Enteric NeuroScience Program, Division of Gastroenterology and Hepatology, Mayo Clinic , Rochester , MN , USA.

is expressed in cardiomyocytes and gastrointestinal (GI) smooth muscle cells (SMCs) as the voltage-gated mechanosensitive sodium channel Na1.5. The influx of Na through Na1. Read More

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http://dx.doi.org/10.1080/19336950.2019.1632670DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6629189PMC
December 2019
2 Reads

Kv1.1 channel subunits in the control of neurocardiac function.

Authors:
Edward Glasscock

Channels (Austin) 2019 12;13(1):299-307

a Department of Biological Sciences , Southern Methodist University , Dallas , TX , USA.

Voltage-gated Kv1.1 potassium channel α-subunits are broadly expressed in the nervous system where they act as critical regulators of neuronal excitability. Mutations in the gene, which encodes Kv1. Read More

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http://dx.doi.org/10.1080/19336950.2019.1635864DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6602576PMC
December 2019
1 Read

exposure to venom and constituents activates discrete ionotropic pathways in mast cells.

Channels (Austin) 2019 12;13(1):264-286

a Laboratory of Immunology and Signal Transduction, Division of Natural Sciences and Mathematics , Chaminade University , Honolulu , Hawai'I , USA.

Calcium entry is central to the functional processes in mast cells and basophils that contribute to the induction and maintenance of inflammatory responses. Mast cells and basophils express an array of calcium channels, which mediate responses to diverse stimuli triggered by small bioactive molecules, physicochemical stimuli and immunological inputs including antigens and direct immune cell interactions. These cells are also highly responsive to certain venoms (such as envenomations), which cause histamine secretion, cytokine release and an array of pro-inflammatory functional responses. Read More

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http://dx.doi.org/10.1080/19336950.2019.1629225DOI Listing
December 2019
1 Read

The role of oligodendrocyte gap junctions in neuroinflammation.

Channels (Austin) 2019 12;13(1):247-263

a Neuroscience Laboratory, The Cyprus Institute of Neurology and Genetics and Cyprus School of Molecular Medicine , Nicosia , Cyprus.

Gap junctions (GJs) provide channels for direct cell-to-cell connectivity serving the homeostasis in several organs of vertebrates including the central (CNS) and peripheral (PNS) nervous systems. GJs are composed of connexins (Cx), which show a highly distinct cellular and subcellular expression pattern. Oligodendrocytes, the myelinating cells of the CNS, are characterized by extensive GJ connectivity with each other as well as with astrocytes. Read More

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http://dx.doi.org/10.1080/19336950.2019.1631107DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6602578PMC
December 2019
2 Reads

Airway regeneration using iPS cell-derived airway epithelial cells with Cl channel function.

Channels (Austin) 2019 12;13(1):227-234

a Department of Cellular and Integrative Physiology, School of Medicine , Fukushima Medical University , Fukushima , Japan.

induced pluripotent stem (iPS) cells can be differentiated into various cell types, including airway epithelial cells, since they have the capacity for self-renewal and pluripotency. Thus, airway epithelial cells generated from iPS cells are expected to be potent candidates for use in airway regeneration and the treatment of airway diseases such as cystic fibrosis (CF). Recently, it was reported that iPS cells can be differentiated into airway epithelial cells according to the airway developmental process. Read More

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http://dx.doi.org/10.1080/19336950.2019.1628550DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6602574PMC
December 2019
2 Reads

The potential role of TRPV1 in pulmonary hypertension: Angel or demon?

Channels (Austin) 2019 12;13(1):235-246

a The Second Clinical Medical College, Zhejiang Chinese Medical University , Hangzhou , China.

