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chloride channel activators

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https://www.readbyqxmd.com/read/28924007/multiple-signaling-pathways-coordinately-regulate-forgetting-of-olfactory-adaptation-through-control-of-sensory-responses-in-c-elegans
#1
Tomohiro Kitazono, Sayuri Hara-Kuge, Osamu Matsuda, Akitoshi Inoue, Manabi Fujiwara, Takeshi Ishihara
Forgetting memories is important for animals to properly respond to continuously changing environments. To elucidate the mechanisms of forgetting, we used one of the behavioral plasticities of C. elegans hermaphrodite, olfactory adaptation to an attractive odorant, diacetyl, as a simple model of learning. In C. elegans, the TIR-1/JNK-1 pathway accelerates forgetting of olfactory adaptation by facilitating neural secretion from AWC sensory neurons. In this study, to identify the downstream effectors of the TIR-1/JNK-1 pathway, we conducted a genetic screen for suppressors of the gain-of-function mutant of tir-1 (ok1052), which shows excessive forgetting...
September 18, 2017: Journal of Neuroscience: the Official Journal of the Society for Neuroscience
https://www.readbyqxmd.com/read/28922372/reduction-of-organelle-motility-by-removal-of-potassium-and-other-solutes
#2
John W Murray, David Yin, Allan W Wolkoff
There are surprisingly few studies that describe how the composition of cell culture medium may affect the trafficking of organelles. Here we utilize time lapse multi-channel fluorescent imaging to show that short term exposure of Huh-7 cells to medium lacking potassium, sodium, or chloride strongly reduces but does not eliminate the characteristic back and forth and cell-traversing movement of fluorescent EGF (FL-EGF) containing organelles. We focused on potassium because of its relatively low abundance in media and serum and its energy requiring accumulation into cells...
2017: PloS One
https://www.readbyqxmd.com/read/28920462/involvement-of-atrial-natriuretic-peptide-in-abrogated-cardioprotective-effect-of-ischemic-preconditioning-in-ovariectomized-rat-heart
#3
V K Vishwakarma, A Goyal, J K Gupta, P K Upadhyay, H N Yadav
BACKGROUND: Nitric oxide (NO) is an effective mediator of ischemic preconditioning (IPC)-induced cardioprotection. Atrial natriuretic peptide (ANP) is downregulated after ovariectomy, which results in reduction in the level of NO. The present study deals with the investigation of the role of ANP in abrogated cardioprotective effect of IPC in the ovariectomized rat heart. METHODS: Heart was isolated from ovariectomized rat and mounted on Langendorff's apparatus, subjected to 30 min of ischemia and 120 min of reperfusion...
January 1, 2017: Human & Experimental Toxicology
https://www.readbyqxmd.com/read/28919489/zinc-chloride-induced-trpa1-activation-does-not-contribute-to-toxicity-in-vitro
#4
Dirk Steinritz, Franziska Zehfuß, Bernhard Stenger, Annette Schmidt, Tanja Popp, Kai Kehe, Harald Mückter, Horst Thiermann, Thomas Gudermann
The hygroscopic zinc chloride (ZnCl2) is often used to generate smoke screens. Severe adverse pulmonary health effects have been associated with inhalation of ZnCl2 smokes. The underlying molecular toxicology is not known. Recent studies have shown that the Transient Receptor Potential Channel A1 (TRPA1) is important for sensing toxic chemicals. TRPA1 was shown to be activated by Zn(2+) which was linked to pain and inflammation. In the present study, we investigated whether TRPA1 activation contributes to ZnCl2-mediated toxicity in vitro...
September 14, 2017: Toxicology Letters
https://www.readbyqxmd.com/read/28902351/anoctamin5-regulates-cell-migration-and-invasion-in-thyroid-cancer
#5
Zhengyan Chang, Chunmiao Cai, Dongyan Han, Yaohui Gao, Qianyu Li, Lijin Feng, Wei Zhang, Jiayi Zheng, Jiaoying Jin, Huizhen Zhang, Qing Wei
Anoctamin/TMEM16 family members have recently been identified as novel calcium-activated chloride channels, and dysregulation of many family members participates in tumorigenesis and progression. However, the exact role of anoctamin5 (ANO5), one member of this family, in thyroid cancer is still not clarified. In this study, we firstly found that the expression levels of ANO5 was significantly downregulated in thyroid cancer compared to adjacent normal tissue by mining the public GEO database. Subsequently, we further demonstrated that the expression levels of ANO5 was significantly downregulated in 69...
