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chloride channel activators

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https://www.readbyqxmd.com/read/28334417/pharmacovigilance-database-search-discloses-clc-k-channels-as-a-novel-target-of-the-at1-receptor-blockers-valsartan-and-olmesartan
#1
Paola Imbrici, Domenico Tricarico, Giuseppe Felice Mangiatordi, Orazio Nicolotti, Marcello Diego Lograno, Diana Conte, Antonella Liantonio
BACKGROUND AND PURPOSE: Human ClC-K chloride channels are highly attractive targets for drug discovery for their physiological role and association with genetic disorders. These channels are pivotal in the kidney as they control chloride reabsorption and water diuresis. In addition, loss-of-function mutations of CLCKNB and BSND genes cause Bartter's syndrome (BS), whereas CLCNKA and CLCKNB gain-of-function polymorphisms predispose to a rare form of salt sensitive hypertension. Both disorders lack a personalized therapy that is in most cases only symptomatic...
March 23, 2017: British Journal of Pharmacology
https://www.readbyqxmd.com/read/28300155/volume-sensitive-outwardly-rectifying-chloride-channel-blockers-protect-against-high-glucose-induced-apoptosis-of-cardiomyocytes-via-autophagy-activation
#2
Lin Wang, Mingzhi Shen, Xiaowang Guo, Bo Wang, Yuesheng Xia, Ning Wang, Qian Zhang, Lintao Jia, Xiaoming Wang
Hyperglycemia is a well-characterized contributing factor for cardiac dysfunction and heart failure among diabetic patients. Apoptosis of cardiomyocytes plays a major role during the onset and pathogenesis of diabetic cardiomyopathy (DCM). Nonetheless, the molecular machinery underlying hyperglycemia-induced cardiac damage and cell death remains elusive. In the present study, we found that chloride channel blockers, 4,4'-diisothiocya-natostilbene-2,2'- disulfonic acid (DIDS) and 4-(2-butyl-6,7-dichlor-2-cyclopentyl-indan-1-on-5-yl) oxybutyric acid (DCPIB), inhibited high glucose-activated volume-sensitive outwardly rectifying (VSOR) Cl(-) channel and improved the viability of cardiomyocytes...
March 16, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28299581/expression-of-anoctamin-1-is-associated-with-advanced-tumor-stage-in-patients-with-non-small-cell-lung-cancer-and-predicts-recurrence-after-surgery
#3
Y He, H Li, Y Chen, P Li, L Gao, Y Zheng, Y Sun, J Chen, X Qian
PURPOSE: Anoctamin 1 (ANO1), a recently identified calcium-activated chloride channel, has been found to have a critical role in tumorigenesis and tumor progression in several types of cancer. However, its role in non-small cell lung cancer (NSCLC) remains to be elucidated. In this study, we evaluated the utility of ANO1 as a prognostic marker. PATIENTS AND METHODS: ANO1 expression was detected in tumor tissues and paraneoplastic tissues of I-IV stage NSCLC patients who received surgical treatment by using immunohistochemical and quantitative RT-PCR analyses...
March 15, 2017: Clinical & Translational Oncology
https://www.readbyqxmd.com/read/28293832/the-mechanistic-role-of-the-calcium-activated-chloride-channel-ano1-in-tumor-growth-and-signaling
#4
Anke Bill, Larry Alex Gaither
Multiple studies have described the high expression and amplification of Anoctamin 1 (ANO1) in various cancers, including, but not limited to breast cancer, head and neck cancer, gastrointestinal stromal tumors and glioblastoma. ANO1 has been demonstrated to be critical for tumor growth in breast and head and neck cancers through its regulation of EGFR signaling and pathway modulators like MAPK and protein kinase B. However, the discovery of ANO1 as a calcium activated chloride channel came as a surprise to the field and has given rise to many questions...
March 15, 2017: Advances in Experimental Medicine and Biology
https://www.readbyqxmd.com/read/28293191/an-exploration-of-charge-compensating-ion-channels-across-the-phagocytic-vacuole-of-neutrophils
#5
Juliet R Foote, Philippe Behe, Mathew Frampton, Adam P Levine, Anthony W Segal
Neutrophils phagocytosing bacteria and fungi exhibit a burst of non-mitochondrial respiration that is required to kill and digest the engulfed microbes. This respiration is accomplished by the movement of electrons across the wall of the phagocytic vacuole by the neutrophil NADPH oxidase, NOX2. In this study, we have attempted to identify the non-proton ion channels or transporters involved in charge compensation by examining the effect of inhibitors on vacuolar pH and cross-sectional area, and on oxygen consumption...