Pulmonary hypertension (PH) is a pathological state defined by increased pulmonary artery pressure, the pathogenesis of which is related to genetic mutations, intracellular calcium ([Ca]), inflammation and proliferation. Transient receptor potential vanilloid subfamily member 1 (TRPV1) is a nonselective cation channel expressed in neural and nonneural cells, including pulmonary vessels and nerves. As a calcium channel, TRPV1 can make vessels contracted, and promote smooth muscle cells proliferation through calcium-dependent transcription factors. Read More

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http://dx.doi.org/10.1080/19336950.2019.1631106DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6602577PMC
December 2019
3 Reads
2.410 Impact Factor

TRP ion channels: Proteins with conformational flexibility.

Channels (Austin) 2019 12;13(1):207-226

a Departamento de Neurociencia Cognitiva, División Neurociencias , Instituto de Fisiología Celular, Universidad Nacional Autónoma de México , Mexico , Mexico.

Ion channels display conformational changes in response to binding of their agonists and antagonists. The study of the relationships between the structure and the function of these proteins has witnessed considerable advances in the last two decades using a combination of techniques, which include electrophysiology, optical approaches (i.e. Read More

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http://dx.doi.org/10.1080/19336950.2019.1626793DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6602575PMC
December 2019
7 Reads
2.410 Impact Factor

Mechano-electrical transduction in trabecular meshwork involves parallel activation of TRPV4 and TREK-1 channels.

Channels (Austin) 2019 12;13(1):168-171

a Department of Ophthalmology and Visual Sciences , University of Utah , Salt lake City , UT , USA.

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http://dx.doi.org/10.1080/19336950.2019.1618149DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6557601PMC
December 2019
5 Reads
2.410 Impact Factor

Stimulation of TRPA1 attenuates ischemia-induced cardiomyocyte cell death through an eNOS-mediated mechanism.

Channels (Austin) 2019 12;13(1):192-206

b Department of Biomedical Sciences , Kent State University , Kent , OH , USA.

The functional expression of transient receptor potential cation channel of the ankyrin-1 subtype (TRPA1) has recently been identified in adult mouse cardiac tissue where stimulation of this ion channel leads to increases in adult mouse ventricular cardiomyocyte (CM) contractile function via a Ca-Calmodulin-dependent kinase (CaMKII) pathway. However, the extent to which TRPA1 induces nitric oxide (NO) production in CMs, and whether this signaling cascade mediates physiological or pathophysiological events in cardiac tissue remains elusive. Freshly isolated CMs from wild-type (WT) or TRPA1 knockout (TRPA1) mouse hearts were treated with AITC (100 µM) and prepared for immunoblot, NO detection or ischemia protocols. Read More

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http://dx.doi.org/10.1080/19336950.2019.1623591DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6557600PMC
December 2019
3 Reads
2.410 Impact Factor

Diverse TRPV1 responses to cannabinoids.

Channels (Austin) 2019 12;13(1):172-191

a Laboratory of Immunology and Signal Transduction , Chaminade University , Honolulu , HI , USA.

Cannabinoid compounds are potential analgesics. Users of medicinal report efficacy for pain control, clinical studies show that cannabis can be effective and opioid sparing in chronic pain, and some constituent cannabinoids have been shown to target nociceptive ion channels. Here, we explore and compare a suite of cannabinoids for their impact upon the physiology of TRPV1. Read More

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http://dx.doi.org/10.1080/19336950.2019.1619436DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6557596PMC
December 2019
2 Reads

Cannabinoid interactions with ion channels and receptors.

Channels (Austin) 2019 12;13(1):162-167

a Department of Biomedical Physiology and Kinesiology , Simon Fraser University , Burnaby , BC , Canada.

Cannabidiol (CBD), the non-psychoactive component of Cannabis sativa, acts on a diverse selection of membrane proteins with promising therapeutic potential in epilepsy and chronic pain. One such protein is the voltage-gated sodium channel (Na). CBD shows a lack of specificity for sodium channels; however, the method of interaction is still unknown. Read More

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http://dx.doi.org/10.1080/19336950.2019.1615824DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6527074PMC
December 2019