October 2017: International Journal of Oncology
https://www.readbyqxmd.com/read/28900649/ionic-effects-on-the-proton-transfer-mechanism-in-aqueous-solutions
#6
Joonyoung F Joung, Sangin Kim, Sungnam Park
Proton dissociation (PD) reactions of weak acids and proton transfer (PT) processes in aqueous solutions are strongly influenced by ions. However, a detailed molecular picture that describes how ions affect the rates of PD and PT processes is still missing. Here, we utilize time-resolved fluorescence spectroscopy combined with quantum chemical calculations to investigate the excited-state proton transfer (ESPT) reaction of a photoacid in aqueous metal chloride solutions. The activation energy (Ea) for the ESPT of the photoacid increases with increasing charge density of cations (ρcat)...
September 13, 2017: Physical Chemistry Chemical Physics: PCCP
https://www.readbyqxmd.com/read/28899969/tmem16a-ano1-inhibits-apoptosis-via-down-regulation-of-bim-expression
#7
Neal R Godse, Nayel I Khan, Zachary A Yochum, Roberto Gomez-Casal, Carolyn Kemp, Daniel J Shiwarski, Raja Seethala, Scott Kulich, Mukund Seshadri, Timothy F Burns, Umamaheswar Duvvuri
PURPOSE: TMEM16A is a calcium-activated chloride channel that is amplified in a variety of cancers, including 30% of head and neck squamous cell carcinomas (HNSCC), raising the possibility of an anti-apoptotic role in malignant cells. The present study investigated this using a multi-modal, translational investigation. EXPERIMENTAL DESIGN: Combination of 1) in vitro HNSCC cell culture experiments assessing cell viability, apoptotic activation, and protein expression 2) in vivo studies assessing similar outcomes, and 3) molecular and staining analysis of human HNSCC samples...
September 12, 2017: Clinical Cancer Research: An Official Journal of the American Association for Cancer Research
https://www.readbyqxmd.com/read/28893247/cell-specific-mechanisms-of-tmem16a-ca-2-activated-chloride-channel-in-cancer
#8
REVIEW
Hui Wang, Liang Zou, Ke Ma, Jiankun Yu, Huizhe Wu, Minjie Wei, Qinghuan Xiao
TMEM16A (known as anoctamin 1) Ca(2+)-activated chloride channel is overexpressed in many tumors. TMEM16A overexpression can be caused by gene amplification in many tumors harboring 11q13 amplification. TMEM16A expression is also controlled in many cancer cells via transcriptional regulation, epigenetic regulation and microRNAs. In addition, TMEM16A activates different signaling pathways in different cancers, e.g. the EGFR and CAMKII signaling in breast cancer, the p38 and ERK1/2 signaling in hepatoma, the Ras-Raf-MEK-ERK1/2 signaling in head and neck squamous cell carcinoma and bladder cancer, and the NFκB signaling in glioma...
September 11, 2017: Molecular Cancer
https://www.readbyqxmd.com/read/28887352/a-single-amino-acid-substitution-in-the-third-transmembrane-region-has-opposite-impacts-on-the-selectivity-of-the-parasiticides-fluralaner-and-ivermectin-for-ligand-gated-chloride-channels
#9
Yunosuke Nakata, Toshinori Fuse, Kohei Yamato, Miho Asahi, Kunimitsu Nakahira, Fumiyo Ozoe, Yoshihisa Ozoe
Fluralaner (BravectoTM) is a recently marketed isoxazoline ectoparasiticide. This compound potently inhibits γ-aminobutyric acid (GABA)-gated chloride channels (GABACls) and less potently glutamate-gated chloride channels (GluCls) in insects. The mechanism underlying this selectivity is unknown. Therefore, we sought to identify the amino acid residue(s) causing the low potency of fluralaner toward GluCls. We examined the fluralaner sensitivity of mutant housefly (Musca domestica) GluCls in which amino acid residues in the transmembrane subunit interface (TSI) were replaced with the positionally equivalent amino acids of Musca GABACls...
September 8, 2017: Molecular Pharmacology
https://www.readbyqxmd.com/read/28887112/protein-and-lipid-interactions-modulating-cftr-trafficking-and-rescue
#10
Carlos M Farinha, Elizabeth Miller, Nael McCarty
Different levels of CFTR regulation in the cell contribute to a stringent control of chloride secretion in epithelia. Tuning of chloride transport is achieved by modulating CFTR biogenesis, exit from the endoplasmic reticulum, trafficking, membrane stability and channel activity. In this short review, we summarize recent findings identifying interactions with other proteins - directly or through membrane lipids - and briefly discuss how these observations can provide clues to the design of better therapeutic approaches...