2017: Frontiers in Pharmacology
https://www.readbyqxmd.com/read/28289711/the-volume-regulated-anion-channel-lrrc8-in-nodose-neurons-is-sensitive-to-acidic-ph
#6
Runping Wang, Yongjun Lu, Susheel Gunasekar, Yanhui Zhang, Christopher J Benson, Mark W Chapleau, Rajan Sah, François M Abboud
The leucine rich repeat containing protein 8A (LRRC8A), or SWELL1, is an essential component of the volume-regulated anion channel (VRAC) that is activated by cell swelling and ionic strength. We report here for the first time to our knowledge its expression in a primary cell culture of nodose ganglia neurons and its localization in the soma, neurites, and neuronal membrane. We show that this neuronal VRAC/SWELL1 senses low external pH (pHo) in addition to hypoosmolarity. A robust sustained chloride current is seen in 77% of isolated nodose neurons following brief exposures to extracellular acid pH...
March 9, 2017: JCI Insight
https://www.readbyqxmd.com/read/28285851/ivermectin-old-drug-new-tricks
#7
REVIEW
Roz Laing, Victoria Gillan, Eileen Devaney
Ivermectin is one of the most important drugs in veterinary and human medicine for the control of parasitic infection and was the joint focus of the 2015 Nobel Prize in Physiology or Medicine, some 35 years after its remarkable discovery. Although best described for its activity on glutamate-gated chloride channels in parasitic nematodes, understanding of its mode of action remains incomplete. In the field of veterinary medicine, resistance to ivermectin is now widespread, but the mechanisms underlying resistance are unresolved...
March 9, 2017: Trends in Parasitology
https://www.readbyqxmd.com/read/28280458/jmv5656-a-novel-derivative-of-tlqp-21-triggers-the-activation-of-a-calcium-dependent-potassium-outward-current-in-microglial-cells
#8
Ilaria Rivolta, Anna Binda, Laura Molteni, Laura Rizzi, Elena Bresciani, Roberta Possenti, Jean-Alain Fehrentz, Pascal Verdié, Jean Martinez, Robert J Omeljaniuk, Vittorio Locatelli, Antonio Torsello
TLQP-21 (TLQPPASSRRRHFHHALPPAR) is a multifunctional peptide that is involved in the control of physiological functions, including feeding, reproduction, stress responsiveness, and general homeostasis. Despite the huge interest in TLQP-21 biological activity, very little is known about its intracellular mechanisms of action. In microglial cells, TLQP-21 stimulates increases of intracellular Ca(2+) that may activate functions, including proliferation, migration, phagocytosis and production of inflammatory molecules...
2017: Frontiers in Cellular Neuroscience
https://www.readbyqxmd.com/read/28274876/hypotonic-stress-promotes-atp-release-reactive-oxygen-species-production-and-cell-proliferation-via-trpv4-activation-in-rheumatoid-arthritis-rat-synovial-fibroblasts
#9
Fen Hu, Zhenhai Hui, Wei Wei, Jianyu Yang, Ziyuan Chen, Bu Guo, Fulin Xing, Xinzheng Zhang, Leiting Pan, Jingjun Xu
Rheumatoid arthritis (RA) is a chronic and systemic autoimmune-disease with complex and unclear etiology. Hypotonicity of synovial fluid is a typical characteristic of RA, which may play pivotal roles in RA pathogenesis. In this work, we studied the responses of RA synovial fibroblasts to hypotonic stress in vitro and further explored the underlying mechanisms. Data showed that hyposmotic solutions significantly triggered increases in cytosolic calcium concentration ([Ca(2+)]c) of synoviocytes. Subsequently, it caused rapid release of ATP, as well as remarkable production of intracellular reactive oxygen species (ROS)...
March 6, 2017: Biochemical and Biophysical Research Communications
https://www.readbyqxmd.com/read/28267675/international-union-of-basic-and-clinical-pharmacology-c-nomenclature-and-properties-of-calcium-activated-and-sodium-activated-potassium-channels
#10
REVIEW
Leonard K Kaczmarek, Richard W Aldrich, K George Chandy, Stephan Grissmer, Aguan D Wei, Heike Wulff
A subset of potassium channels is regulated primarily by changes in the cytoplasmic concentration of ions, including calcium, sodium, chloride, and protons. The eight members of this subfamily were originally all designated as calcium-activated channels. More recent studies have clarified the gating mechanisms for these channels and have documented that not all members are sensitive to calcium. This article describes the molecular relationships between these channels and provides an introduction to their functional properties...