September 5, 2017: Journal of Cystic Fibrosis: Official Journal of the European Cystic Fibrosis Society
https://www.readbyqxmd.com/read/28875346/cftr-supports-cell-death-through-ros-dependent-activation-of-tmem16f-anoctamin-6
#11
Filipa Simões, Jiraporn Ousingsawat, Podchanart Wanitchakool, Ana Fonseca, Inês Cabrita, Roberta Benedetto, Rainer Schreiber, Karl Kunzelmann
Cystic fibrosis transmembrane conductance regulator (CFTR) is the essential chloride and bicarbonate channel in the apical membrane of epithelial cells. CFTR was also proposed earlier to conduct glutathione (GSH) out of airway epithelial cells to be enriched in the apical airway surface liquid to neutralize reactive oxygen species (ROS). Although earlier studies suggested that release of GSH by wild type (wt) CFTR may lead to an increase in cytosolic ROS, we did not detect different ROS levels in cells expressing wt-CFTR and mutant F508del-CFTR, independent of CFTR-activation or exposure to the ROS donor tert-butyl hydroperoxide...
September 5, 2017: Pflügers Archiv: European Journal of Physiology
https://www.readbyqxmd.com/read/28873176/pro-secretory-activity-and-pharmacology-in-rabbits-of-an-aminophenyl-1-3-5-triazine-cftr-activator-for-dry-eye-disorders
#12
Christian M Felix, Sujin Lee, Marc H Levin, Alan S Verkman
Purpose: Pharmacological activation of ocular surface cystic fibrosis transmembrane conductance regulator (CFTR) chloride channels is a potential pro-secretory approach to treat dry eye disorders. We previously reported the discovery of aminophenyl-1,3,5-triazines, one of which, N-methyl-N-phenyl-6-(2,2,3,3-tetrafluoropropoxy)-1,3,5-triazine-2,4-diamine (herein called CFTRact-K267), fully activated human wildtype CFTR with EC50 ∼ 30 nM and increased tear volume for 8 hours in mice. Here, functional and pharmacological studies of CFTRact-K267 were done in adult New Zealand white rabbits...
September 1, 2017: Investigative Ophthalmology & Visual Science
https://www.readbyqxmd.com/read/28869532/cftr-nherf2-lpa%C3%A2-complex-in-the-airway-and-gut-epithelia
#13
REVIEW
Weiqiang Zhang, Zhihong Zhang, Yanhui Zhang, Anjaparavanda P Naren
The cystic fibrosis transmembrane conductance regulator (CFTR) is a cAMP- and cGMP-regulated chloride (Cl(-)) and bicarbonate (HCO₃(-)) channel localized primarily at the apical plasma membrane of epithelial cells lining the airway, gut and exocrine glands, where it is responsible for transepithelial salt and water transport. Several human diseases are associated with altered CFTR channel function. Cystic fibrosis (CF) is caused by the absence or dysfunction of CFTR channel activity, resulting from mutations in the gene...
September 4, 2017: International Journal of Molecular Sciences
https://www.readbyqxmd.com/read/28862243/association-of-anti-clic2-and-anti-hmgb1-autoantibodies-with-higher-disease-activity-in-systemic-lupus-erythematosus-patients
#14
C S Syahidatulamali, W G Wan Syamimee, Y Nor Azwany, K K Wong, C H Che Maraina
BACKGROUND: Systemic lupus erythematosus (SLE) is a systemic autoimmune disease characterized by numerous autoantibodies. In this study, we investigated the presence of anti-chloride intracellular channel 2 (anti-CLIC2) and anti-high mobility group box 1 (anti-HMGB1) autoantibodies in SLE patients (n = 43) versus healthy controls ([HCs] n = 43), and their association with serological parameters (antinuclear antibody [ANA], anti-double-stranded DNA [anti-dsDNA], and C-reactive protein [CRP]) and disease activity using Systemic Lupus Erythematosus Disease Activity Index (SLEDAI) score (active or inactive)...
August 31, 2017: Journal of Postgraduate Medicine
https://www.readbyqxmd.com/read/28852814/identification-of-resveratrol-an-herbal-compound-as-an-activator-of-the-calcium-activated-chloride-channel-tmem16a
#15
Ran Chai, Yafei Chen, Hongbo Yuan, Xuzhao Wang, Shuai Guo, Jinlong Qi, Hailin Zhang, Yong Zhan, Hailong An
Calcium-activated chloride channels (CaCCs) play vital roles in a variety of physiological processes. Dysfunction of the CaCCs is implicated in many diseases. Drug discovery targeting at CaCCs has recently become possible with the determination that TMEM16A is the molecular identity of CaCCs. In this study, we demonstrated that resveratrol (RES), a Chinese traditional medicine compound, is a novel activator of TMEM16A. The yellow fluorescence protein quenching assay and measurement of intracellular calcium fluorescence intensity show that RES activates TMEM16A channels in an intracellular Ca(2+)-independent way...
August 29, 2017: Journal of Membrane Biology
https://www.readbyqxmd.com/read/28832263/vasorelaxant-properties-of-vernonia-amygdalina-ethanol-extract-and-its-possible-mechanism
#16
Yung Sing Ch'ng, Yean Chun Loh, Chu Shan Tan, Mariam Ahmad, Mohd Zaini Asmawi, Wan Maznah Wan Omar, Mun Fei Yam
CONTEXT: Vernonia amygdalina Del. (VA) (Asteraceae) is commonly used to treat hypertension in Malaysia. OBJECTIVE: This study investigates the vasorelaxant mechanism of VA ethanol extract (VAE) and analyzes its tri-step FTIR spectroscopy fingerprint. MATERIALS AND METHODS: Dried VA leaves were extracted with ethanol through maceration and concentrated using rotary evaporator before freeze-dried. The vasorelaxant activity and the underlying mechanisms of VAE using the cumulative concentration (0...
December 2017: Pharmaceutical Biology
https://www.readbyqxmd.com/read/28808008/mathematical-model-reveals-role-of-nucleotide-signaling-in-airway-surface-liquid-homeostasis-and-its-dysregulation-in-cystic-fibrosis
#17
Conner I Sandefur, Richard C Boucher, Timothy C Elston
Mucociliary clearance is composed of three components (i.e., mucin secretion, airway surface hydration, and ciliary-activity) which function coordinately to clear inhaled microbes and other foreign particles from airway surfaces. Airway surface hydration is maintained by water fluxes driven predominantly by active chloride and sodium ion transport. The ion channels that mediate electrogenic ion transport are regulated by extracellular purinergic signals that signal through G protein-coupled receptors. These purinoreceptors and the signaling pathways they activate have been identified as possible therapeutic targets for treating lung disease...
August 29, 2017: Proceedings of the National Academy of Sciences of the United States of America
https://www.readbyqxmd.com/read/28803966/a-chimeric-prokaryotic-eukaryotic-pentameric-ligand-gated-ion-channel-reveals-interactions-between-the-extracellular-and-transmembrane-domains-shape-neurosteroid-modulation
#18
Borna Ghosh, Tzu-Wei Tsao, Cynthia Czajkowski
Pentameric ligand-gated ion channels (pLGICs) are the targets of several clinical and endogenous allosteric modulators including anesthetics and neurosteroids. Molecular mechanisms underlying allosteric drug modulation are poorly understood. Here, we constructed a chimeric pLGIC by fusing the extracellular domain (ECD) of the proton-activated, cation-selective bacterial channel GLIC to the transmembrane domain (TMD) of the human ρ1 chloride-selective GABAAR, and tested the hypothesis that drug actions are regulated locally in the domain that houses its binding site...
October 2017: Neuropharmacology
https://www.readbyqxmd.com/read/28802235/steviol-stabilizes-polycystin-1-expression-and-promotes-lysosomal-degradation-of-cftr-and-%C3%AE-catenin-proteins-in-renal-epithelial-cells
#19
Chaowalit Yuajit, Chatchai Muanprasat, Sureeporn Homvisasevongsa, Varanuj Chatsudthipong
Malfunction of polycystin 1 (PC1) is linked to abnormally high epithelial cell proliferation and fluid secretion, eventually leading to renal cyst development and declined renal function as found in autosomal dominant polycystic kidney disease (ADPKD). Currently, there is no effective therapy for ADPKD. Recent studies report PC1 regulates CFTR chloride channels and β-catenin levels in normal renal epithelial cells. Concurrently, our previous study found steviol retarded renal cyst enlargement in an in vitro and in an in vivo models by reducing CFTR expression and activity...
October 2017: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
https://www.readbyqxmd.com/read/28798690/risk-of-myopathy-in-patients-in-therapy-with-statins-identification-of-biological-markers-in-a-pilot-study
#20
Giulia M Camerino, Olimpia Musumeci, Elena Conte, Kejla Musaraj, Adriano Fonzino, Emanuele Barca, Marco Marino, Carmelo Rodolico, Domenico Tricarico, Claudia Camerino, Maria R Carratù, Jean-François Desaphy, Annamaria De Luca, Antonio Toscano, Sabata Pierno
Statin therapy may induce skeletal muscle damage ranging from myalgia to severe rhabdomyolysis. Our previous preclinical studies showed that statin treatment in rats involves the reduction of skeletal muscle ClC-1 chloride channel expression and related chloride conductance (gCl). An increase of the activity of protein kinase C theta (PKC theta) isoform, able to inactivate ClC-1, may contribute to destabilize sarcolemma excitability. These effects can be detrimental for muscle function leading to drug-induced myopathy...
2017: Frontiers in Pharmacology
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