January 2017: Pharmacological Reviews
https://www.readbyqxmd.com/read/28259964/effect-of-chloride-channel-activity-on-retinal-pigment-cell-proliferation-and-migration
#11
Jing Zhao, Wei Zhong, Lixia Sun, Yuan Yin, Yajuan Zheng
The present study aimed to investigate the effects of chloride channels (ClC) on the proliferation and migration of retinal pigment epithelial (RPE) cells, a primary component of proliferative vitreoretinopathy (PVR) membranes. An RPE cell model of phagocytosis was established using fibronectin‑coated latex beads. Cell proliferation was measured by live cell counting. The cell cycle and phagocytosis index was assessed by flow cytometry. Intracellular calcium concentration was quantified using Fura‑2‑acetoxymethyl ester...
February 14, 2017: Molecular Medicine Reports
https://www.readbyqxmd.com/read/28257396/maxi-anion-channels-play-a-key-role-in-glutamate-induced-atp-release-from-mouse-astrocytes-in-primary-culture
#12
Bin Zhao, Li Gu, Kaixi Liu, Mingming Zhang, Hongtao Liu
Astrocytes are an abundant source of ATP, which might be released from the cytosol into extracellular spaces under various conditions and even affect cell fate under some circumstances. In the present study, we aimed to evaluate the pathway(s) contributing toward glutamate-induced ATP release from mouse astrocytes. Firstly, our study of cultured astrocytes showed marked ATP release in response to stimuli of glutamate at different concentrations (0.1-1 mM), with an interesting bimodal distribution in time course...
March 2, 2017: Neuroreport
https://www.readbyqxmd.com/read/28256198/calcium-activated-chloride-channels-as-a-new-target-to-control-the-spiking-pattern-of-neurons
#13
Go Eun Ha, Eunji Cheong
Neuronal firing patterns and frequencies determine the nature of encoded information in the neural circuits. Here we discuss the molecular identity and cellular mechanisms of spike-frequency adaptation in central nervous system (CNS). Spike-frequency adaptation in thalamocortical (TC) and CA1 hippocampal neurons is mediated by the Ca2+-activated Cl- channel (CACC) anoctamin-2 (ANO2). Knockdown of ANO2 in these neurons results in significantly reduced spike-frequency adaptation along with increased number of spikes...
March 3, 2017: BMB Reports
https://www.readbyqxmd.com/read/28255969/-optogenetics-a-therapeutic-option-for-advanced-retinal-dystrophies
#14
A Swiersy, S D Klapper, V Busskamp
Optogenetics refers to the genetic modification of cells to express light-sensitive proteins, which mediate ion flow or secondary signalling cascades upon light exposure. Channelrhodopsin, the most famous example, is an unselective cation channel, which opens when exposed to blue light, thus mediating the depolarisation of the expressing cell. Along with other light-sensitive proteins such as the chloride pump eNpHR, which mediates light-activated hyperpolarisation, the optogenetic toolset offers a wide range of non-invasive single cell manipulations...
March 2, 2017: Klinische Monatsblätter Für Augenheilkunde
https://www.readbyqxmd.com/read/28255270/activated-clc-2-inhibits-p-akt-to-repress-myelination-in-gdm-newborn-rats
#15
Feixiang He, Yuchen Peng, Zhi Yang, Zilu Ge, Yanping Tian, Teng Ma, Hongli Li
This study aims to investigate the effect and mechanism of type 2 voltage-gated chloride channel (ClC-2) on myelin development of newborn rats' cerebral white matter with gestational diabetes mellitus (GDM). In this study, GDM model was induced in late pregnant rat model. The alteration of ClC-2 expression in various developmental stages of cerebral white matter with/without being exposed to high glucose was analyzed using RT-PCR, active oxygen detection, TUNEL staining, Western Blot as well as immuno-histochemical staining...
2017: International Journal of Biological Sciences
https://www.readbyqxmd.com/read/28242698/synergy-of-camp-and-calcium-signaling-pathways-in-cftr-regulation
#16
Zoltan Bozoky, Saumel Ahmadi, Tal Milman, Tae Hun Kim, Kai Du, Michelle Di Paola, Stan Pasyk, Roman Pekhletski, Jacob P Keller, Christine E Bear, Julie D Forman-Kay
Cystic fibrosis results from mutations in the cystic fibrosis transmembrane conductance regulator (CFTR) chloride channel, leading to defective apical chloride transport. Patients also experience overactivation of inflammatory processes, including increased calcium signaling. Many investigations have described indirect effects of calcium signaling on CFTR or other calcium-activated chloride channels; here, we investigate the direct response of CFTR to calmodulin-mediated calcium signaling. We characterize an interaction between the regulatory region of CFTR and calmodulin, the major calcium signaling molecule, and report protein kinase A (PKA)-independent CFTR activation by calmodulin...
February 27, 2017: Proceedings of the National Academy of Sciences of the United States of America
https://www.readbyqxmd.com/read/28225032/4-isopropylcyclohexanol-has-potential-analgesic-effects-through-the-inhibition-of-anoctamin-1-trpv1-and-trpa1-channel-activities
#17
Yasunori Takayama, Hidemasa Furue, Makoto Tominaga
Interactions between calcium-activated chloride channel anoctamin 1 (ANO1) and transient receptor potential vanilloid 1 (TRPV1) enhance pain sensations in mice, suggesting that ANO1 inhibition could have analgesic effects. Here we show that menthol and the menthol analogue isopropylcyclohexane (iPr-CyH) inhibited ANO1 channels in mice. The iPr-CyH derivative 4-isopropylcyclohexanol (4-iPr-CyH-OH) inhibited mouse ANO1 currents more potently than iPr-CyH. Moreover, 4-iPr-CyH-OH inhibited the activities of TRPV1, TRP ankyrin 1 (TRPA1), TRP melastatin 8 (TRPM8) and TRPV4...
February 22, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28223230/myotoxicity-of-statins-mechanism-of-action
#18
REVIEW
Patrick du Souich, Ghislaine Roederer, Robert Dufour
Statins are effective drugs to reduce cardiovascular events secondary to dyslipidemia; however, they cause frequent undesirable side effects. The incidence of statin-induced myotoxicity (SIM) is presented by 7 to 29% of patients, depending upon the report. SIM may develop in presence of abnormally high concentrations of statins in the myocyte and/or in presence of muscular conditions that may predispose to SIM. High concentrations of statins in the myocyte may occur whenever the activity of liver influx membrane transporters, namely OATP1B1, of drug metabolizing enzymes, and of liver and muscular efflux transporters, MDR1 and BCRP, is reduced...
February 14, 2017: Pharmacology & Therapeutics
https://www.readbyqxmd.com/read/28218274/trapping-of-ivermectin-by-a-pentameric-ligand-gated-ion-channel-upon-open-to-closed-isomerization
#19
Nurit Degani-Katzav, Moshe Klein, Moran Har-Even, Revital Gortler, Ruthi Tobi, Yoav Paas
Ivermectin (IVM) is a broad-spectrum anthelmintic drug used to treat human parasitic diseases like river blindness and lymphatic filariasis. By activating invertebrate pentameric glutamate-gated chloride channels (GluCl receptors; GluClRs), IVM induces sustained chloride influx and long-lasting membrane hyperpolarization that inhibit neural excitation in nematodes. Although IVM activates the C. elegans heteromeric GluClα/β receptor, it cannot activate a homomeric receptor composed of the C. elegans GluClβ subunits...
February 20, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28217875/mechanisms-of-pruritogen-induced-activation-of-itch-nerves-in-isolated-mouse-skin
#20
F Ru, H Sun, D Jurcakova, R A Herbstsomer, J Meixong, X Dong, B J Undem
Chloroquine (CQ) and histamine are pruritogens commonly used to study itch in the mouse. A novel skin-nerve preparation was used to evaluate chloroquine (CQ)- and histamine- induced activation of afferent nerves in the dorsal thoracic skin of the mouse. All CQ sensitive nerves were C-fibres, and were also sensitive to histamine. The response to CQ, but not histamine, was largely absent in mrgpr cluster Δ -/- mice supporting the hypothesis that CQ evokes itch largely via stimulation of MrgprA3 receptors. The CQ-induced action potential discharge was largely absent in phospholipase Cβ3 knockout animals...
February 19, 2017: Journal of Physiology
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